The effect of an anti-malarial herbal remedy, Maytenus senegalensis, on electrocardiograms of healthy Tanzanian volunteers.

BACKGROUND: The emergence of resistance to artemisinin-based combination therapy necessitates the search for new, more potent antiplasmodial compounds, including herbal remedies. The whole extract of Maytenus senegalensis has been scientifically investigated for potential biological activities both in vitro and in vivo, demonstrating strong antimalarial activity. However, there is a lack of data on the electrocardiographic effects of M. senegalensis in humans, which is a crucial aspect in the investigation of malaria treatment. Assessing the electrocardiographic effects of M. senegalensis is essential, as many anti-malarial drugs can inadvertently prolong the QT interval on electrocardiograms. Therefore, the study's objective was to evaluate the electrocardiographic effects of M. senegalensis in healthy adult volunteers. METHODS: This study is a secondary analysis of an open-label single-arm dose escalation. Twelve healthy eligible Tanzanian males, aged 18 to 45, were enrolled in four study dose groups. A single 12-lead electrocardiogram (ECG) was performed at baseline and on days 3, 7, 14, 28, and 56. RESULTS: No QTcF adverse events occurred with any drug dose. Only one volunteer who received the highest dose (800 mg) of M. senegalensis experienced a moderate transient change (△QTcF > 30 ms; specifically, the value was 37 ms) from baseline on day 28. There was no difference in maximum QTcF and maximum △QTcF between volunteers in all four study dose groups. CONCLUSIONS: A four-day regimen of 800 mg every 8 h of M. senegalensis did not impact the electrocardiographic parameters in healthy volunteers. This study suggests that M. senegalensis could be a valuable addition to malaria treatment, providing a safer alternative and potentially aiding in the battle against artemisinin-resistant malaria. The results of this study support both the traditional use and the modern therapeutic potential of M. senegalensis. They also set the stage for future research involving larger and more diverse populations to explore the safety profile of M. senegalensis in different demographic groups. This is especially important considering the potential use of M. senegalensis as a therapeutic agent and its widespread utilization as traditional medicine. Trial registration ClinicalTrials.gov, NCT04944966. Registered 30 June 2021-Retrospectively registered, https://clinicaltrials.gov/ct2/show/NCT04944966?term=kamaka&draw=2&rank=1.

Novel guanidine derivatives targeting leukemia as selective Src/Abl dual inhibitors: Design, synthesis and anti-proliferative activity.

A new series of benzene-sulfonamide derivatives 3a-i was designed and synthesized via the reaction of N-(pyrimidin-2-yl)cyanamides 1a-i with sulfamethazine sodium salt 2 as dual Src/Abl inhibitors. Spectral data IR, 1H-, 13C- NMR and elemental analyses were used to confirm the structures of all the newly synthesized compounds 3a-i and 4a-i. Crucially, we screened all the synthesized compounds 3a-i against NCI 60 cancer cell lines. Among all, compound 3b was the most potent, with IC50 of 0.018 µM for normoxia, and 0.001 µM for hypoxia, compared to staurosporine against HL-60 leukemia cell line. To verify the selectivity of this derivative, it was assessed against a panel of tyrosine kinase EGFR, VEGFR-2, B-raf, ERK, CK1, p38-MAPK, Src and Abl enzymes. Results revealed that compound 3b can effectively and selectively inhibit Src/Abl with IC500.25 µM and Abl inhibitory activity with IC500.08 µM, respectively, and was found to be more potent on these enzymes than other kinases that showed the following results: EGFR IC500.31 µM, VEGFR-2 IC500.68 µM, B-raf IC500.33 µM, ERK IC501.41 µM, CK1 IC500.29 µM and p38-MAPK IC500.38 µM. Moreover, cell cycle analysis and apoptosis performed to compound 3b against HL-60 suggesting its antiproliferative activity through Src/Abl inhibition. Finally, molecular docking studies and physicochemical properties prediction for compounds 3b, 3c, and 3 h were carried out to investigate their biological activities and clarify their bioavailability.

Multicomponent reaction for synthesis, molecular docking, and anti-inflammatory evaluation of novel indole-thiazole hybrid derivatives.

In this article, novel thiazol-indolin-2-one derivatives 4a-f have been synthesized via treatment of thiosemicarbazide (1) with some isatin derivative 2a-f and N-(4-(2-bromoacetyl)phenyl)-4-tolyl-sulfonamide (3) under reflux in ethanol in the presence of triethyl amine (TEA). The structures of new products were elucidated by elemental and spectral analyses. Moreover, all compounds were investigated for their in vivo anti-inflammatory activity using celecoxib as a reference drug. The target compound 4b was the most active anti-inflammatory candidate and exhibited higher edema inhibition (EI = 38.50%) than that recorded by celecoxib (EI = 34.58%) after 3 h. Furthermore, the most active compounds 4b and 4f were subjected to a molecular docking study inside COX-2 enzyme to show their binding interactions. Both compounds 4b and 4f showed good fitting into COX-2 binding site with docking energy scores - 11.45 kcal/mol and - 10.48 kcal/mol, respectively which indicated that compound 4b revealed the most promising and effective anti-inflammatory potential.

Design, Characterization and SAR Studies of Novel Bioactive Benzylideneacetophenone Derivatives as Insecticidal Agents against Spodoptera frugiperda (Lepidoptera: Noctuidae).

Unintentional environmental effects brought on by insecticides encourage the creation of safer substitutes. A very polyphagous migrating lepidopteran pest species in Africa called S. Frugiperda causes terrible damage. In the current paper, treatment of 4-acetylphenyl 4-methylbenzenesulfonate with different aromatic aldehydes in the presence of NaOH afforded benzylideneacetophenones. The structure of the newly prepared compounds were proved by different spectroscopic techniques such as IR, 1 H-NMR, 13 C NMR, and elemental analysis. We looked at the association between contact with S. frugiperda and stricture reaction to examine their harmful effect. Additionally, S. frugiperda was used for testing the newly created compounds for their ability to kill insects. The majority of substances have been proven to be effective and promising. It has been found that 4-[3-(4-Methylphenyl)prop-2-enoyl]phenyl-4-methyl benzenesulfonate (4) was the most active with an LC50 =3.46 mg/L of 2nd instar larvae and LC50 =9.45 mg/L of 4th instar larvae. Moreover, some of biological and histopathological aspects of the synthesized products were investigated under laboratory conditions.

Salinity-induced desertification in oasis ecosystems: challenges and future directions.

Salinity-induced desertification is a pressing environmental issue that poses a significant threat to the sustainability of oasis ecosystems worldwide. These ecosystems are vital to the livelihoods of millions of people living in hyper-arid, arid and semi-arid regions, providing essential resources such as food, water and other necessities. However, overexploitation of natural resources, changes in land use and climate change have led to the degradation of these ecosystems, resulting in soil salinisation, waterlogging and other adverse effects. Combating salinity-induced desertification requires a comprehensive approach that addresses both the underlying causes of ecosystem degradation and the direct consequences for local communities. The strategy may include measures for sustainable land use, reforestation and water conservation. It is also essential to involve local communities in these activities and to ensure that their perspectives are heard. The aim of this article is to examine the causes and processes of salinity-induced desertification in oasis ecosystems and the implications for their sustainability. It also examines strategies that are being used to prevent desertification and promote sustainable oasis management. This article aims to raise awareness of this critical issue and to promote action towards a more sustainable future.

Physiological and developmental dysfunctions in the dengue vector Culex pipiens (Diptera: Culicidae) immature stages following treatment with zinc oxide nanoparticles.

The medical value of mosquitoes attracted researchers worldwide to search for a valuable way to control such serious insects. The continuous development of resistance against chemical insecticides pushed toward looking for novel and promising compounds against mosquitoes. In this study, the toxicity and physio-developmental effects of 10-30 nm spherical zinc oxide nanoparticles (ZnONPs) in aqueous suspension was addressed against the first larval instar of Culex pipiens mosquito. The calculated value of LC50 was about 0.892 g/L while the sub lethal concentration LC20 recorded about 0.246 g/L. Larvae treated with ZnONPs suffered reduced growth rate, longer developmental period and malformations in the breathing tube. Furthermore, the treated larvae showed clear abnormal appearance of the gastric caeca and midgut epithelia under transmission electron microscope (TEM). These abnormalities appeared as condensation of the nuclear chromatin, abnormal shape or absence of microvilli, highly increased amount of smooth endoplasmic reticulum in the cytoplasm and appearance of numerous vacuoles. Additionally, ZnONPs interfered with several biochemical pathways such as induction of oxidative stress which appeared in the form of increased levels of hydrogen peroxide and inability to activate the detoxifying enzymes alkaline phosphatase (ALP), catalase and glutathione peroxidase (GPX). On the contrary, the activity of the antioxidant enzyme superoxide dismutase (SOD) increased in treated larvae. Furthermore, LC20 and LC50 of ZnONPs inhibited the growth rate of the larval gut fauna in vitro. These results clearly show that ZnONPs target several tissues leading to serious alteration in the physiological and developmental processes in C. pipiens mosquito larvae.

Design and Synthesis of Pyridine and Thiazole Derivatives as Eco-friendly Insecticidal to Control Olive Pests.

Treatment of p-tosyloxybenzaldehyde (1) with ethyl cyanoacetate afforded ethyl 2-cyano-3-(4-{[(4-methylphenyl)sulfonyl]oxy}phenyl)acrylate (2) which reacted with some active methylene derivatives under microwave irradiation in presence of ammonium acetate yielded pyridine derivatives 3-7. On the other hand, when treatment of compound 1 with thiosemicarbazide gave 4-tosyloxybenzylidenethiosemicarbazone (8), which allowed to react with some active methylene compounds, such as: ethyl bromoacetate, chloroacetonitrile or phenacyl bromide derivatives gave thiazole derivatives 9-13. The structure of all products were confirmed by elemental and spectroscopic analyses such as IR, 1 H-NMR, 13 CNMR and mass spectra. The advanced of this method are short reaction time (3-7 min), excellent yield, pure products, and low-cost processing. In the final category, the toxicological characteristics of all compounds were tested towards Saissetia oleae (Olivier, 1791) (Hemiptera: Coccidae). With respect to the LC50 values. It has been found that compound 3 possesses the highest insecticidal bioefficacy compared with other products, with values of 0.502 and 1.009 ppm, for nymphs and adults female, respectively. This study paves the way towards discovering new materials for potential use as insecticidal active agents.

Enhanced QoS Routing Protocol for an Unmanned Ground Vehicle, Based on the ACO Approach.

Improving models for managing the networks of firefighting unmanned ground vehicles in crowded areas, as a recommendation system (RS), represented a difficult challenge. This challenge comes from the peculiarities of these types of networks. These networks are distinguished by the network coverage area size, frequent network connection failures, and quick network structure changes. The research aims to improve the communication network of self-driving firefighting unmanned ground vehicles by determining the best routing track to the desired fire area. The suggested new model intends to improve the RS regarding the optimum tracking route for firefighting unmanned ground vehicles by employing the ant colony optimization technique. This optimization method represents one of the swarm theories utilized in vehicles ad-hoc networks and social networks. According to the results, the proposed model can enhance the navigation of self-driving firefighting unmanned ground vehicles towards the fire region, allowing firefighting unmanned ground vehicles to take the shortest routes possible, while avoiding closed roads and traffic accidents. This study aids in the control and management of ad-hoc vehicle networks, vehicles of everything, and the internet of things.

Intelligent Traffic Model for Unmanned Ground Vehicles Based on DSDV-AODV Protocol.

Traffic systems have been built as a result of recent technological advancements. In application, dependable communication technology is essential to link any system needs. VANET technology is used to communicate data about intelligent traffic lights, which are focused on infrastructure during traffic accidents and mechanisms to reduce traffic congestion. To ensure reliable data transfer in VANET, appropriate routing protocols must be used. This research aims to improve data transmission in VANETs implemented in intelligent traffic lights. This study investigates the capability of combining the DSDV routing protocol with the routing protocol AODV to boost AODV on an OMNET++ simulator utilizing the 802.11p wireless standard. According to the simulation results obtained by analyzing the delay parameters, network QoS, and throughput on each protocol, the DSDV-AODV routing protocol performs better in three scenarios compared to QoS, delay, and throughput parameters in every scenario that uses network topology adapted to the conditions on the road intersections. The topology with 50 fixed + 50 mobile nodes yields the best results, with 0.00062 s delay parameters, a network QoS of 640 bits/s, and a throughput of 629.437 bits/s. Aside from the poor results on the network QoS parameters, the addition of mobile nodes to the topology influences both the results of delay and throughput metrics.

Fabrication of Antibacterial and Antioxidant ZnO-Impregnated Amine-Functionalized Chitosan Bio-Nanocomposite Membrane for Advanced Biomedical Applications.

Developing a variety of safe and effective functioning wound dressings is a never-ending objective. Due to their exceptional antibacterial activity, biocompatibility, biodegradability, and healing-promoting properties, functionalized chitosan nanocomposites have attracted considerable attention in wound dressing applications. Herein, a novel bio-nanocomposite membrane with a variety of bio-characteristics was created through the incorporation of zinc oxide nanoparticles (ZnONPs) into amine-functionalized chitosan membrane (Am-CS). The developed ZnO@Am-CS bio-nanocomposite membrane was characterized by various analysis tools. Compared to pristine Am-CS, the developed ZnO@Am-CS membrane revealed higher water uptake and adequate mechanical properties. Moreover, increasing the ZnONP content from 0.025 to 0.1% had a positive impact on antibacterial activity against Gram-positive and Gram-negative bacteria. A maximum inhibition of 89.4% was recorded against Escherichia coli, with a maximum inhibition zone of 38 ± 0.17 mm, and was achieved by the ZnO (0.1%)@Am-CS membrane compared to 72.5% and 28 ± 0.23 mm achieved by the native Am-CS membrane. Furthermore, the bio-nanocomposite membrane demonstrated acceptable antioxidant activity, with a maximum radical scavenging value of 46%. In addition, the bio-nanocomposite membrane showed better biocompatibility and reliable biodegradability, while the cytotoxicity assessment emphasized its safety towards normal cells, with the cell viability reaching 95.7%, suggesting its potential use for advanced wound dressing applications.

Pumice as a Novel Natural Heterogeneous Catalyst for the Designation of 3,4-Dihydropyrimidine-2-(1H)-ones/thiones under Solvent-Free Conditions.

In this study, pumice is used as a novel natural heterogeneous catalyst for the synthesis of 3,4-dihydropyrimidine-2-(1H)-ones/thiones via the one-pot multi-component condensation of aromatic aldehydes, urea/thiourea, and ethyl acetoacetate or acetylacetone in excellent yields (up to 98%). The physical and chemical properties of the catalyst were studied. Their geochemical analysis revealed a basaltic composition. Furthermore, X-ray diffraction showed that it is composed of amorphous materials with clinoptilolite and heulandites zeolite minerals in its pores. Moreover, pumice has a porosity range from 78.2-83.9% (by volume) and is characterized by a mesoporous structure (pore size range from 21.1 to 64.5 nm). Additionally, it has a pore volume between 0.00531 and 0.00781 m2/g and a surface area between 0.053 and 1.47 m2/g. The latter facilitated the reaction to proceed in a short time frame as well as in excellent yields. It is worth noting that our strategy tolerates the use of readily available, cheap, non-toxic, and thermally stable pumice catalyst. The reactions proceeded smoothly under solvent-free conditions, and products were isolated without tedious workup procedures in good yields and high purity. Indeed, pumice can be reused for at least five reuse cycles without affecting its activity.

Using Hand-Held Chlorophyll Meters and Canopy Reflectance Sensors for Fertilizer Nitrogen Management in Cereals in Small Farms in Developing Countries.

To produce enough food, smallholder farmers in developing countries apply fertilizer nitrogen (N) to cereals, sometimes even more than the local recommendations. During the last two decades, hand-held chlorophyll meters and canopy reflectance sensors, which can detect the N needs of the crop based on transmission and reflectance properties of leaves through proximal sensing, have been studied as tools for optimizing crop N status in cereals in developing countries. This review aims to describe the outcome of these studies. Chlorophyll meters are used to manage fertilizer N to maintain a threshold leaf chlorophyll content throughout the cropping season. Despite greater reliability of the sufficiency index approach, the fixed threshold chlorophyll content approach has been investigated more for using chlorophyll meters in rice and wheat. GreenSeeker and Crop Circle crop reflectance sensors take into account both N status and biomass of the crop to estimate additional fertilizer N requirement but only a few studies have been carried out in developing countries to develop N management strategies in rice, wheat and maize. Both chlorophyll meters and canopy reflectance sensors can increase fertilizer N use efficiency by reduction of N rates. Dedicated economic analysis of the proximal sensing strategies for managing fertilizer N in cereals in developing countries is not adequately available.

Primary chondro-osseous melanoma (chondrosarcomatous and osteosarcomatous melanoma).

Melanoma can rarely show malignant chondro-osseous differentiation and can cause diagnostic confusion. We report 3 cases of primary melanoma with extensive bone and cartilage matrix. The first case arose in the nasal mucosa of a 72-year-old woman, the second case in the left index finger of a 26-year-old woman and the third case in the left cheek of a 68-year-old woman. In tumors where osseous and chondroid differentiation appear in mucosa and skin, primary melanoma with chondro-osteosarcomatous differentiation should be considered in the differential. Careful histological examination together with clinical correlation and ancillary immunohistochemical studies can ensure the correct diagnosis is made.

The status of maternal and newborn health care services in Zanzibar.

BACKGROUND: It is estimated that 287,000 women worldwide die annually from pregnancy and childbirth-related conditions, and 6.9 million under-five children die each year, of which about 3 million are newborns. Most of these deaths occur in sub-Saharan Africa. The maternal health situation in Tanzania mainland and Zanzibar is similar to other sub-Saharan countries. This study assessed the availability, accessibility and quality of emergency obstetric care services and essential resources available for maternal and child health services in Zanzibar. METHODS: From October and November 2012, a cross-sectional health facility survey was conducted in 79 health facilities in Zanzibar. The health facility tools developed by the Averting Maternal Death and Disability program were adapted for local use. RESULTS: Only 7.6 % of the health facilities qualified as functioning basic EmONC (Emergency Obstetric and Neonatal Care) facilities and 9 % were comprehensive EmONC facilities. Twenty-eight percent were partially performing basic EmONC and the remaining 55.7 % were not providing EmONC. Neonatal resuscitation was performed in 80 % of the hospitals and only 17.4 % of the other health facilities that were surveyed. Based on World Health Organisation (WHO) criteria, the study revealed a gap of 20 % for minimum provision of EmONC facilities per 500,000 population. The met need at national level (proportion of women with major direct obstetric complications treated in a health facility providing EmONC) was only 33.1 % in the 12 months preceding the survey. The study found that there was limited availability of human resources in all visited health facilities, particularly for the higher cadres, as per Zanzibar minimum staff requirements. CONCLUSION: There is a need to strengthen human resource capacity at primary health facilities through training of health care providers to improve EmONC services, as well as provision of necessary equipment and supplies to reduce workload at the higher referral health facilities and increase geographic access.

The antitrichomonal efficacy of garlic and metronidazole against Trichomonas gallinae infecting domestic pigeons.

Trichomonas gallinae is the causative agent of canker in pigeon. This work was carried out to investigate in the vitro and in vivo efficacy of aqueous water extract of garlic (AGE) on the growth of T. gallinae infecting pigeons compared to those of metronidazole (MTZ). MTZ and AGE were added, at different concentrations, to glucose-serum broth medium containing 1 × 10(4) trophozoites/ml. In the in vivo experiment, 48 squabs were grouped into four groups. The first group (gr. I) was not infected and not treated. Each squab of the other group was infected with 1 × 10(4) trophozoites. The second group (gr. II) was infected and not treated. On day 0, the third group (gr. III) was treated with MTZ (50 mg/kg BW) and the fourth group (gr. IV) was treated with AGE (200 mg/kg BW) for seven successive days in drinking water. In vitro study revealed that the MLC, 24, 48, and 72 h post treatment were 50, 25, and 12.5 µg/ml, respectively, for MTZ and 75, 50, and 50 mg/ml, respectively, for AGE. Garlic (200 mg/kg BW) had the highest antitrichomonal effect and shortened course of treatment of pigeons from 7 days in gr. III to 5 days. Squabs in gr. II suffered from macrocytic hypochromic anemia, whereas squabs in grs. III and IV showed normal blood pictures. Serum total protein, albumin, and globulin were increased, whereas AST, ALT, and the total cholesterol were decreased in grs. III and IV when compared to those of gr. II. Pigeons protected with AGE showed increased body weight and reduced mortality percentage than the other groups. Our results indicated that garlic may be a promising phytotherapeutic agent for protection against trichomoniasis in pigeons.

(2E)-2-(1,3-Benzo-thia-zol-2-yl)-3-(di-methyl-amino)-prop-2-ene-nitrile.

The mol-ecular conformation of title compound, C12H11N3S, is almost planar [maximum deviation = 0.063 (2) Å]; an intra-molecular C-H⋯N hydrogen bond is noted. In the crystal, mol-ecules inter-act with each other via π-π stacking inter-actions between thia-zole rings [centroid-centroid distance = 3.7475 (9) Å] and methyl-H⋯π(C6) inter-actions, forming columns along the a axis.

N-(2-Hy-droxy-phen-yl)-4-methyl-benzene-sulfonamide.

In the title compound, C13H13NO3S, the dihedral angle between the benzene rings is 64.15 (7)° and the C-S-N-C torsion angle is -57.18 (12)°. An intra-molecular N-H⋯O hydrogen bond closes an S(5) ring. In the crystal, O-H⋯O hydrogen bonds link the mol-ecules into C(8) chains propagating in [100]. Weak C-H⋯π inter-actions are also observed.

A selective colorimetric chemosensor for detecting Ni(II) in aqueous solutions based on 4-[{[4-(3-chlorophenyl)-1,3-thiazol-2-yl]hydrazono}methyl]phenyl 4-methyl benzene sulfonate (CTHMBS).

Among the toxic heavy metals, Ni(II) can cause a variety of side effects on human health, such as allergy, cardiovascular and kidney diseases, lung fibrosis, lung, and nasal cancer. It is therefore critical from a public health and environmental perspective to determine and monitor Ni(II) ions in drinking water, foods, and environmental samples. In this study, a novel selective chemosensor (4-[{[4-(3-Chlorophenyl)-1,3-Thiazol-2-yl]Hydrazono}Methyl]phenyl4-methylBenzene Sulfonate (CTHMBS) was developed for the colorimetric detection of Ni(II) in aqueous medium. The presence of Ni(II) led to a distinct naked-eye color change from yellow to reddish-brown in aqueous solution. To examine the binding mechanism of CTHMBS to Ni(II), UV-vis spectroscopy analysis and DFT calculations were conducted. The detection limit of CTHMBS for Ni(II) was 11.87 µM, and the sensing ability of CTHMBS for Ni(II) was successfully carried out in real water samples.

One-Pot, Four-Component Reaction for the Design, Synthesis, and SAR Studies of Novel Pyridines for Insecticidal Bioefficacy Screening against Cowpea Aphid (Aphis craccivora).

In this paper, novel pyridines 2-8 were designed and synthesized via the one-pot, four-component reaction of 2-formylphenyl 4-tolylsulfonate with malononitrile, ammonium acetate, and phenols or 2-thioxo-1,3-thiazolidin-4-one or 6-aminopyrimidine-2,4(1H,3H)-dione under microwave irradiation in an aqueous solution of water and ethanol (1:1 ratio). The structures of new pyridines 2-8 were elucidated by elemental and spectral analyses such as IR, 1H NMR, and 13CNMR. This application has many advantages, such as having easy workup, eco-friendliness, reaction time being short (6-13 min), high production (94-98%), inexpensiveness, and avoiding the use of harmful solvents. Moreover, all compounds have been investigated as insecticidal agents against cowpea aphid (Aphis craccivora) insects, and the toxicity effect was studied, followed by the structure-activity relationship. From the LC50 values, it has been found that compounds 7 and 8 were excellent and promising insecticidal agents, with LC50 values of 0.05 and 0.09 ppm against nymphs and 0.93 and 1.01 ppm against adults of cowpea aphid. Furthermore, the obtained results indicated that compounds 2-8 can be applied as insecticidal agents for the control of cowpea aphids and to protect agricultural crops from this destructive pest, which effects crop production and causes major economic damage.

Design and evaluation of sulfadiazine derivatives as potent dual inhibitors of EGFRWT and EGFRT790M: integrating biological, molecular docking, and ADMET analysis.

A series of derivatives (5-14) were synthesized through the diazotization of sulfadiazine with active methylene compounds. The chemical structures of these newly designed compounds were validated through spectral and elemental analysis techniques. The antiproliferative potential of derivatives 5-14 was assessed against three distinct cancer cell lines (A431, A549, and H1975) using the MTT assay. The results revealed that compounds 8, 12, and 14 exhibited the most potent antiproliferative activity, with IC50 values ranging from 2.31 to 7.56 µM. Notably, these values were significantly lower than those of known EGFR inhibitors, including erlotinib, gefitinib, and osimertinib, suggesting the potential of these derivatives as novel antiproliferative agents. Furthermore, compound 12 was identified as the most potent inhibitor of both EGFRWT and EGFRT790M protein kinases, with IC50 values of 14.5 and 35.4 nM, respectively. These results outperformed those of gefitinib and osimertinib, which exhibited IC50 values of 18.2 and 368.2 nM, and 57.8 and 8.5 nM, respectively. Molecular docking studies of compounds 8, 12, and 14 within the ATP-binding sites of both EGFRWT and EGFRT790M corroborated the in vitro results when compared to erlotinib, gefitinib, and osimertinib. The docking results indicated that compound 8 exhibited a favorable binding affinity for both EGFRWT and EGFRT790M, with binding scores of -6.40 kcal mol-1 and -7.53 kcal mol-1, respectively, which were comparable to those of gefitinib and osimertinib, with binding scores of -8.01 and -8.72 kcal mol-1, respectively. Furthermore, an assessment of the most promising EGFR inhibitors (8, 12, and 14) using the egg-boiled method for their in silico ADME properties revealed significant lipophilicity, blood-brain barrier (BBB) penetration, and gastrointestinal (GIT) absorption. Collectively, our designed analogs, particularly compounds 8, 12, and 14, exhibit promising dual antiproliferative and EGFRWT and EGFRT790M kinase inhibitory properties, positioning them as efficient candidates for further therapeutic development.