Ameliorative potential of rosmarinic acid in a rat model of polycystic ovary syndrome: Targeting MCP-1 and VEGF: A histological, immunohistochemical, and biochemical study.

Polycystic ovary syndrome (PCOS) is a multidisciplinary endocrinopathy that affects women of reproductive age. It is characterized by menstrual complications, hyperandrogenism, insulin resistance, and cardiovascular issues. The current research investigated the efficacy of rosmarinic acid in letrozole-induced PCOS in adult female rats as well as the potential underlying molecular mechanisms. Forty female rats were divided into the control group, the rosmarinic acid group (50 mg/kg per orally, po) for 21 days, PCOS group; PCOS was induced by administration of letrozole (1 mg/kg po) for 21 days, and rosmarinic acid-PCOS group, received rosmarinic acid after PCOS induction. PCOS resulted in a marked elevation in both serum luteinizing hormone (LH) and testosterone levels and LH/follicle-stimulating hormone ratio with a marked reduction in serum estradiol and progesterone levels. A marked rise in tumor necrosis factor-α (TNF-α), interleukin-1ß, monocyte chemotactic protein-1, and vascular endothelial growth factor (messenger RNA) in the ovarian tissue was reported. The histological analysis displayed multiple cystic follicles in the ovarian cortex with markedly thin granulosa cell layer, vacuolated granulosa and theca cell layers, and desquamated granulosa cells. Upregulation in the immune expression of TNF-α and caspase-3 was demonstrated in the ovarian cortex. Interestingly, rosmarinic acid ameliorated the biochemical and histopathological changes. In conclusion, rosmarinic acid ameliorates letrozole-induced PCOS through its anti-inflammatory and antiangiogenesis effects.

Ameliorative Potential of Bone Marrow-Derived Mesenchymal Stem Cells Versus Prednisolone in a Rat Model of Lung Fibrosis: A Histological, Immunohistochemical, and Biochemical Study.

Idiopathic pulmonary fibrosis (IPF) is a progressive lung disease of unknown origin with limited treatment options and poor prognosis. The encouraging findings from preclinical investigations utilizing mesenchymal stem cells (MSCs) indicated that they could serve as a promising therapeutic alternative for managing chronic lung conditions, such as IPF. The objective of this study was to compare the efficiency of bone marrow-derived MSCs (BM-MSCs) versus prednisolone, the standard anti-inflammatory medication, in rats with bleomycin (BLM)-induced lung fibrosis. Four groups were created: a control group, a BLM group, a prednisolone-treated group, and a BM-MSCs-treated group. To induce lung fibrosis, 5 mg/kg of BLM was administered intratracheally. BLM significantly increased serum levels of pro-inflammatory cytokines and oxidative stress markers. The disturbed lung structure was also revealed by light and transmission electron microscopic studies. Upregulation in the immune expression of alpha-smooth muscle actin, transforming growth factor beta-1, and Bax was demonstrated. Interestingly, all findings significantly regressed on treatment with prednisolone and BM-MSCs. However, treatment with BM-MSCs showed better results than with prednisolone. In conclusion, BM-MSCs could be a promising approach for managing lung fibrosis.

Level of and factors associated with foot self-care among people with diabetes in Idlib Province of Northwest Syria: A cross-sectional study.

Background and aims: Diabetic foot and lower limb problems are among the most neglected complications during the Syrian armed conflict due to the absence of a functioning health infrastructure, including early detection and timely management of limb-threatening wounds. This study aimed to determine self-reported diabetes-related foot disease (DRFD), adherence to recommended foot self-care (FSC) practices, and associated factors among people with diabetes in war-torn Northwest Syria (NWS). Methods: This was a cross-sectional study conducted at six primary care clinics in Idlib, NWS, between March 27 and April 17, 2022, utilizing the validated interviewer-administered Diabetes Foot Disease and Foot Care Questionnaire. Data on demographic characteristics, DRFD, and FSC practices were collected. FSC score was determined by adding the points from all 12 FSC items, with a maximum score of 48, and were categorized into very poor (≤12), poor (13-24), moderate (25-36), and good (37-48). A convenience sample of 331 consecutive Syrians, aged ≥18 years, with diabetes, were invited. Multiple linear regression was used to identify variables associated with FSC practices. Results: A total of 328 patients completed the questionnaire (response rate: 99.1%). The overall FSC score was average (mean total score 27.24, SD 7.03). Over one-third (37.8%) had a very poor/poor score, 50.3% had an average score, and 11.9% had a good score. Household income/month of ≥51 USD (ß = 2.6, 95% confidence interval [95% CI]:1.06-4.1, p = 0.001) and diabetes duration of ≥10 years (ß = 1.8, 95% Cl: 0.2-3.4, p = 0.027) significantly predicted better FSC practice. Conclusion: A significant proportion of participants had inadequate adoption FSC behaviors. Higher socioeconomic status was associated with better FSC practices. Future research should evaluate diabetic foot education and professional foot care in this population.

The Cdc14 phosphatase, Clp1, does not affect genome expression.

Schizosaccharomyces pombe Clp1 is a Cdc14-family phosphatase that reverses mitotic Cdk1 phosphorylation. Despite evolutionary conservation, Clp1 's mammalian orthologs do not share this function. Rather, higher eukaryotic Cdc14 enzymes act in DNA repair, ciliogenesis, and gene regulation. To examine if Clp1 regulates gene expression, we compared the transcriptional profiles of cells lacking Clp1 function to that of wildtype. Because clp1∆ cells are sensitive to the actin depolymerizing drug, LatrunculinA, we also investigated whether a transcriptional response was involved. Our results indicate that Clp1 does not detectably affect gene expression and highlight the organism-specific functions of this conserved phosphatase family.

Broad functional profiling of fission yeast proteins using phenomics and machine learning.

Many proteins remain poorly characterized even in well-studied organisms, presenting a bottleneck for research. We applied phenomics and machine-learning approaches with Schizosaccharomyces pombe for broad cues on protein functions. We assayed colony-growth phenotypes to measure the fitness of deletion mutants for 3509 non-essential genes in 131 conditions with different nutrients, drugs, and stresses. These analyses exposed phenotypes for 3492 mutants, including 124 mutants of 'priority unstudied' proteins conserved in humans, providing varied functional clues. For example, over 900 proteins were newly implicated in the resistance to oxidative stress. Phenotype-correlation networks suggested roles for poorly characterized proteins through 'guilt by association' with known proteins. For complementary functional insights, we predicted Gene Ontology (GO) terms using machine learning methods exploiting protein-network and protein-homology data (NET-FF). We obtained 56,594 high-scoring GO predictions, of which 22,060 also featured high information content. Our phenotype-correlation data and NET-FF predictions showed a strong concordance with existing PomBase GO annotations and protein networks, with integrated analyses revealing 1675 novel GO predictions for 783 genes, including 47 predictions for 23 priority unstudied proteins. Experimental validation identified new proteins involved in cellular aging, showing that these predictions and phenomics data provide a rich resource to uncover new protein functions.

Effect of Liraglutide on Osteoporosis in a Rat Model of Type 2 Diabetes Mellitus: A Histological, Immunohistochemical, and Biochemical Study.

Diabetic osteoporosis (DOP) is a diabetic complication associated with a significant disability rate. Liraglutide, a glucagon-like peptide-1 receptor agonist, is a promising and innovative drug for type 2 diabetes mellitus (T2DM), with potential therapeutic implications for bone disorders. This investigation examined the impact of liraglutide on osteoporosis in rats with T2DM and studied the influence of vitamin D receptor Bsm1 polymorphism on liraglutide-induced outcomes. Thirty rats were divided into control, T2DM induced by a combination of a high-fat diet and 25 mg/kg streptozotocin, and T2DM-liraglutide (T2DM treated with 0.4 mg/kg/day liraglutide) groups. After 8 weeks of liraglutide treatment, femurs and blood samples were obtained from all rats for subsequent investigations. Diabetes induced a remarkable rise in the serum levels of receptor activator of nuclear factor kappa B ligand (RANKL) and C-telopeptide of type I collagen (CTX-1) associated with a remarkable decline in osteocalcin and osteoprotegerin (OPG). Impaired bone architecture was also demonstrated by light and scanning electron microscopic study. The immune expression of OPG was down-regulated, while RANKL was up-regulated. Interestingly, the administration of liraglutide ameliorated the previous changes induced by diabetes mellitus. In conclusion, liraglutide can prevent DOP, mostly due to liraglutide's ability to increase bone growth, while inhibiting bone resorption.

Evening primrose oil attenuates oxidative stress, inflammation, fibrosis, apoptosis, and ultrastructural alterations induced by metanil yellow in the liver of rat: a histological, immunohistochemical, and biochemical study.

The food color metanil yellow (Myl) is hazardous to several body systems. Evening primrose oil (EPO) was reported to have anti-inflammatory and anti-oxidant properties. The present work investigated the impact of Myl on the hepatic structure and function of rats and evaluated the protective effect of EPO. Forty adult male rats were divided into four groups: control, EPO (5 g/kg/day), Myl (200 mg/kg/day), and EPO- Myl group. Myl significantly increased liver enzymes, advanced glycation end products (AGE), oxidative stress parameters, pro-inflammatory cytokines, nuclear factor kappa B (NF-κB), and inducible nitric oxide synthase (iNOS). Blood vessels in the liver were dilated and congested, with cellular infiltration around them and associated with fibrosis. The hepatocytes were vacuolated and had dark nuclei. The immunohistochemical expression of iNOS, glial fibrillary acidic protein (GFAP), and Bax was significantly elevated. Ultrastructurally, the hepatocytes showed lipid droplets, irregular condensed nuclei with widened perinuclear space, dilated rER, mitochondria with destructed cristae, and multiple vacuoles. Dilated congested blood sinusoids and collagen fiber bundles were seen between hepatocytes. Interestingly, these alterations were less pronounced in rats co-administrated with EPO and Myl. In conclusion, EPO can protect liver against the toxic effects of Myl due to its anti-inflammatory and anti-oxidant activities.

The Preventive and Therapeutic Effects of Ajwa Date Fruit Extract Against Acute Diclofenac Toxicity-Induced Colopathy: An Experimental Study.

Background: Studies regarding treatment of acute toxicity with diclofenac (ATD) are quite few. Diclofenac is commonly prescribed in neurology, psychiatry, and general medicine practice. This study investigated possible colon-protective effects exerted by Ajwa date fruit extract (ADFE), a prophetic medicine remedy native to Al-Madinah, Saudi Arabia against ATD. Phytochemicals in ADFE as gallic acid and quercetin have reported protective effects against ATD. Methods: Total phenols and flavonoids in ADFE were estimated as equivalents to gallic acid and quercetin. Four experimental groups were allocated each of six rats: control group, ATD group received a single dose of 150 mg diclofenac intraperitoneally, toxicity prevention group received a single dose of ADFE orally followed 4 hours later by diclofenac injection, and toxicity treatment group received a similar diclofenac dose followed 4 hours later by a single dose of ADFE. Four days later, animals were sacrificed. Histological and biochemical examinations were done. Results: ADFE has a total phenolic content of 331.7 gallic acid equivalent/gram extract and a total flavonoid content of 70.23 quercetin equivalent/gram. ATD significantly increased oxidative stress markers as serum malondialdehyde (MDA) and hydrogen peroxide (H2O2). Serum MDA and H2O2 were significantly scavenged by ADFE. ATD significantly (p<0.001) decreased antioxidant power as serum total antioxidant capacity and catalase activity. That was reversed by ADFE in both prevention and treatment groups. Histologically, ATD caused complete destruction of colonic crypts architecture, patchy loss of the crypts, loss of the surface epithelium, absent goblet cells and submucosal exudate, heavy infiltration of the lamina propria and submucosa with inflammatory cells, mainly lymphocytes and eosinophils. There were mucosal haemorrhages and submucosal dilated congested blood vessels. All that was prevented and treated using ADFE. Conclusion: ADFE is rich in quercetin and gallic acid equivalents that exert potent antitoxic effects. ADFE is strongly recommended for preventive and therapeutic colon effects against ATD.

Evaluation of blood and biochemical parameters of COVID-19 patients in Suez Canal University Hospital; A retrospective study.

INTRODUCTION: The severe acute respiratory syndrome coronavirus 2 (SARS CoV2-CoV-2) viral outbreak in Wuhan (China) caused thousands of confirmed cases and deaths around the world. Severe viral pneumonia with respiratory failure and death are the ultimate consequence of infection. AIM: This study aimed to evaluate the regularly performed standard laboratory parameters that can assist in COVID-19 case identification and establish an effective approach to help care and management of (COVID-19) patients. METHODOLOGY: COVID-19 (n = 129) patients were hospitalized in the Suez Canal University Hospital and were retrospectively examined. Laboratory parameters were gathered from patients upon admission (n = 129) during the period from the 20th of June to 15th of August 2020. SARS-CoV-2 cases were diagnosed clinically and radiologically by chest Computed Tomography (CT) and confirmed by RT-PCR. RESULTS: The results showed that COVID-19 survivors exhibited lower hemoglobin (Hb) and hematocrit (HCT), while showed higher Red Cell Distribution Width (RDW), neutrophil lymphocyte ratio (NLR), and lymphocytes. Logistic regression analysis showed that age greater than 60 years old, neutrophilia and high NLR were associated with more deaths. CONCLUSION: Monitoring of lymphopenia, neutrophilia and NLR may help categorizing patients who may need Intensive care.

Ameliorating effect of gum arabic on the liver tissues of the uremic rats; A biochemical and histological study.

BACKGROUND: Gum Arabic (GA) has a protective role against experimental nephrotoxicity and hepatotoxicity. This study explores the possible ameliorating effect of Gum Arabic on the liver tissues of the uremic rats. MATERIALS & METHODS: 50 adult male albino rats were divided into 5 groups; Group I, (negative control). Group II: two flank incisions were made and the kidneys were kindly manipulated. Group III: the rats have received a daily oral dose of GA. Group IV: subtotal nephrectomy in the left kidney was done followed by total nephrectomy on the right kidney 1 week later to induce uremia. Group V: the rats received GA one day after the second operation and daily for 5 weeks. At the end of the work, the rats were sacrificed, blood samples were collected for biochemical analysis. The abdomen was opened and the liver was dissected for light, electron microscopic and immunohistochemical studies. RESULTS: The biochemical results were increased in the uremic group, but greatly improved after GA administration. Light and electron studies showed histopathological changes of the liver tissues in the uremic group, which was improved after GA administration and confirmed by the morphometric measures. CONCLUSION: GA ameliorates the histopathological changes of the liver tissues caused by uremic toxins and has a protective effect against the development of hepatocellular carcinoma.

Release characterization and biological effect of Glass Ionomer Functionalized with two different chlorohexidine derivatives: an in vitro study

ABSTRACT Objective: To evaluate the effect of adding two different chlorohexidine derivatives; chlorhexidine hexametaphosphate and chlorhexidine digluconate to glass ionomer at three different concentrations (0.25%, 0.75%and 1.5%) regarding the antibacterial effect, chlorhexidine release and fluoride release. Methods: A total of 405 specimens were prepared and tested after 7 days, 3 months and 6 months of storage in distilled water (n=5).For testing antibacterial effect, chlorhexidine release and fluoride release, the mix was packed in a ready-made Split Teflon molds to obtain disc-shaped specimen with dimensions 10 mm in diameter and 2 mm thickness according to ISO standardizations. One-way ANOVA and One-way repeated measure ANOVA test were used for statistical analysis of data. Results: The incorporation of chlorhexidine into ChemFil Superior glass ionomer cement in both derivatives has high significance ability to provide a long-term antimicrobial effect on Streptococcus mutans and Lactobacillius acidophilus. The chlorhexidine release was increased by adding chlorhexidine in both derivatives to GIC than the unmodified Glass-ionomer cement for study duration. However, the fluoride release was decreased in the modified specimens than the original one. Conclusion: Addition of chlorhexidine enhanced the antibacterial effect of the glass ionomer and chlorhexidine release. However, fluoride release was reduced than original

Pattern and determinants of COVID-19 infection and mortality across countries: An ecological study.

BACKGROUND: This work aimed to identify the mathematical model and ecological determinants of COVID-19 infection and mortality across different countries during the first six months of the pandemic. METHODOLOGY: In this study, authors used the online available data sources of randomly selected 18 countries to figure out potential determinants of COVID-19 transmissibility and mortality. The studied variables were environmental factors (daily average temperature, daily humidity), socioeconomic attributes (population age structure, count and density, human development index, per capita income (PCI), gross domestic product, internet coverage) mobility trends and chronic diseases. Researchers used the linear and exponential time series analysis, and further utilized multivariate techniques to explain the variance in the monthly increase in cases and deaths. RESULTS: In the first two months, the R2 of linear models for the cases and deaths were higher than that of the corresponding R2 of the exponential model. Later one, R2 of the exponential model was occasionally relatively higher than that of the linear model. The exponential growth rate of new cases was significantly associated with mobility trends (ß = 0.00398, P = 0.002), temperature (ß = 0.000679, P = 0.011), humidity (ß = 0.000249, P < 0.001), and the proportion of population aged ≥65 years (ß = -0.000959, P = 0.012). Similarly, the exponential growth rate of deaths was significantly associated with mobility trends (ß = 0.0027, P = 0.049), temperature (ß = 0.0014, P < 0.001), humidity (ß = -0.0026, P < 0.001), and PCI of countries. During this period, COVID-19 transmissibility was evident to be controlled as soon as social mobility is decreased by about 40% of the baseline over 3 months controlling for the other predictors. CONCLUSION: Controlling of COVID-19 pandemic is based mainly on controlling social mobility. Role of environmental determinants like temperature and humidity was well noticed on disease fatality and transmissibility. Socio-demographic determinants of COVID-19 spread and fatality included modifiable risk factors like PCI and non-modifiable risk factors like ageing.

The potential ameliorative impacts of cerium oxide nanoparticles against fipronil-induced hepatic steatosis.

Fipronil (FIP) is a phenylpyrazole insecticide that is commonly used in agricultural and veterinary fields for controlling a wide range of insects, but it is a strong environmentally toxic substance. Exposure to FIP has been reported to increase the hepatic fat accumulation through altered lipid metabolism, which ultimately can contribute to nonalcoholic fatty liver disease (NAFLD) development. The present study aimed to examine the function of cerium oxide nanoparticles (CeNPs) in protecting against hepatotoxicity and lipogenesis induced by FIP. Twenty-eight male albino rats were classified into four groups: FIP (5 mg/kg/day per os), CTR, CeNPs (35 mg/kg/day p.o.), and FIP + CeNPs (5 (FIP) + 35 (CeNPs) mg/kg/day p.o.) for 28 consecutive days. Serum lipid profiles, hepatic antioxidant parameters and pathology, and mRNA expression of adipocytokines were assessed. The results revealed that FIP increased cholesterol, height-density lipoprotein, triacylglyceride, low-density lipoprotein (LDL-c), and very-low-density lipoprotein (VLDL-c) concentrations. It also increased nitric oxide (NO) and malondialdehyde (MDA) hepatic levels and reduced glutathione peroxidase (GPx) and superoxide dismutase (SOD) enzyme activities. Additionally, FIP up-regulated the fatty acid-binding protein (FABP), acetyl Co-A carboxylase (ACC1), and peroxisome proliferator-activated receptor-alpha (PPAR-α). Immunohistochemically, a strong proliferation of cell nuclear antigen (PCNA), ionized calcium-binding adapter molecule 1 (Iba-1), cyclooxygenase-2 (COX-2) reactions in the endothelial cells of the hepatic sinusoids, and increased expression of caspase3 were observed following FIP intoxication. FIP also caused histological changes in hepatic tissue. The CeNPs counteracted the hepatotoxic effect of FIP exposure. So, this study recorded an ameliorative effect of CeNPs against FIP-induced hepatotoxicity.

Chemo-Protective Potential of Cerium Oxide Nanoparticles against Fipronil-Induced Oxidative Stress, Apoptosis, Inflammation and Reproductive Dysfunction in Male White Albino Rats.

Fipronil (FIP) is an insecticide commonly used in many fields, such as agriculture, veterinary medicine, and public health, and recently it has been proposed as a potential endocrine disrupter. The purpose of this study was to inspect the reproductive impacts of FIP and the possible protective effects of cerium nanoparticles (CeNPs) on male albino rats. Rats received FIP (5 mg/kg bwt; 1/20 LD50), CeNPs (35 mg/kg bwt) and FIP+CeNPs per os daily for 28 days. Serum testosterone levels, testicular oxidative damage, histopathological and immunohistochemical changes were evaluated. FIP provoked testicular oxidative damage as indicated by decreased serum testosterone (≈60%) and superoxide dismutase (≈50%), glutathione peroxidase activity (≈46.67%) and increased malondialdehyde (≈116.67%) and nitric oxide (≈87.5%) levels in testicular tissues. Furthermore, FIP induced edematous changes and degeneration within the seminiferous tubules, hyperplasia, vacuolations, and apoptosis in the epididymides. In addition, FIP exposure upregulated interleukin-1ß (IL-1ß), nitric oxide synthase 2 (NOS), caspase-3 (Casp3) and downregulated the Burkitt-cell lymphomas (BCL-2), inhibin B proteins (IBP), and androgen receptor (Ar) mRNA expressions Casp3, nitric oxide synthase (iNOS), ionized calcium-binding adapter molecule 1(IBA1), and IL-1ß immunoreactions were increased. Also, reduction of proliferating cell nuclear antigen (PCNA), mouse vasa homologue (MVH), and SOX9 protein reactions were reported. Interestingly, CeNPs diminished the harmful impacts of FIP on testicular tissue by decreasing lipid peroxidation, apoptosis and inflammation and increasing the antioxidant activities. The findings reported herein showed that the CeNPs might serve as a supposedly new and efficient protective agent toward reproductive toxicity caused by the FIP insecticide in white male rats.

Design, efficient synthesis and molecular docking of some novel thiazolyl-pyrazole derivatives as anticancer agents.

Pyrazoles, thiazoles and fused thiazoles have been reported to possess many biological activities. 3-Methyl-5-oxo-4-(2-arylhydrazono)-4,5-dihydro-1H-pyrazole-1-carbothioamides 3a,b (obtained from the reaction of ethyl 3-oxo-2-(2-arylhydrazono)butanoates 1a,b with thiosemicarbazide) could be transformed into a variety of thiazolyl-pyrazole derivatives 6a-h, 10a-c, 15a-c, 17, 19 and 21 via their reaction with a diversity hydrazonoyl chlorides as well as bromoacetyl derivatives. Moreover, the computational studies were carried out for all new compounds. The results indicated that five compounds showed promising binding affinities (10a: - 3.4 kcal/mol, 6d: - 3.0 kcal/mol, 15a: - 2.2 kcal/mol, 3a: - 1.6 kcal/mol, and 21: - 1.3 kcal/mol) against the active site of the epidermal growth factor receptor kinase (EGFR). The cytotoxicity of the potent products 3a, 6d, 10a, 15a, and 21 was examined against human liver carcinoma cell line (HepG-2) and revealed activities close to Doxorubicin standard drug. There was an understanding between the benefits of restricting affinities and the data obtained from the practical anticancer screening of the tested compounds.

Study of handling of medico-legal cases in governmental hospitals in Cairo.

Medico-legal case (MLC) represents an integral part of medical practice in the emergency departments and causalities. Therefore, the physicians should have the sufficient knowledge of their roles and responsibilities while handling these cases to aid legal justice. This study on the physicians working in governmental hospitals in Cairo aimed to assess physicians' knowledge, practice and attitude regarding handling of MLCs. The study included 452 physicians working in 7 governmental hospitals in Cairo. There were non-significant differences in physicians' knowledge, practice and attitude scores according to their age groups, gender, job titles or duration of work experience. Physicians working in the day surgery centre had the lowest knowledge and attitude scores. Daily rate of confrontation with MLCs was reported by 42% the participants (190 physicians) and weekly rate was reported by 21.7% (98 physicians). Writing ML report was found as the most frequently encountered difficulty faced the participants during handling of MLCs (67.1%), followed by dealing with the patients' relatives. In conclusion, this study revealed absence of a well defined protocol for recognition and handling of MLCs in all included governmental hospitals in Cairo.

Green Synthesis and Molecular Docking of Thiazolyl-thiazole Derivatives as Potential Cytotoxic Agents.

METHOD: A series of novel thiazole derivatives were synthesized in a good yield via reaction of 2-(1-(4-methyl-2-phenylthiazol-5-yl)ethylidene)hydrazine carbothioamide with hydrazonoyl halides. The reaction was performed in the presence of DABCO as an organocatalyst in short reaction times, easy workup, good to excellent yields. The structure of the newly synthesized products was elucidated via elemental analysis, spectral data and alternative routes whenever possible. Ten compounds were evaluated for their anti-cancer activity against the colon carcinoma cell line (HCT-116). RESULTS & CONCLUSION: The results revealed that most of the tested compounds showed high or moderate anti-cancer activity. The molecular docking of five novel thiazolyl-thiazole derivatives was performed by the Molecular Operating Environment (MOE) program.

Synthesis, biological evaluation, and molecular docking studies of new pyrazol-3-one derivatives with aromatase inhibition activities.

A new series derived from 4-(2-chloroacetyl)-1,2-dihydro-1,5-dimethyl-2-phenyl-3H-pyrazol-3-one was synthesized, characterized and its pharmacological activity toward aromatase enzyme inhibition was screened and compared to the reference native ligand letrozole. The most active compound of the series was 16, showing IC50 value of 0.0023 ± 0.0002 µm compared to letrozole with IC50 of 0.0028 ± 0.0006 µm. In addition, compounds 26 and 36 exhibit good inhibition activities close to letrozole with IC50 values 0.0033 ± 0.0001 and 0.0032 ± 0.0003 µm, respectively. Moreover, molecular docking studies were conducted to support the findings.