Decoration of viscose fibers with silver nanoparticle-based titanium-organic framework for use in environmental applications.

To effectively remove pharmaceuticals, nitroaromatic compounds, and dyes from wastewater, an efficient multifunctional material was created based on silver nanoparticles (Ag) and MIL-125-NH2 (MOF) immobilized on viscose fibers (VF) as a support substrate. Firstly, silver nanoparticles (Ag) were immobilized on the surface of viscose fibers (VF) via in situ synthesis using trisodium citrate (TSC) as a reducing agent to create (VF-Ag). Then, VF and VF-Ag were decorated with the titanium metal-organic framework MIL-125-NH2 (MOF) to create VF-MOF and VF-Ag-MOF. The influence of VF-Ag, VF-MOF, and VF-Ag-MOF on the sonocatalytic or sonophotocatalytic degradation of sulfa drugs was investigated. The results show that VF-Ag-MOF showed excellent sonocatalytic and sonophotocatalytic activity towards the degradation of sulfa drugs compared to VF-Ag and VF-MOF. Furthermore, sonophotodegradation showed a dramatic enhancement in the efficiency of degradation of sulfa drugs compared to sonodegradation. The sonophotodegradation degradation percentage of sulfanilamide, sulfadiazine, and sulfamethazine drugs in the presence of VF-Ag-MOF was 65, 90, and 95 after 45 min of ultrasonic and visible light irradiation. The catalytic activity of VF-Ag, VF-MOF, and VF-Ag-MOF was evaluated through the conversion of p-nitrophenol (4-NP) to p-aminophenol (4-AP). The results demonstrate that VF-Ag-MOF had the highest catalytic activity, followed by VF-Ag and VF-MOF. The conversion percentage of 4-NP to 4-AP was 69%. The catalytic or photocatalytic effects of VF-Ag, VF-MOF, and VF-Ag-MOF on the elimination of methylene blue (MB) dye were investigated. The results demonstrate that VF-Ag-MOF showed high efficiency in removing the MB dye through the reduction (65%) or photodegradation (71%) after 60 min. VF-Ag-MOF composites structure-activity relationships represent that doping within silver NPs enhanced the photocatalytic activity of MIL-125-NH2, which could be explained as follows: (i) Due to the formation of a Schottky barrier at the junction between MIL-125-NH2 and Ag NPs, the photogenerated electrons in the conduction band of MIL-125-NH2 were supposed to be quickly transferred to the valence band of the Ag NPs, and subsequently, the electrons were transferred to the conduction band of Ag NPs. This considerable electron transferring process, which is reported as Z scheme heterojunction, can efficiently suppress the recombination of electron/hole pairs in VF-Ag-MIL-125-NH2 composites. (ii) Sufficient separation between the photogenerated charge carriers (holes and electrons) and avoiding their recombination enhanced the photocatalytic activity of composites.

Pyrimidine-5-carbonitrile derivatives as sprout for CQDs proveniences: Antitumor and anti-inflammatory potentiality.

A comparative study is proposed to show the effect of variation in the heteroatoms in the main skeleton of CQDs proveniences, on their affinity for nucleation of CQDs, as anti-inflammatory and anticancer drugs. Heterocyclic-based CQDs sprout was successfully exploited for preparation of three CQDs proveniences, named as; 2-(2,5-dimethoxyphenyl)-4,6-dioxo-6,11-dihydro-4H-pyrimido[2,1-b] quinazoline-3-carbonitrile (compound A), 2-(2,5-dimethoxyphenyl)-4,6-dioxo-4H,6H-benzo[e]pyrimido[2,1-b][1,3]oxazine-3-carbonitrile (compound S) and 2-(2,5-dimethoxyphenyl)-4,6-dioxo-4H,6H-benzo[e]pyrimido[2,1-b][1,3] thiazine-3-carbonitrile (compound T). Chemical formulas of CQDs proveniences & CQDs were verified via FTIR, 1HNMR, 13CNMR & XRD. Particle size of TM-CQDs, A-CQDs, S-CQDs & T-CQDs were estimated to be 3.7 ± 1.4, 4.6 ± 1.6, 5.9 ± 1.6 nm and 3.0 ± 1.3 nm, respectively. All of CQDs proveniences & CQDs were examined for their affinity as anti-inflammatory drugs via Griess assay. CQDs ingrained from TM (TM-CQDs) were detected with the highest NO inhibition% by increasing its concentration from 10 up to 100 µM to be 40 % to 89 %, respectively. Moreover, their anti-tumor performance against MCF-7: breast Adenocarcinoma cell line was approved via sulforhodamine B assay, whereas, IC50 was evaluated for TM-CQDs, A-CQDs, S-CQDs and T-CQDs to be 38.16, 36.09, 100 and 100 µg/ml, respectively.

Selective separation of chlorophyll-a using recyclable hybrids based on Zn-MOF@cellulosic fibers.

Chlorophyll-a as pigments, exist in the green organelles for plants that act in photosynthesis. Different studies were considered with demonstration of an effective separation technique of Chlorophyll-a without decomposition; however, the reported methods were disadvantageous with expensiveness and low quantum yield. The current work uniquely represents an investigative method for the separation of Chlorophyll-a from spinach extract using cellulosic hybrids based on ZIF-8 @cellulosic fibers (Zn-zeolitic imidazolate frameworks@cellulosic fibers) as a cost effective and recyclable absorbents. To obtain hybrids, ZIF-8 was in-situ prepared over the cellulosic fibers (bamboo, modal and cotton). The untreated and treated fibers were well characterized via FTIR, SEM, EDX, XRD, in order to approve the successive impregnation of ZIF-8. Whereas, the microscopic images showed that, microcrystalline ZIF-8 rods with length of 1.3-4.4 µm were grown over the cellulosic fibers. The obtained hybrids and the untreated fibers were exploited in the separation of Chlorophyll-a via the adsorption/desorption process. The chlorophyll-adsorption was followed Langmuir isotherm and pseudo-second order model. The Langmuir maximum capacities of Chlorophyll-a onto hybrids were followed the order of ZIF-8@cotton (583.6 mg/g) > ZIF-8@modal (561.3 mg/g) > ZIF-8@bamboo (528.7 mg/g). After incorporation of ZIF-8, the maximum adsorption capacities of cellulosic fibers were enhanced by 1.4-1.9 times. Adsorption of chlorophyll onto the applied hybrids was lowered by 27-28%, after five repetitive washing cycles. The data summarized that; chlorophyll was effectively separated by the synthesized ZIF-8@cellulosic fibers hybrids, whereas, the prepared hybrids showed good reusability for application on wider scaled purposes.

Efficient phenolic compounds adsorption by immobilization of copper-based metal-organic framework anchored polyacrylonitrile/chitosan beads.

The application of newly formulated beads from copper-benzenetricarboxylate (Cu-BTC), polyacrylonitrile (PAN), and chitosan (C), Cu-BTC@C-PAN, C-PAN, and PAN, for the removal of phenolic chemicals from water, is described in the current paper. Phenolic compounds (4-chlorophenol (4-CP) and 4-nitrophenol (4-NP)) were adsorbed using beads and the adsorption optimization looked at the effects of several experimental factors. The Langmuir and Freundlich models were used to explain the adsorption isotherms in the system. A pseudo-first and second-order equation is performed for describing the kinetics of adsorption. The obtained data fit (R2 = 0.999) supports the suitability of the Langmuir model and pseudo-second-order kinetic equation for the adsorption mechanism. Cu-BTC@C-PAN, C-PAN, and PAN beads' morphology and structure were investigated using X-ray diffraction (XRD), scanning electron microscopy (SEM), and Fourier transforms infrared spectroscopy (FT-IR). According to the findings, Cu-BTC@C-PAN has very high adsorption capacities of 277.02, and 324.74 mg g-1, for 4-CP and 4-NP, respectively. The Cu-BTC@C-PAN beads showed 2.55 times higher adsorption capacity than PAN in the case of 4-NP, but in the case of 4-CP, it was higher by 2.64 times.

Maillard reaction for nucleation of polymer quantum dots from chitosan-glucose conjugate: Antagonistic for cancer and viral diseases.

Polymer dots (PDs) ingrained from biopolymers are characterized by their biocompatibility & non-toxicity to be superiorly applicable for biomedicines. The point of novelty in the current study is to focus on the effect of Maillard reaction for conjugation of chitosan with glucose to enhance the affinity of chitosan as a biological resource of PDs. Chitosan-glucose conjugate was firstly prepared by Maillard reaction. PDs were nucleated from chitosan (C1 acidic, 10.6 nm & C2 basic, 11.4 nm) and chitosan-glucose conjugate (C3 acidic, 6.8 nm & C4 basic, 5.7 nm). The affinity of chitosan versus chitosan-glucose conjugate as molecular precursors for PDs as antiviral and anticancer laborers was studied. The synthesized PDs were tested against lung cancer (NSCLC, A549) and the estimated IC50 was 282.4 & 165.4 µg/mL for PDs (C3 & C4) ingrained from chitosan-glucose conjugate. The antiviral action of PDs against Coronavirus (229E) was estimated and the obtained IC50 for C3 & C4 was 43.6 and 19.3 mg/mL, respectively. PDs ingrained from chitosan-glucose conjugate showed higher anticancer and antiviral activities compared to that clustered from chitosan. Consequently, the modification of chitosan via Maillard reaction enhanced the biological affinity of the obtained PDs to be effectively applicable as antitumor and antiviral laborers.

Size-tunable effect of CaCO3/nanocellulose hybrid composites on the removal of paracetamol from aqueous solution.

Paracetamol is a ubiquitous drug used by animals and humans but is not fully metabolized within their bodies, and thus often finds its way into raw wastewater. This study represents a new class of adsorbent nanocomposite with high adsorption capacity towards paracetamol removal. Herein, both the kinetic study and the removal of paracetamol from aqueous solutions were investigated in terms of diverse CaCO3/nanocellulose composites with different surface charges and different particle sizes. To fine-tune these parameters, the latter was hydrothermally synthesized by manipulating of three nanocelluloses types. Precisely, micro-crystalline cellulose (MCC), nano-crystalline cellulose (CNC), and nano-fibrillated cellulose (NFC) were used as templates for precipitating CaCO3 particles from CaCl2 solution with the aid of Na2CO3. Results revealed the successful in situ deposition of calcite form of CaCO3 with size varied relying on the base of nanocellulose. For MCC, CNC, and NFC, the size of CaCO3 was disclosed in the range of 850-1200 nm, 350-600 nm, and 150-200 nm, respectively, regarding their surface charge. While the process of paracetamol adsorption was described by Freundlich and Langmuir isotherms, it was observed that, for MCC, the best fit of the experimental data was achieved with the Freundlich model, while the Langmuir model was the most appropriate for CNC and NFC. Also, the highest max adsorption capacities of paracetamol varied respectively to both size and surface charge of hybrid composite used. Among them, MCC/CaCO3 composite exhibited the highest max adsorption capacity at 428 mg g-1, clarifying that the low surface zeta potential of the latter hybrid nanocomposite is responsible for the accumulation of CaCO3 at a bigger size with a higher affinity to adsorb paracetamol with the highest capacity due to its weak repulsion. Results also demonstrated that the material is highly effective and economical for removal of paracetamol and reusability with marginal diminishing in adsorption capacity up to 10% after five reuse cycles.

Observable removal of pharmaceutical residues by highly porous photoactive cellulose acetate@MIL-MOF film.

Pharmaceutical products are used tremendously worldwide and subsequently released into wastewater even at very low concentration caused serious environmental problem due to their high activity. Therefore, the present work focuses on remarkable removal of paracetamol as one from the most used pharmaceutical intermediates, by using porous film based on cellulose acetate@metal organic framework (CA@Ti-MIL-NH2). The film was designed to achieve extreme removal of paracetamol by action of both of adsorption and degradation. Metal organic frame work was directly synthesized and inserted within the pre-prepared porous CA film to obtain porous CA@Ti-MIL-NH2 film. The synthesized films were applied in adsorption and photo-degradation of paracetamol separately and together. Due to the photocatalytic activity of Ti-MIL-NH2, the photo-degradation of paracetamol in visible-light was much effective and considerably high degradation of paracetamol was observed (k1 = 760.0 m-1) comparing to the adsorption (k1 = 160.0 m-1). The overall removal of paracetamol was significantly enlarged from 82.7 mg/g for CA film to 519.1 mg/g for porous CA@Ti-MIL-NH2 film. The used film exhibited quite good reusability and the removal of paracetamol was lowered from 96% to 85% after 5 regeneration cycles. Results of total organic carbon confirmed that paracetamol was fully degraded to CO2 and water.

Effective Pharmacophore for CDC25 Phosphatases Enzyme Inhibitors: Newly Synthesized Bromothiazolopyrimidine Derivatives.

BACKGROUND: Thiazolopyrimidine analogues are versatile synthetic scaffold possessing wide spectrum of biological interests involving potential anticancer activity. OBJECTIVE: To report the synthesis of novel bromothiazolopyrimidine derivatives and the study of both molecular modeling and in-vitro anticancer activity. METHODS: Novel bromothiazolopyrimidine derivatives 5-18 have been prepared from 2-bromo-3-(4- chlorophenyl)-1-(3,4-dimethylphenyl)-propenone 3 as a key starting compound. The anti-cancer activities of the new compounds were evaluated against HepG2, MCF-7, A549 and HCT116 cell lines. RESULTS: The compounds 16, 17 and 18 showed cytotoxic and growth inhibitory activities on both colon and lung cells. The cytotoxic activities of the novel synthetic compounds 8, 9, 11, 16, 17 and 18 were due to CDC25 phosphatases inhibition as shown by the enzymatic binding assay. Although compounds 8, 9 and 11 have only demonstrated CDC25B phosphatases inhibition. CONCLUSION: The novel bromothiazolopyrimidine derivatives showed promising in vitro anticancer activities against colon cancer HCT116 and lung cancer A549 cell lines comparable to the anticancer drug doxorubicin.

Synthesis of arylidene hydrazinylpyrido[2,3-d]pyrimidin-4-ones as potent anti-microbial agents.

Combination of arylidene hydrazinyl moiety with pyrido[2,3-d]pyrimidin-4-one skeleton in compounds 7‒26 results in the output of unprecedented anti-microbial agents. Arylidene hydrazinyl based on Pyrido[2,3-d]pyrimidin-4-one analoges 7‒26 prepared by the treatment of [2,3-d]pyrimidin-4-ones 6a,b with various aromatic aldehydes. The antimicrobial action for recently synthesized compounds was considered towards gram positive bacterial species (Staphylococcus aurous ATCC- 47077; Bacillus cereus ATCC-12228), gram negative bacterial species (Escherichia coli ATCC-25922; Salmonella typhi ATCC-15566) and Candida albicans ATCC-10231 as fungal strains. The antimicrobial action expanded by expanding the electron donating group in position 2 and 5 for Pyrido[2,3-d]pyrimidin-4-one core. Derivatives 13, 14, 15, 16 and 12; individually appeared hopeful anti-microbial action towards all strains utilized with inhibition zone higher than that of standard reference drug with lowest MIC.

Employable metal (Ag & Pd)@MIL-125-NH2@cellulose acetate film for visible-light driven photocatalysis for reduction of nitro-aromatics.

The effective and reusable photocatalyst film based on metal @metal organic framework@cellulose acetate [metal (Ag & Pd)@MIL-125-NH2@CA] was systematically studied. Nano-silver was grown over the crystalline disc of MIL-125-NH2 within CA film, while, self-assembly of crystalline trees like the structure of Pd)@MIL-125-NH2 was observed inside CA matrix. The calculated band gap was diminished from 2.53 eV to 2.38-1.99 eV after doping of metal (Ag & Pd) within MIL-125-NH2@CA film. Compared to MIL-125-NH2@CA; metal (Ag & Pd)@MIL-125-NH2@CA film showed a considerably higher photocatalytic reduction of nitro-aromatics in visible light. After 60 min, 80.6-93.5 % of 2-nitrophenol was photoreduced when metal (Ag & Pd)@MIL-125-NH2@CA film was used. After 5 recycles, the photoreduction percentage of 2-nitrophenol was lowered to 54.4-62.0. The produced metal@MIL-125-NH2@CA films showed an effective photocatalytic reduction of nitro-aromatics in the visible light, reflecting their promising performance in preparation of intermediates useful in many industrial products.

Capture of iodide from wastewater by effective adsorptive membrane synthesized from MIL-125-NH2 and cross-linked chitosan.

The mainly nuclear waste is radioactive iodine (129I or131I) so its disposal have great significance to produce safe water. Porous metal-organic works (MOFs) have awesome potential as high-effective adsorbents for water treatment. In any case, destitute separation limits their viable application. All in all, we worked on the development of MOFs with cross linked chitosan as a promising adsorbent material for the remediation of environmental water polluted by iodine. Due to the drawbacks of current adsorbents such as low uptake capacity, high cost, and non-recyclability; a novel cross-linked chitosan-MOF composite was synthesized and used in the adsorptive removal of iodine from wastewater. The novel composite shows high iodine removal capacity 399.68 mg g-1 at room temperature. The cross-linked chitosan-MOF composite shows chemical and thermal stability, high removal efficiency for capture of iodine from wastewater and furthermore good recyclability.

First Synthesis for Bis-Spirothiazolidine Derivatives as a Novel Heterocyclic Framework and Their Biological Activity.

BACKGROUND: Spirothiazolidines are versatile synthetic scaffold possessing wide spectrum of biological interests involving potential anticancer activity. OBJECTIVE: To report the first synthesis of Bis Spiro-thiazolidine as a novel heterocyclic ring system. METHODS: One-pot three-component reaction including condensation of p-phenyllene diamine; cyclohexanone and thioglycolic acid produced Spiro-thiazolidine 4, which underwent further condensation with cyclohexanone and thioglycolic acid with equimolar ratio to introduce Bis-Spiothiazolidine 5 as the first synthesis. Also, bis spiro-thiazolidine arylidene derivatives 6-13 were synthesized by the reaction of Bis-Spiothiazolidine 5 with different aromatic benzaldehydes. RESULTS: Four compounds 13, 12, 9 and 11 have shown highly significant anticancer activity compared to Doxorubicin® (positive control) against Human liver carcinoma (HepG2) and Human Normal Retina pigmented epithelium (RPE-1) cell lines. CONCLUSION: The novel bis-spirothiazolidine deriviatives have been synthesized for the first time and showed excellent anticancer activities compare with the corresponding spirothiazolidine derivatives.

Development of a Novel Series of Anticancer and Antidiabetic: Spirothiazolidines Analogs.

4-(4-Aminophenyl)-1-thia-4-azaspiro[4.5]decan-3-one 1 was prepared and allowed to react with nitrogen nucleophiles to give the corresponding hydrazones 2-4. Further, compound 1 underwent diazotization and afforded the parallel hydrazono derivative 5; moreover, compound 1 refluxed with active methylene derivatives yielded the corresponding aminospirothiazolo pyridine-carbonitrile derivative 6 and spirothiazolopyridinone-carbonitrile derivative 7. Condensation of spirothiazolidine 1 with 4-chlorobenzaldehyde gave the corresponding spiro arylidiene derivative 8, which was utilized as a component of Micheal addition to react with excess of nitrogen nucleophiles to yield novel ring frameworks 4-(3'-(4-chlorophenyl)-spiro [cyclohexane-1,5'-pyrazolo[3,4-d]thiazol]-6'(1'H)-yl)aniline (9) and 4-(3'-(4-chlorophenyl)-6'H- spiro[cyclohexane-1,5'-thiazolo[5,4-d]isoxazol]-6'-yl)aniline (10). Finally, when spirothiazolo pyridinone-carbonitrile derivative 7 sodium salt generated in situ was reacted with different alkyl halides, it produced the corresponding N-derivatives 12-16. Three compounds, 6, 14, and 16, showed high significantly anticancer activities compared with Doxorubicin® (positive control) against human breast carcinoma (MCF-7) and human liver carcinoma (HepG-2) cell lines. On the other hand, compounds 6 and 9 showed higher therapeutic indices for both of alpha-amylase inhibitor and alpha-glucosidase inhibitor than the other tested compounds compared with the antidiabetic Acarbose (positive control).

Synthesis, Molecular Docking and in Vitro Screening of Some Newly Synthesized Triazolopyridine, Pyridotriazine and Pyridine⁻Pyrazole Hybrid Derivatives.

A series of novel pyridine and fused pyridine derivatives have been prepared starting from 6-(3,4-dimethylphenyl)-2-hydrazinyl-4-(thiophen-2-yl)-pyridine-3-carbonitrile 1 which on treatment with appropriate formic acid, acetic acid/ acetic anhydride, benzoyl chloride and/or carbon disulfide afforded the corresponding triazolopyridine derivatives 2⁻5. Also, treatment of hydrazide 1 with diethyloxalate, chloroacetyl chloride, chloroacetic acid and/or 1,2-dichloroethane yielded the corresponding pyridotriazine derivatives 7⁻10. Further transformation of compound 1 with a different active methylene group, namely acetyl acetone, diethylmalonate, ethyl cyanoacetate, ethyl benzoylacetate and/or ethyl acetoacetate, produced the pyridine⁻pyrazole hybrid derivatives 11⁻15. These newly synthesized compounds (1⁻15) were subjected to in silico molecular docking screenings towards GlcN-6-P synthase as the target protein. The results revealed moderate to good binding energies of the ligands on the target protein. All the newly prepared products exhibited antimicrobial and antioxidant activity.

Synthesis of Some New Pyridazine Derivatives for Anti-HAV Evaluation.

4-(2-(4-Halophenyl)hydrazinyl)-6-phenylpyridazin-3(2H)-ones 1a,b were prepared and treated with phosphorus oxychloride, phosphorus pentasulphide and ethyl chloroformate to give the corresponding chloropyridazine, pyridazinethione, oxazolopyridazine derivatives 2-4, respectively. Compound 2 reacted with hydrazine hydrate to afford hydrazinylpyridazine 7. The reaction of 4-(2-(4-chlorophenyl)hydrazinyl)-3-hydrazinyl-6-phenylpyridazine (7) with acetic anhydride, p-chlorobenzaldehyde and carbon disulphide gave the corresponding pyridazinotriazine derivatives 8-10. On the other hand, 5-(4-chlorophenylamino)-7-(3,5-dimethoxybenzylidene)-3-phenyl-5H-pyridazino[3,4-b][1,4]thiazin-6(7H)-one (11) was prepared directly from the reaction of compound 3 with chloroacetic acid in presence of p-chlorobenzaldehyde. Compound 11 reacted with nitrogen nucleophiles (hydroxylamine hydrochloride, hydrazine hydrate) and active methylene group-containing reagents (malononitrile, ethyl cyanoacetate) to afford the corresponding fused compounds 12-15, respectively. Pharmacological screening for antiviral activity against hepatitis A virus (HAV) was performed for the new compounds. 4-(4-Chlorophenylamino)-6-phenyl-1,2-dihydropyridazino[4,3-e][1,2,4]triazine-3(4H)-thione (10) showed the highest effect against HAV.

Recombinase polymerase amplification as a promising tool in hepatitis C virus diagnosis.

Hepatitis C virus (HCV) infection represents a significant health problem and represents a heavy load on some countries like Egypt in which about 20% of the total population are infected. Initial infection is usually asymptomatic and result in chronic hepatitis that give rise to complications including cirrhosis and hepatocellular carcinoma. The management of HCV infection should not only be focus on therapy, but also to screen carrier individuals in order to prevent transmission. In the present, molecular detection and quantification of HCV genome by real time polymerase chain reaction (PCR) represent the gold standard in HCV diagnosis and plays a crucial role in the management of therapeutic regimens. However, real time PCR is a complicated approach and of limited distribution. On the other hand, isothermal DNA amplification techniques have been developed and offer molecular diagnosis of infectious dieses at point-of-care. In this review we discuss recombinase polymerase amplification technique and illustrate its diagnostic value over both PCR and other isothermal amplification techniques.

Anticancer evaluation of some newly synthesized N-nicotinonitrile derivative.

Some novel N-nicotinonitrile derivatives 3-14 have been synthesized starting with compound 1. The key step of this work is the coupling between compound 1 and activated sugars to afford the corresponding cyclic nucleosides 3-6. Moreover, the cytotoxicity and in vitro anticancer evaluation of the prepared compounds have also been assessed against breast MCF-7 cancer, liver HepG2 cancer and lung A549 carcinoma cell lines with investigation the effect of the synthesized compounds on the expression of urokinase plasminogen activator (uPA). The results revealed that, although all the compounds showed no anticancer activity against A549 cells without showing any effect on the expression of uPA, the tested compounds exhibited remarkable cytotoxicity activity against MCF-7 and HepG2 cell lines. Among the tested compounds, compounds 11 and 12 revealed promising anticancer activity compared to the activity of the commonly used anticancer drug, doxorubicin with inhibiting the expression of uPA.

New pyrimidinone and fused pyrimidinone derivatives as potential anticancer chemotherapeutics.

A series of novel substituted pyrimidinones and fused pyrimidinones (compounds 3-18) were synthesized starting with oxiranylmethanone 2. The in vitro cytotoxicity against a human breast adenocarcinoma (MCF-7) cell line was investigated and most of the tested compounds showed potent cytotoxic activity against the MCF-7 cell line comparable to the activity of the commonly used anticancer drug cisplatin. Treatment of MCF-7 cells with increasing doses (2, 5, 10, and 20 µg/mL) of the tested compounds revealed that the activity of superoxide dismutase and the level of hydrogen peroxide were significantly increased, while the activities of catalase and glutathione peroxidase and the levels of reduced glutathione were significantly lowered compared with control MCF-7 cells. In general, derivatives 11 and 16 revealed the highest anticancer activity among the tested compounds.