A5066270766- Synthesis and biological activity
- Quinazolinone synthesis and applications
- Synthesis and Biological Evaluation
- Cancer therapeutics and mechanisms
- Angiogenesis and VEGF in Cancer
- HER2/EGFR in Cancer Research
- Synthesis and Characterization of Heterocyclic Compounds
- PI3K/AKT/mTOR signaling in cancer
- Phenothiazines and Benzothiazines Synthesis and Activities
- Bioactive Compounds and Antitumor Agents
- Click Chemistry and Applications
- Lung Cancer Treatments and Mutations
- Cancer Mechanisms and Therapy
- Synthesis and Reactions of Organic Compounds
- Multiple Myeloma Research and Treatments
- Chemical Reaction Mechanisms
- Protein Degradation and Inhibitors
- Enzyme function and inhibition
- Synthesis of Tetrazole Derivatives
- Nanoparticle-Based Drug Delivery
- Neuroscience and Neuropharmacology Research
- Cancer Treatment and Pharmacology
- Multicomponent Synthesis of Heterocycles
- Bioactive Natural Diterpenoids Research
- Cytokine Signaling Pathways and Interactions
Al-Azhar University
2016-2025
Heliopolis University
2019-2025
Al-Azhar University
2013-2025
Abstract Novel series of benzoxazole s 4 a‐f ‐16 were designed, synthesized, and evaluated for anticancer activity against HepG2, HCT‐116, MCF‐7 cells. HCT‐116 was the most sensitive cell line to influence new derivatives. In particular, compound 5 e found be potent with IC 50 = 4.13 ± 0.2, 6.93 0.3, 8.67 0.5 µM, respectively. Compounds c , f 6 b d showed highest activities HepG2 cells 5.93 6.58 0.4, 8.10 0.7, 8.75 9.95 0.9 respectively; 7.14 9.10 0.8, 7.91 0.6, 9.52 0.5, 12.48 1.1 8.93...
Abstract A novel series of benzoxazole/benzothiazole derivatives 4a–c – 11a–e were designed, synthesized, and evaluated for anticancer activity against HepG2, HCT‐116, MCF‐7 cells. HCT‐116 was the most sensitive cell line to influence new derivatives. In particular, compound 4c found be potent derivative cells, with IC 50 values = 9.45 ± 0.8, 5.76 0.4, 7.36 0.5 µM, respectively. Compounds 4b, 9f , 9c showed highest activities HepG2 cells 9.97 9.99 11.02 1.0 respectively, 6.99 0.5, 7.44 8.15...
Eleven new quinoxaline derivatives were designed and synthesized as modified VEGFR-2 inhibitors of our previous work.
Abstract Targeting the epidermal growth factor receptors (EGFRs) with small inhibitor molecules has been validated as a potential therapeutic strategy in cancer therapy. Pyrazolo[3,4‐ d ]pyrimidine is versatile scaffold that exploited for developing anticancer agents. On basis of fragment‐based drug discovery, considering essential pharmacophoric features potent EGFR tyrosine kinase (TK) inhibitors, herein, we report design and synthesis new hybrid pyrazolo[3,4‐ linked diverse fragments...
The resistance of pathogenic microbes to currently available antimicrobial agents has been considered a global alarming concern.
Newly designed thiazolidine-2,4-diones 3-7a-c were synthesized, and their anticancer activities screened against three cancer lines. They showed potent HepG2 compared to the other HCT116 MCF-7 tumor cell Compounds 7c 6c detected as highly effective derivatives (IC50 = 7.78 8.15 µM), 5.77 7.11 µM) 8.82 8.99 µM). The 6a-c 7a-c tested VERO normal All evaluated for VEGFR-2 inhibitory actions demonstrated high low activities, with IC50 values varying from 0.08 0.93 µM. Moreover, 5a-c, assessed...
Abstract The effectiveness of a new series thiopyrimidine and thiourea containing sulfonamides moieties was tested on HCT‐116, MCF‐7, HepG2, A549. HepG2 cell line the one that all derivatives affected most. greatest potent compounds against four HCT116, A549 lines were 8f 8g with IC 50 = 4.13, 6.64, 5.74, 6.85 µM 4.09, 4.36, 4.22, 7.25 correspondingly. Compound exhibited higher activity than sorafenib HCT116 MCF‐7 but lower Moreover, activities erlotinib demonstrated most cytotoxic 6f , 6g...
New phenyldiazene scaffold-linked heterocyclic pyrazole, pyrimidinone, pyrimidinthione, and/or triazine rings have been developed and synthesized. Cytotoxicity of our derivatives was estimated on four cancer VERO normal cell lines targeting EGFRT790M (epidermal growth factor receptor) VEGFR-2 (vascular endothelial receptor-2) enzymes. Our new selectively inhibited both EGFR as they the essential structural requirements for inhibitors receptors. Derivative 14 most active A549, HCT116, HepG2,...
Novel series of phthalazine derivatives 6 – 11 were designed, synthesized, and evaluated for their anticancer activity against two human tumor cell lines, HCT‐116 colon adenocarcinoma MCF‐7 breast cancer cells, targeting the VEGFR‐2 enzyme. Compounds 7a , b 8b c showed highest activities both HCT116 cells with IC 50 6.04 ± 0.30, 13.22 0.22, 18 0.20, 35 0.45 μM, respectively, 8.8 0.45, 17.9 0.50, 25.2 0.55, 44.3 0.49 in comparison to sorafenib as reference drug 5.47 0.3 7.26 respectively....
In continuation of our previous work on the design and synthesis topoisomerase II (Topo II) inhibitors DNA intercalators, a new series quinoxaline derivatives were designed synthesized. The synthesized compounds evaluated for their cytotoxic activities against panel three cancer cell lines (Hep G-2, Hep-2, Caco-2). Compounds 18b, 19b, 23, 25b, 26 showed strong potencies all tested with IC50 values ranging from 0.26 ± 0.1 to 2.91 µM, comparable those doxorubicin (IC50 0.65 0.81 µM). most...
Abstract A new series of 2‐substituted‐2,3‐dihydrophthalazine‐1,4‐diones ( 2 ‒ 9 ) were designed and synthesized to evaluate their anticonvulsant activity. The neurotoxicity was assessed using the rotarod test. Molecular docking performed for compounds assess binding affinities as γ‐aminobutyric acid (GABA‐A) receptor agonists a possible mechanism action, rationalize activity in qualitative way. data obtained from molecular modeling strongly matched with that biological screening, which...
Abstract A novel series of 5‐(4‐methoxybenzylidene)thiazolidine‐2,4‐dione derivatives, 5a–g and 7a–f , was designed, synthesized, evaluated for their anticancer activity against HepG2, HCT116, MCF‐7 cells. HepG2 HCT116 were the most sensitive cell lines to influence new derivatives. In particular, compounds 7f 7e 7d 7c found be potent derivatives all tested cancer lines. Compound (IC 50 = 6.19 ± 0.5, 5.47 0.3, 7.26 0.3 µM, respectively) exhibited a higher than sorafenib 9.18 0.6, 8.37 0.7,...