A5066013126- Synthesis and biological activity
- Synthesis and Biological Evaluation
- Cancer therapeutics and mechanisms
- Quinazolinone synthesis and applications
- Multicomponent Synthesis of Heterocycles
- Angiogenesis and VEGF in Cancer
- PI3K/AKT/mTOR signaling in cancer
- Cancer Mechanisms and Therapy
- Antibiotic Resistance in Bacteria
- Peroxisome Proliferator-Activated Receptors
- Melanoma and MAPK Pathways
- Antimicrobial Resistance in Staphylococcus
- Eicosanoids and Hypertension Pharmacology
- Cancer Treatment and Pharmacology
- Advanced Breast Cancer Therapies
- Cancer-related Molecular Pathways
- Computational Drug Discovery Methods
- Click Chemistry and Applications
- Bacterial biofilms and quorum sensing
- Cancer, Lipids, and Metabolism
Al-Azhar University
2017-2025
Al-Azhar University
2021
A series of hybrid triazoloquinoxaline-chalcone derivatives 7a-k were designed, synthesized, fully characterized, and evaluated for their cytotoxic activity against three target cell lines: human breast adenocarcinoma (MCF-7), colon carcinoma (HCT-116), hepatocellular (HEPG-2). The preliminary results showed that some these chalcones like 7b-c, 7e-g exhibited significant antiproliferative effects most the lines, with selective or non-selective behavior, indicated by IC50 values in 1.65 to...
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 A new series of 1,2,4‐triazolo[4,3‐ c ]quinazoline derivatives was designed and synthesized as Topo II inhibitors DNA intercalators. The cytotoxic effect the members evaluated in vitro against a group cancer cell lines including HCT‐116, HepG‐2, MCF‐7. Compounds 14 , d e 15 b 18 19 exhibited highest activities with IC 50 values ranging from 5.22 to 24.24 µM. Furthermore, inhibitory intercalating affinities most promising candidates were possible mechanism for antiproliferative...
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,...
The narrow antibacterial spectrum of phenylthiazole antibiotics was expanded by replacing central thiazole with a pyrazole ring while maintaining its other pharmacophoric features. most promising derivative, compound 23, more potent than vancomycin against multidrug-resistant Gram-positive clinical isolates, including vancomycin- and linezolid-resistant methicillin-resistant Staphylococcus aureus (MRSA), minimum inhibitory concentration (MIC) value as low 0.5 μg/mL. Moreover, 23 superior to...
Novel quinoline-based derivatives 2a-e and 4a-j have been designed synthesized as potential antiproliferative agents. The compounds were screened for their activity against sixty cell lines according to NCI protocol. promising hybrids 4d-g are by MTT assays on three cancer lines: leukemia (MOLT-4), lung (HOP-92), breast (T47D), with IC50 values ranging from 4.982 ± 0.2 36.52 1.46 µM compared Staurosporine, compound 4e being the most effective. Derivatives evaluated inhibitory EGFR BRAFV600E....
Novel heterocyclic derivatives (4-22) were designed, synthesized, and evaluated against hepatocellular carcinoma type (HepG2) breast cancer (MCF-7) cells, targeting the VEGFR-2 enzyme. Compounds 18, 10, 13, 11, 14 found to be most potent both HepG2 MCF-7 cell lines, with GI50 = 2.11, 2.54 µM, 3.16, 3.64 3.24, 6.99 7.41, 6.49 µM 8.08, 10.46 respectively. 18 10 showed higher activities cells than sorafenib (GI50 9.18, 5.47 respectively) doxorubicin 7.94, 8.07 respectively). but lower cells....
CDK2 is a key player in cell cycle processes. It has crucial role the progression of various cancers. Hepatocellular carcinoma (HCC) and colorectal cancer (CRC) are two common cancers that affect humans worldwide. The available therapeutic options suffer from many drawbacks including high toxicity decreased specificity. Therefore, there need for more effective safer agents. A series new pyrazolo[3,4-d]pyrimidine analogs was designed, synthesized, evaluated as anticancer agents against CRC...
Phenylpyrazolo[3,4-d]pyrimidine is considered a milestone scaffold known to possess various biological activities such as antiparasitic, antifungal, antimicrobial, and antiproliferative activities. In addition, the urgent need for selective potent novel anticancer agents represents major route in drug discovery process. Herein, new aryl analogs were synthesized evaluated their effects on panel of cancer cell lines: MCF-7, HCT116, HePG-2. Some these compounds showed cytotoxicity, with...