期刊
SYNTHETIC COMMUNICATIONS
卷 51, 期 18, 页码 2782-2795出版社
TAYLOR & FRANCIS INC
DOI: 10.1080/00397911.2021.1941113
关键词
Erlotinib; isoxazole and anticancer; luminespib; quinazoline
资金
- Dean of Scientific Research, King Khalid University [R.G.P2/83/41]
A new library of structurally modified aryl quinazoline-isoxazole derivatives were synthesized and evaluated for their anticancer activities against four human cancer cell lines. Most of the compounds exhibited good to moderate anticancer activities, with some showing more potent effects. Docking studies showed that all synthesized compounds had good binding interactions with the targeted proteins.
A new library of structurally modified aryl quinazoline-isoxazole (12a-j) derivatives have been designed, synthesized and characterized by (HNMR)-H-1, (CNMR)-C-13 and mass spectral data. Further these compounds were evaluated for anticancer applications against four human cancer cell lines including PC3, DU-145 (prostate cancer), A549 (lung cancer) and MCF-7 (breast cancer) by utilizing the MTT assay. The results were compared with etoposide which was used as positive control. Most of the compounds showed good to moderate anticancer activities against the four cancer cell lines. Among them, compounds 12a, 12b, 12c, 12d and 12j exhibited more potent activities. Further, molecular docking studies were carried out for all synthesized compounds against the cancer targets Selective Human Androgen Receptor (PDB ID: 3V49) and Abl-Tyrosine kinase (PDB ID: 1IEP). All the docked ligands have exhibited good binding interactions with the targeted protein.
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