期刊
CHEMICO-BIOLOGICAL INTERACTIONS
卷 355, 期 -, 页码 -出版社
ELSEVIER IRELAND LTD
DOI: 10.1016/j.cbi.2022.109838
关键词
Benzochromene; Antitumor activity; Topoisomerase; Tyrosine kinase receptors; Molecular docking
资金
- Deanship of Science Research at King Khalid University, Saudi Arabia [RGP.1/189/42]
A series of novel oxygen-containing heterocyclic linked 1H-benzo[f]chromene moieties were designed and synthesized, showing anti-proliferative activity against cancer cell lines, particularly MCF-7, HCT-116, and HepG-2. The compounds exhibited potential mechanisms involving cell cycle arrest and inhibition of topoisomerase enzymes.
A novel oxygen-containing heterocyclic linked 1H-benzo[f]chromene moieties (4a-g) and (6a-g) with anti proliferative activity against cancer cell lines was designed, synthesized, and established on the basis of spectral data. All the prepared compounds were evaluated in vitro for their anti-proliferative activity against MCF-7, HCT-116, HepG-2 cell lines and normal cell lines HFL-1, WI-38. Compounds 4a, 4b, and 6e exhibited good activity against MCF-7, HCT-116, and HepG-2 cell lines, comparable to that of Vinblastine and Doxorubicin, and weak active against normal cell lines. Moreover, the potential mechanisms of the cytotoxic activity of the promising compounds 4a, 4b, and 6e on the more sensitive cell line MCF-7 were studied. We found that compounds 4a, 4b, and 6e induce cell cycle arrest at G2/M phases for MCF-7 treated cells compared to untreated cells, which causes apoptosis and inhibits both the topoisomerase I and II enzymes. In addition, compounds 4a and 4b exhibited comparable inhibitory activity on tyrosine kinase receptors EGFR and VEGFR-2 kinases to that of the reference protein kinases inhibitor Sorafenib. The in silico molecular docking of the most active compounds into the active sites of EGFR kinase and Topo I & II enzymes provides us with a reasonable clarification of the interpreted biological data.
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