pmid: 31724435,   nlmid 101150203,  doi:10.1080/14756366.2019.1690479

Synthesis, biological evaluation, and molecular modelling of new naphthalene-chalcone derivatives as potential anticancer agents on MCF-7 breast cancer cells by targeting tubulin colchicine binding site.


Wang, Guangcheng Liu, Wenjing Gong, Zipeng Huang, Yong Li, Yongjun Peng, Zhiyun

Vol. 35, Issue 35, Dec.2020

Journal of enzyme inhibition and medicinal chemistry (J Enzyme Inhib Med Chem),  ISSN 1475-6374

Abstract

A series of naphthalene-chalcone derivatives () were prepared and evaluated as tubulin polymerisation inhibitor for the treatment of breast cancer. All compounds were evaluated for their antiproliferative activity against MCF-7 cell line. The most of compounds displayed potent antiproliferative activity. Among them, compound displayed the most potent antiproliferative activity with an IC value of 1.42?▒?0.15?ÁM, as compared to cisplatin (IC?=?15.24?▒?1.27?ÁM). Additionally, the promising compound demonstrated relatively lower cytotoxicity on normal cell line (HEK293) compared to tumour cell line. Furthermore, compound was found to induce significant cell cycle arrest at the G/M phase and cell apoptosis. Compound displayed potent tubulin polymerisation inhibitory activity with an IC value of 8.4?ÁM, which was slightly more active than the reference compound colchicine (IC?=?10.6?ÁM). Molecular docking analysis suggested that interact and bind at the colchicine binding site of the tubulin.


MESH Headings


Article Keywords

Chalcone | anticancer | synthesis | tubulin inhibitor |


Chemical

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