NDLI: 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

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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

Content Provider	Scilit
Author	Wang, Guangcheng Liu, Wenjing Gong, Zipeng Huang, Yong Li, Yongjun Peng, Zhiyun
Copyright Year	2019
Description	A series of naphthalene-chalcone derivatives (3a–3t) 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 3a displayed the most potent antiproliferative activity with an $IC_{50}$ value of 1.42 ± 0.15 µM, as compared to cisplatin $(IC_{50}$ = 15.24 ± 1.27 µM). Additionally, the promising compound 3a demonstrated relatively lower cytotoxicity on normal cell line (HEK293) compared to tumour cell line. Furthermore, compound 3a was found to induce significant cell cycle arrest at the $G_{2}$/M phase and cell apoptosis. Compound 3a displayed potent tubulin polymerisation inhibitory activity with an $IC_{50}$ value of 8.4 µM, which was slightly more active than the reference compound colchicine $(IC_{50}$ = 10.6 µM). Molecular docking analysis suggested that 3a interact and bind at the colchicine binding site of the tubulin.
Related Links	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6882462/pdf
Ending Page	144
Page Count	6
Starting Page	139
ISSN	14756366
e-ISSN	14756374
DOI	10.1080/14756366.2019.1690479
Journal	Journal of Enzyme Inhibition and Medicinal Chemistry
Issue Number	1
Volume Number	35
Language	English
Publisher	Informa UK Limited
Publisher Date	2019-11-14
Access Restriction	Open
Subject Keyword	Medicinal Chemistry Chalcone Tubulin Inhibitor Anticancer Synthesis
Content Type	Text
Resource Type	Article
Subject	Medicine Drug Discovery Pharmacology

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