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Molecular diversity of trimethoxyphenyl-1,2,3-triazole hybrids as novel colchicine site tubulin polymerization inhibitors.

Abstract：

:Structurally diverse trimethoxyphenyl-1,2,3-triazole hybrids were designed, synthesized and evaluated for their antiproliferative activity against three cancer cell lines (PC3, MGC803 and HepG2). Among them, trimethoxyphenyl-1,2,3-triazole containing the coumarin fragement 19c displayed better antiproliferative activity results with IC50 values from 0.13 μM to 1.74 μM than anticancer drug colchicine. Compound 19c could inhibit MGC803 cell growth and colony formation, induce G2/M phase arrest by down expression of CDK1, and promote apoptosis by regulating DR5 and Bcl-2 family. Moreover, 19c strongly inhibited tubulin polymerization by interacting with the colchicine site.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Fu DJ,Li P,Wu BW,Cui XX,Zhao CB,Zhang SY

doi

10.1016/j.ejmech.2019.01.033

subject

Has Abstract

pub_date

2019-03-01 00:00:00

pages

309-322

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(19)30043-1

journal_volume

165

pub_type

杂志文章

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