Literature

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.

DOI： 10.1016/j.ejmech.2019.01.033

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

European Journal of Medicinal Chemistry 2019.0

Synthesis and biological evaluation of cis -restricted triazole/tetrazole mimics of combretastatin-benzothiazole hybrids as tubulin polymerization inhibitors and apoptosis inducers

Bioorganic & Medicinal Chemistry 2017.0

Design, synthesis and bioevaluation of 6-aryl-1-(3,4,5-trimethoxyphenyl)-1H-benzo[d]imidazoles as tubulin polymerization inhibitors

European Journal of Medicinal Chemistry 2021.0

Synthesis and structure–activity relationships of 1,2,4-triazoles as a novel class of potent tubulin polymerization inhibitors

Bioorganic & Medicinal Chemistry Letters 2005.0

Synthesis and structure–activity relationships of pyridinyl-1H-1,2,3-triazolyldihydroisoxazoles as potent inhibitors of tubulin polymerization

European Journal of Medicinal Chemistry 2015.0

Design and synthesis of novel 1,2,3-triazole-pyrimidine hybrids as potential anticancer agents