Design, Synthesis and Anticancer Biological Evaluation of Novel 1,4-Diaryl-1,2,3-triazole Retinoid Analogues of Tamibarotene (AM80)

Journal of the Brazilian Chemical Society

Aleixo, Mariana A. A.¹  Garcia, Taís M.² 

[1] Universidade Federal do Mato Grosso do Sul, Campo Grande, Brazil;Universidade Tecnológica Federal do Paraná, Curitiba, Brazil

关键词: 1;    2;    3-triazole retinoids;    tamibarotene;    click chemistry;    bioisosterism;    anticancer activities.;   

DOI  :  10.21577/0103-5053.20170119

学科分类：化学（综合）

来源: SciELO

【 摘 要 】

We report herein the design and synthesis via click chemistry of twelve novel triazole retinoid analogues of tamibarotene (AM80) and the evaluation of their anticancer activities against six cancer cell lines: HL60, K562, 786, HT29, MCF7 and PC3. Among the synthesized compounds, two were more potent than tamibarotene against solid tumor cells, and one of them had similar potency to tamibarotene against HL60 cells. The bioisosteric exchange between the amide group and the 1,2,3-triazole core in the retinoid agent tamibarotene (AM80) reported in this work is a valid strategy for the generation of useful compounds against cancer.

【 授权许可】

CC BY