Long-chain alkyltriazoles as antitumor agents: synthesis, physicochemical properties, and biological and computational evaluation

被引：8

作者：

Gontijo, Vanessa Silva ^{[1
]}

Oliveira, Michael Eder ^{[2
]}

Resende, Rafael Jose ^{[2
]}

Fonseca, Amanda Luisa ^{[2
]}

Nunes, Renata Rachide ^{[2
]}

Comar Junior, Moacyr ^{[2
]}

Taranto, Alex Gutterres ^{[2
]}

Pereira Oliveira Torres, Natalia Machado ^{[1
]}

Ribeiro Viana, Gustavo Henrique ^{[2
]}

Silva, Luciana Maria ^{[3
]}

Alves, Rosemeire Brondi ^{[1
]}

Varotti, Fernando Pilla ^{[2
]}

Freitas, Rossimiriam Pereira ^{[1
]}

机构：

[1] Univ Fed Minas Gerais, ICEx, Dept Quim, BR-31270901 Belo Horizonte, MG, Brazil

[2] Univ Fed Sao Joao del Rei, BR-35501296 Divinopolis, MG, Brazil

[3] Fundacao Ezequiel Dias, Lab Biol Celular, BR-30535380 Belo Horizonte, MG, Brazil

来源：

MEDICINAL CHEMISTRY RESEARCH | 2015年 / 24卷 / 01期

关键词：

Alkyltriazoles; Antitumoral; Click chemistry; Heterocycles; INHIBITORY-ACTIVITY; 1,2,3-TRIAZOLE; APOPTOSIS; OPTIMIZATION; DERIVATIVES; NUCLEOSIDE; CARCINOMA; ETOPOSIDE; PHASE;

D O I：

10.1007/s00044-014-1137-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel long-chain alkyltriazoles were prepared from commercial diols in a rapid process with good yields. The compounds were evaluated in vitro for their anticancer potential against two human cancer cell lines: colon carcinoma (RKO) and uterine carcinoma (HeLa). The results of colorimetric MTT assays showed that six of fourteen compounds tested decreased cell viability in these cell lines. Compounds 5e and 6a were the most active against RKO cells, with IC50 values of 16.70 and 14.57 mu M, respectively. The same compounds, 5e and 6a, were the most active in HeLa cells as well, with IC50 values of 11.05 and 12.77 mu M, respectively. In addition, compound 5e was found to induce apoptosis in RKO cells, as assessed by TUNEL assay. The results suggest that compound 5e may be a promising prototype anticancer agent.

引用

页码：430 / 441

页数：12

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