Synthesis and in vitro evaluation of novel triazole/azide chalcones

被引：9

作者：

Evangelista, Fernanda C. G. ^{[1
]}

Bandeira, Maralice O. ^{[2
]}

Silva, Graziele D. ^{[3
]}

Silva, Marina G. ^{[3
]}

Andrade, Silmara N. ^{[2
]}

Marques, Deisielly R. ^{[2
]}

Silva, Luciana M. ^{[4
]}

Castro, Whocely V. ^{[2
]}

Santos, Fabio V. ^{[2
]}

Viana, Gustavo H. R. ^{[2
]}

Villar, Jose A. F. P. ^{[3
]}

Sabino, Adriano P. ^{[1
]}

Varotti, Fernando P. ^{[2
]}

机构：

[1] Univ Fed Minas Gerais, Dept Anal Clin & Toxicol, Fac Farm, Av Antonio Carlos 6627, BR-31270901 Belo Horizonte, MG, Brazil

[2] UFSJ, Nucleo Pesquisa Quim Biol NQBio, Av Sebastiao Goncalves Coelho 400, BR-35501296 Divinopolis, MG, Brazil

[3] UFSJ, Lab Sintese Organ & NanoEstruturas, Av Sebastiao Goncalves Coelho 400, BR-35501296 Divinopolis, MG, Brazil

[4] Fundacao Ezequiel Dias FUNED, Rua Conde Pereira Carneiro 80, BR-30510010 Belo Horizonte, MG, Brazil

来源：

MEDICINAL CHEMISTRY RESEARCH | 2017年 / 26卷 / 01期

关键词：

Chalcones; Cytotoxicity; TP53; gene; BIOLOGICAL EVALUATION; ANTICANCER ACTIVITY; CYTOTOXIC ACTIVITY; ANTIMALARIAL ACTIVITY; CANCER CELLS; DESIGN; DERIVATIVES; AGENTS; APOPTOSIS; CLASSIFICATION;

D O I：

10.1007/s00044-016-1705-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 30 novel triazole/azide chalcone derivatives were synthesized by Claisen-Schmidt and Cu(I)-catalyzed cycloaddition reactions. The antiproliferative activity of each compound was evaluated against HeLa, RKO-AS45-1 and Wi-26VA4 cell lines. Terminal deoxynucleotidyl transferase dUTP nick end labeling assays indicated that compounds 4j and 5j significantly reduced the HeLa and RKO-AS45-1cell populations compared to the controls. The relative expression of the TP53 gene revealed changes in both cell lines after exposure to compounds 5j and 4j. The increased expression of the TP53 gene suggests a cellular attempt to repair DNA damage and indicates these triazole/azide chalcone derivatives as promising anticancer agents.

引用

页码：27 / 43

页数：17

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