Design and Synthesis of New Chacones Substituted with Azide/Triazole Groups and Analysis of Their Cytotoxicity Towards HeLa Cells

被引：23

作者：

da Silva, Graziele D. ^{[1
]}

da Silva, Marina G. ^{[1
]}

Souza, Estrela M. P. V. E. ^{[2
]}

Barison, Andersson ^{[2
]}

Simoes, Sarah C. ^{[3
]}

Varotti, Fernando P. ^{[3
]}

Barbosa, Leandro A. ^{[4
]}

Viana, Gustavo H. R. ^{[1
]}

Villar, Jose A. F. P. ^{[1
]}

机构：

[1] Univ Fed Sao Joao Del Rei, Lab Sintese Organ, BR-35501296 Divinopolis, MG, Brazil

[2] Univ Fed Parana, Lab RMN, BR-81531990 Curitiba, Parana, Brazil

[3] Univ Fed Sao Joao Del Rei, Lab Bioquim Parasitos, BR-35501296 Divinopolis, MG, Brazil

[4] Univ Fed Sao Joao Del Rei, Lab Bioquim Celular, BR-35501296 Divinopolis, MG, Brazil

来源：

MOLECULES | 2012年 / 17卷 / 09期

关键词：

chalcone; cycloaddition; O-alkylation; HeLa cells; BIOLOGICAL EVALUATION; NATURAL-PRODUCTS; CHALCONE; DERIVATIVES;

D O I：

10.3390/molecules170910331

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of new chalcones substituted with azide/triazole groups were designed and synthesized, and their cytotoxic activity was evaluated in vitro against the HeLa cell line. O-Alkylation, Claisen-Schmidt condensation and Cu(I)-catalyzed cycloaddition of azides with terminal alkynes were applied in key steps. Fifteen compounds were tested against HeLa cells. Compound 8c was the most active molecule, with an IC50 value of 13.03 mu M, similar to the value of cisplatin (7.37 mu M).

引用

页码：10331 / 10343

页数：13

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