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

Overview

Journal Molecules

Publisher MDPI

Specialty Biology

Date 2012 Aug 31

PMID 22932214

Citations 6

Authors

Graziele D da Silva

Marina G da Silva

Estrela M P V E Souza

Andersson Barison

Sarah C Simoes

Fernando P Varotti

Leandro A Barbosa

Gustavo H R Viana

Jose A F P Villar

Affiliations

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Abstract

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 μM, similar to the value of cisplatin (7.37 μM).

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