Issue 2, 2014
From the journal:

MedChemComm

In vitro anticancer activity and SAR studies of triazolyl aminoacyl(peptidyl) penicillins†

Patricia G. Cornier,a   Carina M. L. Delpiccolo,a   Florencia C. Mascali,a   Dora B. Boggián,a   Ernesto G. Mata,*a   Mariano G. Cárdenas,b   Viviana C. Blankb  and  Leonor P. Roguin*b  

* Corresponding authors

a Instituto de Química Rosario (CONICET – UNR), Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Suipacha 531, 2000 Rosario, Argentina
E-mail: mata@iquir-conicet.gov.ar

b Instituto de Química y Fisicoquímica Biológicas (UBA – CONICET), Facultad de Farmacia y Bioquímica, Universidad de Buenos Aires, Junín 956, C1113AAD, Buenos Aires, Argentina

Abstract

A library of triazolyl aminoacyl(peptidyl) penicillins was designed, synthesized, and evaluated for their antiproliferative activity against HeLa and B16-F0 cell lines. Structure–activity relationship studies were carried out, and minimal structural requirements were determined. Among the tested compounds, derivatives 7f, 7p and 7m demonstrated the highest anticancer activity and a promising selectivity profile against these two cell lines.

Graphical abstract: In vitro anticancer activity and SAR studies of triazolyl aminoacyl(peptidyl) penicillins

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Article information

DOI
https://doi.org/10.1039/C3MD00332A
Article type
Concise Article
Submitted
30 Oct 2013
Accepted
30 Nov 2013
First published
04 Dec 2013

Med. Chem. Commun., 2014,5, 214-218

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In vitro anticancer activity and SAR studies of triazolyl aminoacyl(peptidyl) penicillins

P. G. Cornier, C. M. L. Delpiccolo, F. C. Mascali, D. B. Boggián, E. G. Mata, M. G. Cárdenas, V. C. Blank and L. P. Roguin, Med. Chem. Commun., 2014, 5, 214 DOI: 10.1039/C3MD00332A

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