Issue 2, 2013
From the journal:

MedChemComm

A structure–activity relationship study on multi-heterocyclic molecules: two linked thiazoles are required for cytotoxic activity†

Seong Jong Kim,a   Chun-Chieh Lin,b   Chung-Mao Pan,b   Dimple P. Rananaware,a   Deborah M. Ramseya  and  Shelli R. McAlpine*a  

* Corresponding authors

a School of Chemistry, 219 Dalton, Gate 2 High Street, University of New South Wales, Sydney, NSW, Australia
E-mail: s.mcalpine@unsw.edu.au
Fax: +61-2-9385-4000
Tel: +61-4-1672-8896

b Department of Chemistry, San Diego State University, 5500 Campanile Drive, San Diego, CA 92182-1030, USA

Abstract

We report the synthesis, cytotoxicity, and phenotypic analysis of oxazole and thiazole containing fragments. Evaluating the optimal size and heterocycle for growth inhibition and apoptosis showed that activity required at least two thiazoles sequentially connected. This is the first detailed comparison of biological activity between multi-heterocyclic containing fragments.

Graphical abstract: A structure–activity relationship study on multi-heterocyclic molecules: two linked thiazoles are required for cytotoxic activity

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Article information

DOI
https://doi.org/10.1039/C2MD20291C
Article type
Concise Article
Submitted
28 Sep 2012
Accepted
27 Nov 2012
First published
29 Nov 2012

Med. Chem. Commun., 2013,4, 406-410

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A structure–activity relationship study on multi-heterocyclic molecules: two linked thiazoles are required for cytotoxic activity

S. J. Kim, C. Lin, C. Pan, D. P. Rananaware, D. M. Ramsey and S. R. McAlpine, Med. Chem. Commun., 2013, 4, 406 DOI: 10.1039/C2MD20291C

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