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A structure–activity relationship study on multi-heterocyclic molecules: two linked thiazoles are required for cytotoxic activity†
Seong Jong Kim,Chun-Chieh Lin,Chung-Mao Pan,Dimple P. Rananaware,Deborah M. Ramsey,Shelli R. McAlpine
MedChemComm Pub Date : 11/29/2012 00:00:00 , DOI:10.1039/C2MD20291C
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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