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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
biochemistry, genetics and molecular biology
Structure activity relationship and optimization of N-(3-(2-aminothiazol-4-yl)aryl)benzenesulfonamides as anti-cancer compounds against sensitive and resistant cells
Bioorganic and Medicinal Chemistry Letters, Volume 27, No. 10, Year 2017
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Description
We recently described a new family of bioactive molecules with interesting anti-cancer activities: the N-(4-(3-aminophenyl)thiazol-2-yl)acetamides. The lead compound of the series (1) displays significant anti-proliferative and cytotoxic activities against a panel of cancer cell lines, either sensitive or resistant to standard treatments. This molecule also shows a good pharmacological profile and high in vivo potency towards mice xenografts, without signs of toxicity on the animals. In the present article, we disclose the structure-activity relationships of this lead compound, which have provided clear information about the replacement of the acetamide function and the substitution pattern of the benzenesulfonamide ring. An improved high-yielding synthetic procedure towards these compounds has also been developed. Our drug design resulted in potency enhancement of 1, our new optimized lead compound being 19. These findings are of great interest to further improve this scaffold for the development of future clinical candidates. © 2017 Elsevier Ltd
Authors & Co-Authors
Ronco, Cyril
France, Nice
Institut de Chimie de Nice
Millet, Antoine
France, Nice
Institut de Chimie de Nice
Plaisant, Magali Dodille
France, Paris
Inserm
Abbe, Patricia
France, Paris
Inserm
Hamouda-Tekaya, Nedra
France, Paris
Inserm
Rocchi, Stéphane
France, Paris
Inserm
Benhida, Rachid
France, Nice
Institut de Chimie de Nice
Statistics
Citations: 10
Authors: 7
Affiliations: 2
Identifiers
Doi:
10.1016/j.bmcl.2017.03.054
ISSN:
0960894X
Research Areas
Cancer