Identification of potent and selective TACE inhibitors via the S1 pocket.
ABSTRACT By focusing on the P1 portion of the piperidine beta-sulfone ligands we identified a motif that induces selectivity and resulted in a series of TACE inhibitors that demonstrated excellent in vitro potency against isolated TACE enzyme and excellent selectivity over MMPs 1, 2, 9, 13, and 14.
- SourceAvailable from: Malkeet Singh BahiaJournal of Molecular Modeling 01/2011; 17(1):9. · 1.98 Impact Factor
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ABSTRACT: A four step preparative scale synthesis of eight 2-alkyl- and arylsubstituted thiazole-4-sulfonyl chlorides from chloralamides is reported. Good yields and easy availability of starting materials are valuable advantages of the procedure that gives access to formerly unattainable building blocks.Synthetic Communications 01/2012; 42(19):2866-2875. · 1.06 Impact Factor
- Letters in Drug Design & Discovery 01/2011; 8:430. · 0.85 Impact Factor