Pharmacology Research Today is a free monthly online journal that collates and summarizes the latest research about Pharmacology, including details on pharmacogenomics, drug development, new medications. | ||||||||
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Novel thiol-based TACE inhibitors: rational design, synthesis, and SAR of thiol-containing aryl sulfonamides.Govinda Rao B, Bandarage UK, Wang T, Come JH, Perola E, Wei Y, Tian SK, Saunders JO Vertex Pharmaceuticals Inc., 130 Waverly Street, Cambridge, MA 02139, USA. govinda_rao@vrtx.com A series of potent thiol-containing aryl sulfonamide TACE inhibitors was designed and synthesized. The SAR and MMP selectivity of the series were investigated. In particular, compound 4b has shown excellent in vitro potency against the isolated TACE enzyme and good selectivity over MMP-2, -7, -8, -9, and -13. The X-ray structure of 4b bound to TACE was obtained. Published 2 April 2007 in Bioorg Med Chem Lett, 17(8): 2250-3.
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