Download MendeleyNovel thiol-based TACE inhibitors: rational design, synthesis, and SAR of thiol-containing aryl sulfonamides
Govinda Rao, B., Bandarage, U.K., Wang, T., Come, J.H., Perola, E., Wei, Y., Tian, S.K., Saunders, J.O.(2007) Bioorg Med Chem Lett 17: 2250-2253
- PubMed: 17289381
- DOI: https://doi.org/10.1016/j.bmcl.2007.01.064
- Primary Citation of Related Structures:
2OI0 - PubMed Abstract:
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.
Organizational Affiliation:
Vertex Pharmaceuticals Inc., 130 Waverly Street, Cambridge, MA 02139, USA. govinda_rao@vrtx.com
