Synthesis, preliminary biological evaluation and molecular modeling of some new heterocyclic inhibitors of TACE

  • Eur J Med Chem. 2011 Nov;46(11):5549-55. doi: 10.1016/j.ejmech.2011.09.018.
Prabal Sengupta  1 ,  Chetan S Puri ,  Hemant A Chokshi ,  Chetana K Sheth ,  Ajay S Midha ,  Trinadha Rao Chitturi ,  Rajamannar Thennati ,  Prashant R Murumkar ,  Mange Ram Yadav
Affiliations
  • 1. Organic Synthesis Division, Sun Pharma Advanced Research Company Ltd, Tandalja, Vadodara 390012, Gujarat, India.
PMID: 21963348 DOI: 10.1016/j.ejmech.2011.09.018
Abstract

Central heteroaryl ring analogues belonging to a series of potent hydroxamate TACE inhibitors were synthesized. The TACE inhibitory activities of these compounds were evaluated by in vitro WBA and in silico molecular modeling studies using crystal structure of human TACE. Compound 14 showed very good in vitro inhibition, supported by the in silico docking studies.

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