|
|||||
|
|
Synthesis, preliminary biological evaluation and molecular modeling of some new heterocyclic inhibitors of TACE |
|
| Authors: | Sengupta Prabal Puri Chetan S Chokshi Hemant A Sheth Chetana K Midha Ajay S Chitturi Trinadha Rao Thennati Rajamannar Murumkar Prashant R Yadav Mange Ram |
| Affiliation: | aOrganic Synthesis Division, Sun Pharma Advanced Research Company Ltd., Tandalja, Vadodara 390012, Gujarat, India;bPharmacy Department, Faculty of Technology and Engineering, Kalabhavan, The M. S. University of Baroda, Vadodara 390001, Gujarat, India |
| 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. |
| Keywords: | TACE inhibitor Hydroxamates TNF-α Molecular modeling |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |