Literature DB >> 11934588

Anthranilate sulfonamide hydroxamate TACE inhibitors. Part 2: SAR of the acetylenic P1' group.

J I Levin1, J M Chen, M T Du, F C Nelson, L M Killar, S Skala, A Sung, G Jin, R Cowling, D Barone, C J March, K M Mohler, R A Black, J S Skotnicki.   

Abstract

The SAR of a series of potent sulfonamide hydroxamate TACE inhibitors bearing novel acetylenic P1' groups was explored. In particular, compound 4t bearing a butynyloxy P1' moiety has excellent in vitro potency against isolated TACE enzyme and in cells, good selectivity over MMP-1 and oral activity in an in vivo model of TNF-alpha production.

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Year:  2002        PMID: 11934588     DOI: 10.1016/s0960-894x(02)00136-1

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  4 in total

Review 1.  Application of structural dynamic approaches provide novel insights into the enzymatic mechanism of the tumor necrosis factor-alpha-converting enzyme.

Authors:  Irit Sagi; Marcos E Milla
Journal:  Anal Biochem       Date:  2007-09-26       Impact factor: 3.365

2.  Anthranilate derivatives as TACE inhibitors: docking based CoMFA and CoMSIA analyses.

Authors:  Malkeet Singh Bahia; Shravan Kumar Gunda; Shwetha Reddy Gade; Saikh Mahmood; Ravikumar Muttineni; Om Silakari
Journal:  J Mol Model       Date:  2010-03-28       Impact factor: 1.810

3.  Antimicrobial and anticancer activity of some novel fluorinated thiourea derivatives carrying sulfonamide moieties: synthesis, biological evaluation and molecular docking.

Authors:  Mostafa M Ghorab; Mansour S Alsaid; Mohamed S A El-Gaby; Mahmoud M Elaasser; Yassin M Nissan
Journal:  Chem Cent J       Date:  2017-04-07       Impact factor: 4.215

4.  Schiff bases of sulphonamides as a new class of antifungal agent against multidrug-resistant Candida auris.

Authors:  Asad Hamad; Yiyuan Chen; Mohsin A Khan; Shirin Jamshidi; Naima Saeed; Melanie Clifford; Charlotte Hind; J Mark Sutton; Khondaker Miraz Rahman
Journal:  Microbiologyopen       Date:  2021-08       Impact factor: 3.139

  4 in total

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