863977-54-2Relevant academic research and scientific papers
Discovery of potent, selective and orally bioavailable triaryl-sulfonamide based PTP1B inhibitors
Patel, Dipam,Jain, Mukul,Shah, Shailesh R.,Bahekar, Rajesh,Jadav, Pradip,Joharapurkar, Amit,Dhanesha, Nirav,Shaikh, Mubeen,Sairam, Kalapatapu V.V.M.,Kapadnis, Prashant
supporting information; experimental part, p. 1111 - 1117 (2012/03/11)
A novel series of pTyr mimetics containing triaryl-sulfonamide derivatives (5a-r) are reported as potent and selective PTP1B inhibitors. Some of the test compounds (5o and 5p) showed excellent selectivity towards PTP1B over various PTPs, including TCPTP (
Discovery and structure-activity relationships of novel sulfonamides as potent PTP1B inhibitors
Holmes, Christopher P.,Li, Xianfeng,Pan, Yijun,Xu, Caiding,Bhandari, Ashok,Moody, Claire M.,Miguel, Joy A.,Ferla, Steven W.,De Francisco, M. Nuria,Frederick, Brian T.,Zhou, Siqun,Macher, Natalie,Jang, Larry,Irvine, Jennifer D.,Grove, J. Russell
, p. 4336 - 4341 (2007/10/03)
A series of novel sulfonamides containing a single difluoromethylene- phosphonate group were discovered to be potent inhibitors of protein tyrosine phosphatase 1B. Structure-activity relationships around the scaffold were investigated, leading to the identification of compounds with IC50 or Ki values in the low nanomolar range. These sulfonamide-based inhibitors exhibit 100 and 30 times higher inhibitory activity than the corresponding tertiary amines and carboxamides, respectively.
