Structure based design of a series of potent and selective non peptidic PTP-1B inhibitors.

Journal Article (Journal Article)

A series of benzotriazole phenyldifluoromethylphosphonic acids were found to be potent PTP-1B inhibitors. Molecular modeling on the X-ray crystal structure of the lead structure led to the design of potent PTP-1B inhibitors that show moderate selectivity against TC-PTP, a very closely related protein tyrosine phosphatase.

Full Text

Duke Authors

Cited Authors

  • Lau, CK; Bayly, CI; Gauthier, JY; Li, CS; Therien, M; Asante-Appiah, E; Cromlish, W; Boie, Y; Forghani, F; Desmarais, S; Wang, Q; Skorey, K; Waddleton, D; Payette, P; Ramachandran, C; Kennedy, BP; Scapin, G

Published Date

  • February 2004

Published In

Volume / Issue

  • 14 / 4

Start / End Page

  • 1043 - 1048

PubMed ID

  • 15013020

Electronic International Standard Serial Number (EISSN)

  • 1464-3405

International Standard Serial Number (ISSN)

  • 0960-894X

Digital Object Identifier (DOI)

  • 10.1016/j.bmcl.2003.11.076


  • eng