|
|||||
|
|
Discovery of N-[(1-aryl-1H-indazol-5-yl)methyl]amides derivatives as smoothened antagonists for inhibition of the hedgehog pathway |
|
| Authors: | Gabriella Dessole Danila Branca Federica Ferrigno Olaf Kinzel Ester Muraglia Maria Cecilia Palumbi Michael Rowley Sergio Serafini Christian Steinkühler Philip Jones |
| Institution: | IRBM—Merck Research Laboratories Rome, Via Pontina km 30,600, Pomezia 00040, Rome, Italy |
| Abstract: | We report the synthesis and biological evaluation of N-(1-aryl-1H-indazol-5-yl)methyl]amide derivatives as Smoothened antagonists and inhibitors of the Hedgehog pathway. Identification of the lead structure 1 by HTS, followed by SAR study on the amide and aryl portions led to the discovery of antagonists with nanomolar activity. |
| Keywords: | |
| 本文献已被 ScienceDirect 等数据库收录！ | |