Introduction of fluorine to phenyl group of 4-(2-pyrimidinylamino)benzamides leading to a series of potent hedgehog signaling pathway inhibitors. Issue 15 (1st August 2017)

• Record Type: Journal Article
• Authors: Xin, Minhang; Zhang, Liandi; Wen, Jun; Shen, Han; Zhao, Xinge; Jin, Qiu; Tang, Feng
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 27:Issue 15(2017)
• Page Start: 3259
• Page End: 3263
• Publication Date: 2017-08-01
• Subjects: Hedgehog signaling pathway inhibitors -- 4-(2-Pyrimidinylamino)benzamide scaffold -- Fluorine -- Most potent; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2017.06.030
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: In present study, a novel series of fluorine containing 4-(2-pyrimidinylamino)benzamide analogues were designed and synthesized. The hedgehog (Hh) signaling inhibitory activities for these compounds were evaluated by a luciferase reporter method. The preliminary SAR was discussed and many compounds showed potent Hh signaling inhibitory activities. Compound15h displayed the most potent inhibitory activity, with an IC50 of 0.050 nM. This paper finds the introduction of fluorine to the 4-(2-pyrimidinylamino)benzamide scaffold can lead to a novel series of potent Hh signaling pathway inhibitors.