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Abstract:
In present study, a series of novel containing trifluoromethyl 4-(2-pyrimidinylamino) benzamide derivatives were designed by the fluorine scan strategy. Their Hh signaling inhibitory activities were evaluated by Gli-luciferase reporter method. The comprehensive SAR was discussed and several derivatives were found to display more potent Hh signaling inhibitory activity than positive drug vismodegib. Compound 13d was the most potent compound with IC50 of 1.44 nM against Hh signaling pathway and also exhibited optimal PK properties in the in vivo PK properties study, deserved as an ideal lead compound for further study in future. (C) 2016 Elsevier Ltd. All rights reserved.
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BIOORGANIC & MEDICINAL CHEMISTRY
ISSN: 0968-0896
Year: 2016
Issue: 5
Volume: 24
Page: 1079-1088
2 . 9 3
JCR@2016
3 . 6 4 1
JCR@2020
ESI Discipline: CHEMISTRY;
ESI HC Threshold:177
JCR Journal Grade:2
CAS Journal Grade:3
Cited Count:
WoS CC Cited Count: 11
SCOPUS Cited Count: 10
ESI Highly Cited Papers on the List: 0 Unfold All
WanFang Cited Count:
Chinese Cited Count:
30 Days PV: 3