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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. Compound 15h 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. (C) 2017 Elsevier Ltd. All rights reserved.
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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN: 0960-894X
Year: 2017
Issue: 15
Volume: 27
Page: 3259-3263
2 . 4 4 2
JCR@2017
2 . 8 2 3
JCR@2020
ESI Discipline: CHEMISTRY;
ESI HC Threshold:160
JCR Journal Grade:2
CAS Journal Grade:3
Cited Count:
WoS CC Cited Count: 4
SCOPUS Cited Count: 6
ESI Highly Cited Papers on the List: 0 Unfold All
WanFang Cited Count:
Chinese Cited Count:
30 Days PV: 0