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Abstract:
A series of novel hedgehog signaling pathway inhibitors have been designed by structural modification based on the former reported scaffold of 4-(2-pyrimidinylamino)benzamide. The SAR for this series was described and many derivatives showed potent inhibitory activity. Among these compounds, compounds 12af and 12bf were identified to have high potency and optimal PK profiles. Although both of compounds 12af and 12bf did not show strong antitumor efficacy in LS-174T nude mice model, they were promising candidates as Hh signaling inhibitors due to great potency against Hh signaling pathway and outstanding PK properties, deserving further evaluation in other Hh signaling operative tumor models. (C) 2016 Elsevier Masson SAS. All rights reserved.
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EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
ISSN: 0223-5234
Year: 2016
Volume: 110
Page: 115-125
4 . 5 1 9
JCR@2016
6 . 5 1 4
JCR@2020
ESI Discipline: CHEMISTRY;
ESI HC Threshold:177
JCR Journal Grade:2
CAS Journal Grade:1
Cited Count:
WoS CC Cited Count: 9
SCOPUS Cited Count: 11
ESI Highly Cited Papers on the List: 0 Unfold All
WanFang Cited Count:
Chinese Cited Count:
30 Days PV: 5