In:
Chemical Biology & Drug Design, Wiley, Vol. 97, No. 3 ( 2021-03), p. 546-552
Abstract:
The hedgehog (Hh) signaling pathway is involved in diverse aspects of cellular events. Aberrant activation of Hh signaling pathway drives oncogenic transformation for a wide range of cancers, and it is therefore a promising target in cancer therapy. In the principle of association and ring‐opening, we designed and synthesized a series of Hh signaling pathway inhibitors with phenyl imidazole scaffold, which were biologically evaluated in Gli‐Luc reporter assay. Compound 25 was identified to possess high potency with nanomolar IC 50 , and moreover, it preserved the inhibition against wild‐type and drug‐resistant Smo‐overexpressing cells. A molecular modeling study of compound 25 expounded its binding mode to Smo receptor, providing a basis for the further structural modification of phenyl imidazole analogs.
Type of Medium:
Online Resource
ISSN:
1747-0277
,
1747-0285
Language:
English
Publisher:
Wiley
Publication Date:
2021
detail.hit.zdb_id:
2216600-2
detail.hit.zdb_id:
2219858-1
SSG:
12
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