1004517-05-8Relevant articles and documents
Design and biological evaluation of phenyl imidazole analogs as hedgehog signaling pathway inhibitors
Sun, Chiyu,Zhang, Ying,Wang, Han,Yin, Zhengxu,Wu, Lingqiong,Huang, Yanmiao,Zhang, Wenhu,Wang, Youbing,Hu, Qibo
, p. 546 - 552 (2020/10/06)
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 IC50, 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.
COMPOUNDS AND COMPOSITIONS AS HEDGEHOG PATHWAY MODULATORS
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Page/Page column 34-35, (2008/06/13)
The invention provides a method for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-fu
