Beilstein J. Org. Chem.2012,8, 841–849, doi:10.3762/bjoc.8.94
, Beijing 100871, China 10.3762/bjoc.8.94 Abstract Sant-75 is a newly identified potent inhibitor of the hedgehog pathway. We designed a diversity-oriented synthesis program, and synthesized a series of Sant-75 analogues, which lays the foundation for further investigation of the structure–activity
relationship of this important class of hedgehog-pathway inhibitors.
Keywords: chemical diversity; diversity-oriented; hedgehog pathway; inhibitor; Sant-75; synthesis; Introduction
The Hedgehog (Hh) signaling pathway plays an essential role in embryonic development and adult tissue homeostasis in metazoans
action, and thus it may serve as an interesting scaffold for drug development [35][36]. Recently, we have identified a Smo antagonist Sant-75 through zebrafish-based screening of a SAG-derived chemical library [37]. Interestingly, this antagonist differs from agonist SAG only in the chain length of the
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Graphical Abstract
Figure 1:
Structures of Smo antagonists and agonists.