Beilstein J. Org. Chem.2017,13, 2561–2568, doi:10.3762/bjoc.13.252
imidazo[1,5-a]pyrazine structure show inhibitory activity against kinases BTK [1], MEK [2], ACK1 [3], mTORC1(2) [4], c-Src [5], growth factor IGF-1R [6] and act as the antagonists of Hedgehogpathway dependent malignancies [7]. Imidazo[1,5-a]pyrimidines are inhibitors of the bone morphogenic protein [8
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Graphical Abstract
Scheme 1:
Intramolecular cyclization of 3-(aminomethyl)pyridazines and related compounds (route A). Condition...
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 hedgehogpathway. 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; hedgehogpathway; inhibitor; Sant-75; synthesis; Introduction
The Hedgehog (Hh) signaling pathway plays an essential role in embryonic development and adult tissue homeostasis in metazoans
compounds as Hedgehog-pathway inhibitors. Therefore, the emphasis of the fourth series of structural optimization was placed on the nitrogen atom through capping of the amino group with various acyl chlorides, delivering the corresponding amides 21a–j. It should be noted that the capping of the amino group
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Graphical Abstract
Figure 1:
Structures of Smo antagonists and agonists.