Article ID Journal Published Year Pages File Type
5214384 Tetrahedron 2015 8 Pages PDF
Abstract

The first synthesis of fradcarbazole A (1) has been accomplished by using a biomimetic intramolecular cyclization/dehydration to construct the staurosporine-thiazole-indole skeleton. The phenyl and oxazole analogues of fradcarbazole A (2-4) were also synthesized using the same strategy. Compounds 1-4 displayed cytotoxicity against A549 cell line with IC50 values of 0.4-3.6 μM, induction of G0/G1 arrest of A549 cell cycle at 10 μM, and inhibition of PKC-β kinase with IC50 values of 0.5-0.9 μM.

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Physical Sciences and Engineering Chemistry Organic Chemistry
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