期刊
ORGANIC & BIOMOLECULAR CHEMISTRY
卷 13, 期 11, 页码 3382-3392出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c4ob02694b
关键词
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资金
- Swedish Research Council
- Knut & Alice Wallenberg foundation
- Wilhelm and Martina Lundgrens Science Foundation
Design of Experiments (DoE) has been used to optimize a diversity oriented palladium catalyzed cascade Heck-Suzuki reaction for the construction of 3-alkenyl substituted cyclopenta[b]indole compounds. The obtained DoE model revealed a reaction highly dependent on the ligand. Guided by the model, an optimal ligand was chosen that selectively delivered the desired products in high yields. The conditions were applicable with a variety of boronic acids and were used to synthesize a library of 3-alkenyl derivatized compounds. Focusing on inhibition of kinases relevant for combating melanoma, the library was used in an initial structure-activity survey. In line with the observed kinase inhibition, cellular studies revealed one of the more promising derivatives to inhibit cell proliferation via an apoptotic mechanism.
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