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Bioorg Med Chem. 2012 Nov 1;20(21):6465-81. doi: 10.1016/j.bmc.2012.08.026. Epub 2012 Aug 28.

Potent small molecule Hedgehog agonists induce VEGF expression in vitro.

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Universität Leipzig, Fakultät für Chemie und Mineralogie, Institut für Organische Chemie, Johannisallee 29, 04103 Leipzig, Germany.


Here, we describe the synthesis, SAR studies as well as biological investigations of the known Hedgehog signaling agonist SAG and a small library of its analogues. The SAG and its derivatives were analyzed for their potency to activate the expression of the Hh target gene Gli1 in a reporter gene assay. By analyzing SAR important molecular descriptors for Gli1 activation have been identified. SAG as well as compound 10c proven to be potent activators of VEGF expression in cultivated dermal fibroblasts. Importantly and in contrast to SAG, derivative 10c displayed no toxicity in concentrations up to 250 μm.

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