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Biological Evaluation of Structurally Simplified Staurosporine Analogs on Protein Kinase C Inhibition
Author(s) -
Mowery Patricia,
Pelkey Erin
Publication year - 2015
Publication title -
the faseb journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.709
H-Index - 277
eISSN - 1530-6860
pISSN - 0892-6638
DOI - 10.1096/fasebj.29.1_supplement.721.13
Subject(s) - staurosporine , protein kinase c , chemistry , kinase , small molecule , potency , protein kinase a , biochemistry , stereochemistry , pharmacology , in vitro , biology
Protein kinase C (PKC) is involved in a number of diseases including certain cancers. The most studied inhibitor of PKC is staurosporine, a small molecule produced by Streptomyces spp. We have generated new analogs of staurosporine with simplified heterocyclic backbones using coupling reactions of tetramic acid derivatives as a key synthetic step. We have tested our analogs for their impacts in cell cytotoxicty MTT assays in order to examine their potency. Initial results indicate that size and planar characteristics of the analogs impact their effectiveness at inducing cell toxicity. From these studies we hope to determine structural lessons for PKC inhibition.