| Literature DB >> 20149966 |
Wen Cai1, Mary Hassani, Rajesh Karki, Ervin D Walter, Katherine H Koelsch, Hassan Seradj, Jayana P Lineswala, Hamid Mirzaei, Jeremy S York, Fatemeh Olang, Minoo Sedighi, Jennifer S Lucas, Thomas J Eads, Anthony S Rose, Sahba Charkhzarrin, Nicholas G Hermann, Howard D Beall, Mohammad Behforouz.
Abstract
A series of lavendamycin analogues with two, three or four substituents at the C-6, C-7 N, C-2', C-3' and C-11' positions were synthesized via short and efficient methods and evaluated as potential NAD(P)H:quinone oxidoreductase (NQO1)-directed antitumor agents. The compounds were prepared through Pictet-Spengler condensation of the desired 2-formylquinoline-5,8-diones with the required tryptophans followed by further needed transformations. Metabolism and toxicity studies demonstrated that the best substrates for NQO1 were also the most selectively toxic to NQO1-rich tumor cells compared to NQO1-deficient tumor cells. Copyright 2010 Elsevier Ltd. All rights reserved.Entities:
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Year: 2010 PMID： 20149966 PMCID： PMC2841014 DOI： 10.1016/j.bmc.2010.01.037
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641