Structural simplification of bioactive natural products with multicomponent synthesis. 4. 4H-pyrano-[2,3-b]naphthoquinones with anticancer activity

Bioorg Med Chem Lett. 2012 Aug 15;22(16):5195-8. doi: 10.1016/j.bmcl.2012.06.073.

Igor V Magedov ¹, Artem S Kireev, Aaron R Jenkins, Nikolai M Evdokimov, Dustin T Lima, Paul Tongwa, Jeff Altig, Wim F A Steelant, Severine Van slambrouck, Mikhail Yu Antipin, Alexander Kornienko

Affiliations

Affiliation

1 Department of Chemistry, New Mexico Institute of Mining and Technology, Socorro, NM 87801, USA. imagedov@nmt.edu

PMID: 22819765 DOI: 10.1016/j.bmcl.2012.06.073

Abstract

4H-Pyrano-[2,3-b]naphthoquinone is a structural motif commonly found in Natural Products manifesting Anticancer activities. As part of a program aimed at structural simplification of bioactive Natural Products utilizing multicomponent synthetic processes, we developed a compound library based on this heterocyclic scaffold. We found that several library members displayed low micromolar antiproliferative activity and induced Apoptosis in human Cancer cells. Selected compounds showed promising activity against Cancer cell lines resistant to proapoptotic stimuli, demonstrating their potential in treating cancers with dismal prognoses.

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