Work

Design, synthesis and initial biological evaluation of a novel pladienolide analog scaffold

Year: 2011

Type: article

Abstract: A novel and simplified synthetic scaffold based on pladienolide was designed using a consensus pharmacophore hypothesis. An initial target was synthesized and evaluated to examine the role of the 3-hydroxy group and the methyl groups present at positions 10, 16, 20, 22 in 1, on biological activity. We report the first totally synthetic analog of this macrolide that shows biological activity. Our novel synthetic strategy enables the rapid synthesis of other new analogs of pladienolide in order to develop selective anticancer lead compounds.

Source: MedChemComm

DOI: 10.1039/c1md00040c

Authors: Mahesh Kumar Gundluru, Alan Pourpak, Xiaoli Cui, Stephan W. Morris, Thomas R. Webb

Institution: St. Jude Children's Research Hospital

Language: English

Topic: Biological Activity of Diterpenoids and Biflavonoids

Subfield: Organic Chemistry

Field: Chemistry

Domain: Physical Sciences

SDG: Good health and well-being

Open Access status: green

Funder: National Cancer Institute