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

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.

SUBMITTER: Gundluru MK 

PROVIDER: S-EPMC3171832 | biostudies-literature | 2011 Jan

REPOSITORIES: biostudies-literature

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

Gundluru Mahesh Kumar MK   Pourpak Alan A   Cui Xiaoli X   Morris Stephan W SW   Webb Thomas R TR  

MedChemComm 20110101 9

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  ...[more]

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