Issue 9, 2011
From the journal:

MedChemComm

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

Mahesh Kumar Gundluru,a   Alan Pourpak,b   Xiaoli Cui,b   Stephan W. Morrisbc  and  Thomas R. Webb*a  

* Corresponding authors

a Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, 262 Danny Thomas Place, Memphis, Tennessee, U.S.A
E-mail: thomas.webb@stjude.org
Fax: +901 595 5715
Tel: +901 595 3928

b Pathology, St. Jude Children's Research Hospital, 262 Danny Thomas Place, Memphis, Tennessee, U.S.A

c Oncology, St. Jude Children's Research Hospital, 262 Danny Thomas Place, Memphis, Tennessee, U.S.A

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.

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

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Article information

DOI
https://doi.org/10.1039/C1MD00040C
Article type
Concise Article
Submitted
09 Feb 2011
Accepted
30 Jun 2011
First published
21 Jul 2011

Med. Chem. Commun., 2011,2, 904-908

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

M. K. Gundluru, A. Pourpak, X. Cui, S. W. Morris and T. R. Webb, Med. Chem. Commun., 2011, 2, 904 DOI: 10.1039/C1MD00040C

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