The enone motif of (+)-grandifloracin is not essential for 'anti-austerity' antiproliferative activity

Monika Ali Khan, Pauline J. Wood, Natasha M. Lamb-Guhren, Lorenzo Caggiano, Gabriele Kociok-Köhn, David Tosh, Simon E. Lewis

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Abstract

We report the synthesis and biological evaluation of three analogues of the natural product (+)-grandifloracin (+)-1. All three analogues exhibit enhanced antiproliferative activity against PANC-1 and HT-29 cells compared to the natural product. The retention of activity in an analogue lacking the enone functional group, 9, implies this structural element is not an essential part of the (+)-grandifloracin pharmacophore.
Original languageEnglish
Pages (from-to)2815-2819
Number of pages5
JournalBioorganic & Medicinal Chemistry Letters
Volume24
Issue number13
Early online date5 May 2014
DOIs
Publication statusPublished - 1 Jul 2014

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Biological Products
HT29 Cells
Functional groups
grandifloracin

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The enone motif of (+)-grandifloracin is not essential for 'anti-austerity' antiproliferative activity. / Ali Khan, Monika; Wood, Pauline J.; Lamb-Guhren, Natasha M.; Caggiano, Lorenzo; Kociok-Köhn, Gabriele; Tosh, David; Lewis, Simon E.

In: Bioorganic & Medicinal Chemistry Letters, Vol. 24, No. 13, 01.07.2014, p. 2815-2819.

Research output: Contribution to journalArticle

Ali Khan, Monika ; Wood, Pauline J. ; Lamb-Guhren, Natasha M. ; Caggiano, Lorenzo ; Kociok-Köhn, Gabriele ; Tosh, David ; Lewis, Simon E. / The enone motif of (+)-grandifloracin is not essential for 'anti-austerity' antiproliferative activity. In: Bioorganic & Medicinal Chemistry Letters. 2014 ; Vol. 24, No. 13. pp. 2815-2819.
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