Anti-Cancer Agents in Medicinal Chemistry

(Formerly Current Medicinal Chemistry - Anti-Cancer Agents)

Michelle Prudhomme  
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex
France

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Synthesis and Structure Activity Relationship Study of N-substituted 3,5-diarylidenepiperidin- 4-ones as Potential Antitumor Agents

Author(s): Hala Bakr El-Nassan.

Abstract:

A new series of N-substituted diarylidenepiperidin-4-ones was synthesized and screened for their possible anticancer activity at the NCI Developmental Therapeutic Program. Almost all the synthesized compounds showed more potent antiproliferative activity than curcumin. The most active compound in this study was 3,5-bis(4-bromobenzylidene)-1-propanoylpiperidin-4-one (8a) with MGMID GI50, TGI, and LC50 values of 0.35, 1.62 and 9.12 µM, respectively. Compound 8a displayed broad spectrum antiproliferative activity with GI50 values below 1 µM in 81% of the tested cell lines and was found to be two folds more potent than EF-24. A detailed study of the structure activity relationship of the N-substitution was also described.

Keywords: Curcumin derivatives, antitumor, structure-activity relationship, 3, 5-diarylidene-4-piperidones.

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Article Details

VOLUME: 14
ISSUE: 2
Page: [319 - 330]
Pages: 12
DOI: 10.2174/18715206113136660859
Price: $58