Diarylpentanoids with antitumor activity: A critical review of structure-activity relationship studies

Diarypentanoids are commonly considered as monocarbonyl analogues of curcumin. Since the discovery of this compound in 1962, twenty one diarylpentanoids have been isolated and almost 600 synthetic analogues with antitumor activity have been synthesized. This review reports the exploitation of diaryl...

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Bibliographic Details
Published in:European journal of medicinal chemistry 2020-04, Vol.192, p.112177-112177, Article 112177
Main Authors: Moreira, Joana, Saraiva, Lucilia, Pinto, Madalena M., Cidade, Honorina
Format: Article
Language:English
Subjects:
Antitumor activity
C5-curcuminoids
Chemotherapy
Curcumin
Diarylpentanoids
Structure-activity relationship
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Summary:Diarypentanoids are commonly considered as monocarbonyl analogues of curcumin. Since the discovery of this compound in 1962, twenty one diarylpentanoids have been isolated and almost 600 synthetic analogues with antitumor activity have been synthesized. This review reports the exploitation of diarylpentanoids to develop curcumin analogues with improved antitumor activity over the last two decades. The mechanism of action and structure-activity relationship (SAR) studies are also highlighted. More importantly, structural features for the antitumor activity that may guide the design of new and more effective diarylpentanoids are also proposed. [Display omitted] •Synthetic diarylpentanoids, structure related with curcumin, with antitumor activity are reviewed.•Most compounds show greater antitumor activity than curcumin.•The mechanism of action of this class of compounds is discussed.•Structure-activity relationship studies for the antitumor activity are highlighted.•The most relevant molecular features for the antitumor activity of diarylpentanoids are also proposed.
ISSN:0223-5234
1768-3254
DOI:10.1016/j.ejmech.2020.112177