Issue 15, 2017

Arylidene indanone scaffold: medicinal chemistry and structure–activity relationship view

Abstract

Arylidene indanone (AI) scaffolds are considered as the rigid cousins of chalcones, incorporating the α,β-unsaturated ketone system of chalcones forming a cyclic 5 membered ring. They are generally synthesized from 1-indanone and benzaldehydes via an aldol reaction. The furnished molecules have been explored as inhibitors of cholinesterases towards the treatment of Alzheimer’s disease, as tubulin depolymerizing agents, as inhibitors of breast cancer and leukemia, inhibitors of dual specificity phosphatase (DUSP), as antimalarials, and for many other uses. This review is an effort to highlight the biochemical effects of arylidene indanones designed from natural or known drug compounds, discuss their structure–activity relationships (SAR), and correlate them with related chalcones providing insights for further development of this scaffold.

Graphical abstract: Arylidene indanone scaffold: medicinal chemistry and structure–activity relationship view

Article information

Article type
Review Article
Submitted
21 Jan 2016
Accepted
14 Jan 2017
First published
31 Jan 2017
This article is Open Access
Creative Commons BY license

RSC Adv., 2017,7, 9357-9372

Arylidene indanone scaffold: medicinal chemistry and structure–activity relationship view

J. C. J. M. D. S. Menezes, RSC Adv., 2017, 7, 9357 DOI: 10.1039/C6RA28613E

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. You can use material from this article in other publications without requesting further permissions from the RSC, provided that the correct acknowledgement is given.

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