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Open AccessArticle

Design, Synthesis and Evaluation of Indene Derivatives as Retinoic Acid Receptor α Agonists

ZJU-ENS Joint Laboratory of Medicinal Chemistry, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China
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Academic Editor: Santosh K. Katiyar
Molecules 2017, 22(1), 32; https://doi.org/10.3390/molecules22010032
Received: 4 November 2016 / Revised: 22 December 2016 / Accepted: 24 December 2016 / Published: 27 December 2016
(This article belongs to the Special Issue Cancer Chemoprevention)
A series of novel indene-derived retinoic acid receptor α (RARα) agonists have been designed and synthesized. The use of receptor binding, cell proliferation and cell differentiation assays demonstrated that most of these compounds exhibited moderate RARα binding activity and potent antiproliferative activity. In particular, 4-((3-isopropoxy-2,3-dihydro-1H-inden-5-yl)-carbamoyl)benzoic acid (36d), which showed a moderate binding affinity, exhibited a great potential to induce the differentiation of NB4 cells (68.88% at 5 μM). Importantly, our work established indene as a promising skeleton for the development of novel RARα agonists. View Full-Text
Keywords: retinoic acid receptor; agonist; all-trans-retinoic acid derivative; indene; structure and activity relationship retinoic acid receptor; agonist; all-trans-retinoic acid derivative; indene; structure and activity relationship
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MDPI and ACS Style

Guan, X.; Luo, P.; He, Q.; Hu, Y.; Ying, H. Design, Synthesis and Evaluation of Indene Derivatives as Retinoic Acid Receptor α Agonists. Molecules 2017, 22, 32.

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