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

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 antiproliferativ...

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Autores principales: Guan, Xianghong, Luo, Peihua, He, Qiaojun, Hu, Yongzhou, Ying, Huazhou
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2016
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6155728/
https://www.ncbi.nlm.nih.gov/pubmed/28035983
http://dx.doi.org/10.3390/molecules22010032
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author Guan, Xianghong
Luo, Peihua
He, Qiaojun
Hu, Yongzhou
Ying, Huazhou
author_facet Guan, Xianghong
Luo, Peihua
He, Qiaojun
Hu, Yongzhou
Ying, Huazhou
author_sort Guan, Xianghong
collection PubMed
description 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.
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spelling pubmed-61557282018-11-13 Design, Synthesis and Evaluation of Indene Derivatives as Retinoic Acid Receptor α Agonists Guan, Xianghong Luo, Peihua He, Qiaojun Hu, Yongzhou Ying, Huazhou Molecules Article 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. MDPI 2016-12-27 /pmc/articles/PMC6155728/ /pubmed/28035983 http://dx.doi.org/10.3390/molecules22010032 Text en © 2016 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC-BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Guan, Xianghong
Luo, Peihua
He, Qiaojun
Hu, Yongzhou
Ying, Huazhou
Design, Synthesis and Evaluation of Indene Derivatives as Retinoic Acid Receptor α Agonists
title Design, Synthesis and Evaluation of Indene Derivatives as Retinoic Acid Receptor α Agonists
title_full Design, Synthesis and Evaluation of Indene Derivatives as Retinoic Acid Receptor α Agonists
title_fullStr Design, Synthesis and Evaluation of Indene Derivatives as Retinoic Acid Receptor α Agonists
title_full_unstemmed Design, Synthesis and Evaluation of Indene Derivatives as Retinoic Acid Receptor α Agonists
title_short Design, Synthesis and Evaluation of Indene Derivatives as Retinoic Acid Receptor α Agonists
title_sort design, synthesis and evaluation of indene derivatives as retinoic acid receptor α agonists
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6155728/
https://www.ncbi.nlm.nih.gov/pubmed/28035983
http://dx.doi.org/10.3390/molecules22010032
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