Cargando…
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...
Autores principales: | , , , , |
---|---|
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 |
_version_ | 1783357953798045696 |
---|---|
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. |
format | Online Article Text |
id | pubmed-6155728 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2016 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
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 |
work_keys_str_mv | AT guanxianghong designsynthesisandevaluationofindenederivativesasretinoicacidreceptoraagonists AT luopeihua designsynthesisandevaluationofindenederivativesasretinoicacidreceptoraagonists AT heqiaojun designsynthesisandevaluationofindenederivativesasretinoicacidreceptoraagonists AT huyongzhou designsynthesisandevaluationofindenederivativesasretinoicacidreceptoraagonists AT yinghuazhou designsynthesisandevaluationofindenederivativesasretinoicacidreceptoraagonists |