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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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Detalles Bibliográficos
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
Descripción
Sumario: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.