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

作者：Guan, Xianghong; Luo, Peihua; He, Qiaojun; Hu, Yongzhou; Ying, Huazhou^*

来源：Molecules, 2017, 22(1): 32.

DOI：10.3390/molecules22010032

• retinoic acid receptor
• agonist
• all-trans-retinoic acid derivative
• indene
• structure and activity relationship

A series of novel indene-derived retinoic acid receptor alpha (RAR alpha) 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 RAR alpha 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 mu M). Importantly, our work established indene as a promising skeleton for the development of novel RAR alpha agonists.

• 出版日期2017-1
• 单位浙江大学