茚衍生物作为维甲酸受体α激动剂的设计、合成与评价
Design, Synthesis and Evaluation of Indene Derivatives as Retinoic Acid Receptor α Agonists.
作者信息
Guan Xianghong, Luo Peihua, He Qiaojun, Hu Yongzhou, Ying Huazhou
机构信息
ZJU-ENS Joint Laboratory of Medicinal Chemistry, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China.
出版信息
Molecules. 2016 Dec 27;22(1):32. doi: 10.3390/molecules22010032.
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-1-inden-5-yl)-carbamoyl)benzoic acid (), 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.
一系列新型茚衍生的视黄酸受体α（RARα）激动剂已被设计并合成。受体结合、细胞增殖和细胞分化试验表明，这些化合物中的大多数表现出中等的RARα结合活性和强大的抗增殖活性。特别是，4-((3-异丙氧基-2,3-二氢-1-茚-5-基)-氨基甲酰基)苯甲酸（）显示出中等的结合亲和力，具有诱导NB4细胞分化的巨大潜力（5 μM时为68.88%）。重要的是，我们的工作确立了茚作为开发新型RARα激动剂的有前景的骨架。
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