第 49 卷第 1 期 Vol. 49 No. 1 2019 年 2 月 Feb 2019

所属栏目：医药及中间体 芳乙烯类化合物的合成及其细胞IDO1酶抑制活性研究

卜艳鑫，毕 弋，王婉秋，柴宝山，王云华，光海红，冉兆晋* （沈阳化工研究院有限公司，辽宁 沈阳 110021）

摘　要：以4-氯-3-硝基苯乙酮为起始原料，经取代、witting反应、还原、与相应取代的异氰酸酯缩合，制备了9种带有芳乙烯结构的新型IDO1抑制剂。并基于HeLa细胞的犬尿氨酸（kyn）测定法评估了它们对IDO1酶抑制活性。其结构经1H NMR确证。

关键词：IDO1抑制剂；芳香族乙烯；IDO1抑制活性

中图分类号：O626.24　　文献标识码：A　　文章编号：1009-9212（2019）01-0013-05

Synthesis of Aromatic Ethylene Compounds as IDO1 Inhibitors and Their Inhibitory Activity of IDO1 Enzyme in Cells

BU Yan-xin, BI Yi, WANG Wan-qiu, CHAI Bao-shan, WANG Yun-hua, GUANG Hai-hong, RAN Zhao-jin* (Pharmaceutical Research Laboratory, Shenyang Research Institute of Chemical Industry Co., Ltd., Shenyang 110021, China)

Abstract：4-Chloro-3-nitroacetophenone was used as the starting material, and 9 kinds of novel IDO1 inhibitors with arylene structure were prepared through a series of reactions including substitution, witting reaction, reduction and condensation with corresponding substituted isocyanates. Their inhibitory activity against IDO1 enzymes was evaluated based on HeLa cell-based kynurenine (kyn) assays. The structure of the target compound was confirmed by 1H NMR.

Key words：IDO1 inhibitor; aromatic ethylene; antiproliferative activity

基金项目：辽宁省自然科学基金指导计划（20170540730）。

作者简介：卜艳鑫（1989-），女，辽宁沈阳人，硕士，研究方向：药物化学。

联 系 人：冉兆晋，高级工程师，研究方向：药物化学与有机化学（E-mail：ranzhaojin@163.com）。

收稿日期： 2019-02-0