杨亚玺 - 中国科学院上海药物研究所 -

个人简介

简历：中国科学院上海药物研究所，药物化学研究室，副研究员，硕士生导师教育经历： 2005/09-2010/06，华东理工大学，制药工程与技术专业工学博士（2006/03-2010/03，上海药物研究所李援朝研究员课题组联合培养） 2001/09-2005/06，西南大学，学士工作经历： 2012/11 – 至今，中国科学院上海药物研究所，副研究员 2012/07 – 2012/10，中国科学院上海药物研究所，助理研究员 2010/06 – 2012/06，中国科学院上海药物研究所，博士后

研究领域

1. 基于天然产物自身活性特点，对其活性单体进行修饰改造、构效关系研究及新药开发。代表性工作：雷公藤内酯醇构效关系研究及抗肿瘤新药开发。 2. 从事表观遗传修饰相关研究，基于靶点进行小分子抑制剂的设计合成。所涉及的靶点：menin-MLL，Bromodomain，EZH2，DOT1L等。 3. 开展金属催化的C-H活化方法学研究，高效构建活性小分子及天然产物骨架。

近期论文

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Yaxi Yang, Xuan Wang, Yuanchao Li, and Bing Zhou*, A [4+1] Cyclative Capture Approach to 3H-Indole-N-oxides at Room Temperature by Rhodium(III)-Catalyzed C-H Activation, Angew. Chem. Int. Ed., 2015, 54, 15400 -15404. Yaxi Yang, Wei Hou, Lihuai Qin, Juanjuan Du, Huijin Feng, Bing Zhou*, Yuanchao Li*, Rhodium-Catalyzed Directed Sulfenylation of Arene C–H Bonds, Chem. European J., 2014, 20, 416-420. Yaxi Yang, Longtai Zheng, Jingjing Shi, Bo Gao, Yanke Chen, Huichi Yang, Hongli Chen*, Yuanchao Li*, Xuechu Zhen*, Synthesis of 5 alpha-cholestan-6-one derivatives and their inhibitory activities of NO production in activated microglia: Discovery of a novel neuroinflammation inhibitor, Bioorg. Med. Chem. Lett., 2014, 24, 1222-1227. Bing Zhou†*, Yaxi Yang†, Sui Lin and Yuanchao Li*, Rhodium-Catalyzed Direct Addition of Indoles to N-Sulfonylaldimines, Adv. Synth. Catal., 2013, 355, 360-364. Yaxi Yang, Bing Zhou* and Yuanchao Li*, Rhodium-Catalyzed Oxidative ortho-Acylation of Aryl Ketone O-Methyl Oximes with Aryl and Alkyl Aldehydes, Adv. Synth. Catal., 2012, 354, 2916-2920. Bing Zhou†, Yaxi Yang†, Yuanchao Li*, Rhodium-catalyzed oxidative C2-acylation of indoles with aryl and alkyl aldehydes, Chem. Commun., 2012, 48, 5163-5165. Zhaoli Zhou†, Yaxi Yang†, Jian Ding, Yuanchao Li*, Zenghong, Miao, Triptolide: structural modifications, structure-activity relationships, bioactivities, clinical development and mechanisms, Nat. Prod. Rep., 2012, 29, 457-475. Yaxi Yang, Zheng Li, Huijin Feng, Guorong Chen, Yuanchao Li*, Concise synthesis of five-membered ring carbasugars based on key ring-closing metathesis, Tetrahedron Lett., 2010, 51, 3848-3851. Liyan Yue†, Juanjuan Du†, Fei Ye†, Zhifeng Chen, Lianchun Li, Xuan Wang, Fulin Lian, Wen Ai, Bidong Zhang, Naixia Zhang, Yuanyuan Zhang*, Hualiang Jiang, Kaixian Chen, Yuanchao Li, Yaxi Yang* and Cheng Luo*, Identification of novel small-molecule inhibitors targeting menin-MLL interaction, repurposing the antidiarrheals loperamide, Org. Biomol. Chem., 2016, 14, 8503-8519. Bing Zhou*, Zhaoqiang Chen, Yaxi Yang*, Wen Ai, Huanyu, Tang, Yunxiang Wu, Weiliang Zhu*, Yuanchao Li, Redox-Neutral Rhodium-Catalyzed C-H Functionalization of Arylamine N-Oxides with Diazo Compounds: Primary C(sp3)-H/C(sp2)-H Activation and Oxygen-Atom Transfer, Angew. Chem., Int. Ed., 2015, 54, 12121-12126. Xuan Wang, Huanyu, Tang, Huijin Feng, Yuanchao Li*, Yaxi Yang*, Bing Zhou*, Access to Six- and Seven-Membered 1,7-Fused Indolines via Rh(III)-Catalyzed Redox-Neutral C7-Selective C-H Functionalization of Indolines with Alkynes and Alkenes, J. Org. Chem., 2015, 80, 6238-6249. Wen Ai, Yunxiang Wu, Huanyu, Tang, Xueyan Yang*, Yaxi Yang*, Yuanchao Li, Bing Zhou*, Rh(III)- or Ir(III)-catalyzed ynone synthesis from aldehydes via chelation-assisted C-H bond activation, Chem. Commun., 2015, 51, 7871-7874. Wen Ai, Xueyan Yang, Yunxiang Wu, Xuan Wang, Yuanchao Li, Yaxi Yang*, Bing Zhou*, Rhodium(III)- and Iridium(III)-Catalyzed C7 Alkylation of Indolines with Diazo Compounds, Chem. European J., 2014, 20, 17653-17657. Bing Zhou*, Juanjuan Du, Yaxi Yang*, Huijin Feng and Yuanchao Li, Rh(III)-Catalyzed C–H Amidation with N-Hydroxycarbamates: A New Entry to N-Carbamate-Protected Arylamines, Org. Lett., 2014, 16, 592-595.