个人简历

学科方向\t 药物化学，有机全合成
大约90%的 癌症死因，源于癌症的复发和转移。越来越多的科学研究发现：癌症干细胞是大多数癌症产生、发展、复发、耐药和转移的根源。目前临床使用的药物治疗与放疗手 段，均只针对普通癌细胞，而不能选择性杀灭癌症干细胞。癌症干细胞在各种手段治疗以后，往往能够存活下来，引起癌症的复发和转移。靶向癌症干细胞的药物研 究，有望显著降低癌症复发和转移的几率，为某些癌症在一定程度上的根治，提供新的希望。但是，目前还很难发现靶向癌症干细胞的化合物；而已经确认靶向癌症 干细胞的化合物，无论在种类和数量上，均非常有限。在抗癌症干细胞天然产物的骨架基础上，本课题组通过合理的设计、全合成与半合成的手段，以及多种生物活性测试，发现了多个系列的靶向癌症干细胞的化合物。目前，第一代候选药物DMAMCL（即ACT001） 在多个癌症动物试验中，取得了部分实验动物长期生存的优异疗效。合作公司已完成该候选药物的药学、药理、药代、与安全性评价，申报了临床试验并已经通过现场考察，报国家局进行技术评审，同时获准进入澳大利亚临床试验。在药物化学研究的基础上，课题组还设计与合成了分子探针，用于探索药物作用于癌症干细胞的相关靶点。

研究领域

""靶向癌症干细胞的药物化学""""

近期论文

Jing Li, Shanshan Li, Jianshuang Guo, Qiuying Li, Jing Long, Cheng Ma, Yahui Ding, Chunli Yan, Liangwei Li, Zhigang Wu, He Zhu, Keqin Li, Liuqing Wen, Quan Zhang, Qingqing Xue, Caili Zhao, Ning Liu, Ivaylo Ivanov, Ming Luo, Rimo Xi, Haibo Long, Peng Wang, * Yue Chen,* Natural Product Micheliolide (MCL) Irreversibly Activates Pyruvate Kinase M2 and Suppresses Leukemia. J. Med. Chem., (DOI:10.1021/acs.jmedchem.8b00241, selected to be featured in ACS Editors' Choice)\r
\r
Jian Chen, Jingpei Li, Lingling Wu, Yan Geng, Jianming Yu, Chuanke Chong, Mengmeng Wang, Yuan Gao, Cuigai Bai, Yahui Ding,* Quan Zhang,* Yue Chen,* Synthesis and Anti-pancreatic Cancer Activities of Rakicidin A analogues. Eur. J. Med. Chem., DOI:10.1016/j. ejmech. 2018.03.078\r
\r
Yunfeng Tian1, Xiaolong Xu1, Yahui Ding, Xin Hao, Yanju Bai, Yang Tang, Xuemei Zhang, Qiuying Li, Zhantao Yang, Weicheng Zhang,* Yue Chen,* Synthesis and Biological Evaluation of Nannocystin Analogues toward Understanding the Binding Role of the (2R,3S)-Epoxide in Nannocystin A. Eur. J. Med. Chem., 2018, 150, 626-632.\r
\r
Huiying Li, Dingdi He, Xiujuan Zhao, Tongyan Sun, Quan Zhang, Cuigai Bai,* Yue Chen,* Design and synthesis of novel dasatinib derivatives as inhibitors of leukemia stem cells. Bioorg. Med. Chem. Lett., 2018, 28, 700-706.\r
\r
Yin Jiang, Huiying Li, Xiaohui Li, Jun Lu, Quan Zhang, Cuigai Bai,* Yue Chen,* Therapeutic Effects of Isothiocyanate Prodrugs on Rheumatoid Arthritis. Bioorg. Med. Chem. Lett., 2018, 28, 737-741.\r
\r
Yuanjun Sun1, Yahui Ding1,Dongmei Li, Ruifei Zhou, Xiuwen Su, Juan Yang, Xiaoqian Guo, Chuanke Chong, Jinghan Wang, Weicheng Zhang, Cuigai Bai, Liang Wang*, Yue Chen,* Cyclic Depsipeptide BE-43547A2: Synthesis and Activity against Pancreatic Cancer Stem Cells. Angew. Chem. Int. Ed., 2017, 56, 14627-14631.(hot paper, press release)\r
\r
Zhongjin Yang1, Beijia Kuang1, Ning Kang, Yahui Ding, Weizhi Ge, Lihui Lian, Yuan Gao, Yuqing Wei, Yue Chen*, Quan Zhang,* Synthesis and anti-acute myeloid leukemia activity of C-14 modified parthenolide derivatives. Eur. J. Med. Chem., 2017, 127, 296-304.\r
\r
Jinghan Wang, Beijia Kuang, Xiaoqian Guo, Jianwei Liu, Yahui Ding, Jiangnan Li, Shende Jiang, Ying Liu, Fang Bai, Luyuan Li, Quan Zhang, Xiao-Yu Zhu, Bo Xia, Chun-Qi Li, Liang Wang*, Guang Yang*, Yue Chen,* Total Syntheses and Biological Activities of Vinylamycin Analogs. J. Med. Chem., 2017, 60, 1189-1209.\r
\r
Zhantao Yang, Xiaolong Xu, Chun-Hua Yang, Yunfeng Tian, Xinyi Chen, Lihui Lian,Wenwei Pan, Xuncheng Su,Weicheng Zhang* and Yue Chen,* Total Synthesis of Nannocystin A. Org. Lett., 2016, 18, 5768–5770.\r
\r
Zhantao Yang, Meiyan Ma, ChunHua Yang, Yuan Gao, Quan Zhang and Yue Chen,* Determination of the Absolute Configurations of Microtermolide A and B. J. Nat. Prod., 2016, 79, 2408-2412.\r
\r
Ding Y, Gao H, Zhang Y, Li Y, Vasdev N, Gao Y, Chen Y, Zhang Q,* Alantolactone Selectively Ablates Acute Myeloid Leukemia Stem and Progenitor Cells. Journal of hematology &oncology, 2016, 9, 93.\r
\r
Ye-Hui Shi, Dong-Fang Dai, Jing Li, Yan-Wei Dong, Yin Jiang, Huan-Gong Li,Yuan Gao, Chuan-Ke Chong, Hui-Ying Li, Xiao-Qian Chu, Cheng Yang, Quan Zhang, Zhong-Sheng Tong, Cui-Gai Bai,* and Yue Chen,* Sulforaphane Analogues with Heterocyclic Moieties: Syntheses and Inhibitory Activities against Cancer Cell Lines. Molecules, 2016, 21, 514.\r
\r
Feng Sang,# Yahui Ding,# Jinghan Wang,# Bingxia Sun,# Jianlei Sun,# Yan Geng,# Zhang Zhang, Ke Ding, Ling-Ling Wu, Jian-Wei Liu, Cuigai Bai, Guang Yang,* Quan Zhang,* Lu-Yuan Li,* Yue Chen,* Structure?Activity Relationship Study of Rakicidins: Overcoming Chronic Myeloid Leukemia Resistance to Imatinib with 4?Methylester-Rakicidin A. J. Med. Chem., 2016, 59, 1184-1196.\r
\r
Yong-Tao Li,#Jing-HanWang,#Cheng-Wen Pan, Fan-FeiMeng, Xiao-Qian Chu, Ya-hui Ding, Wen-Zheng Qu, Hui-ying Li, Cheng Yang, Quan Zhang, Cui-Gai Bai,* Yue Chen,* Syntheses and biological evaluation of 1,2,3-triazole and 1,3,4-oxadiazole derivatives of imatinib. Bioorg. Med. Chem. Lett., 2016, 26, 1419-1427.\r
\r
Jing Long, Ya-Hui Ding, Pan-Pan Wang, Quan Zhang, Yue Chen,* Total syntheses and structure–activity relationship study of parthenolide analogues. Tetrahedron Lett., 2016, 57, 874–877.\r
\r
Ya-Hui Ding, Xue Gao, Jing Long, Bei-Jia Kuang, Yue Chen*, Quan Zhang,* Dispirocyclopropyl dehydrocostus lactone selectively inhibits acute myelogenous leukemia cells. Bioorg. Med. Chem. Lett., 2016, 26, 1165-1168.\r
\r
Zhantao Yang, Guang Yang,* Meiyan Ma, Jiangnan Li, Jianwei Liu, Jinghan Wang, Shende Jiang, Quan Zhang, Yue Chen,* Total Synthesis and Determination of the Absolute Configuration of Vinylamycin. Org. Lett., 2015, 17, 5725-5727.\r
\r
Zhong-Jin Yang, Wei-Zhi Ge, Qiu-Ying Li, Yaxin Lu, Jian-Miao Gon, Bei-Jia Kuang, Xiaonan Xi, Haiting Wu, Quan Zhang,* Yue Chen,* Syntheses and Biological Evaluation of Costunolide, Parthenolide and Their Fluorinated Analogues. J. Med. Chem.2015, 58, 7007-7020.\r
\r
Yan Zhao, Sijia Chen, Jiancheng Wang, Hongxin Ni, Qianqian Jia, Xiaowen Chen, Xiaoyan Du, Lu Lu, Bo Huan, Quan Zhang, Yue Chen, Hai-bo Long,* Sesquiterpene Lactones Inhibit Advanced Oxidation Protein Product-Induced MCP-1 Expression in Podocytes via an IKK/NF- к B-Dependent Mechanism. Oxidative Medicine and Cellular Longevity, 2015, 1-13.\r
\r
Feng Sang, Dongmei Li, Xiaolong Sun, Xianqiang Cao, Liang Wang, Jianlei Sun, Bingxia Sun, Lingling Wu, Guang Yang, Xiaoqian Chu, Jinghan Wang, Changming Dong, Yan Geng, Hong Jiang, Haibo Long, Sijia Chen, Guiyan Wang, Shuzhong Zhang, Quan Zhang, Yue Chen,* Total Synthesis and Determination of the Absolute Configuration of Rakicidin A. J. Am. Chem. Soc., 2014, 136, 15787-15791.