陈卓，副研究员，硕士生导师

地址：梅陇路130号实验18楼516室

邮箱：chenzhuonina@163.com/chenzhuo@ecust.edu.cn

研究方向：抗肿瘤新药研发

个人简历：

陈卓，博士，华东理工大学药学院副研究员，主要从事抗肿瘤新药活性评价及机制研究。本项目中主要负责候选药物的体内外药效评价。申请人近年来致力于抗肿瘤候选新药的研究和开发，熟悉国内外相关研究领域发展现状与动态，积累了丰富的研究经验。已在Journal of Medicinal Chemistry, European Journal of Medicinal Chemistry, Chemmedchem, Chemical Communication等国际SCI期刊发表论文26篇，SCI他引200余次，单篇最高他引50余次（Journal of Medicinal Chemistry, 2010）。迄今为止，申请中国发明专利8项，国际PCT专利2项。作为项目负责人承担国家自然科学基金、上海市自然科学基金等项目。

学习及研究经历：

2010年6月，毕业于华东理工大学药物化学专业，获医学博士学位；

2010年7月-2012年10月，中国科学院上海药物研究所肿瘤药理研究室博士后，研究内容：1）靶向FGFR的小分子抑制剂抗肿瘤活性评价及机制研究，2）不可逆EGFR酪氨酸激酶抑制剂艾力替尼临床前药效评价；

2015年9月-2016年9月，国家留学基金委公派密歇根大学访问学者，研究内容：1）靶向LSD1新型小分子抑制剂抗急性粒细胞白血病 (AML)及小细胞肺癌（SCLC）活性评价及作用机制研究，2）BET 蛋白降解诱导新药作用机制研究及药效评价。

2012年11月至今，华东理工大学药学院副研究员，研究内容：1）靶向FLT3-ITD突变候选新药抗AML药效评价及作用机制研究，2）靶向EGFR-T790突变第三代候选新药抗非小细胞肺癌（NSCLC）药效评价及作用机制研究；

论文及专利情况

论文

[1]Zhuo Chen, Weisi Wang, Junmin Yao, Shizhu Li*, Xia Zhang, Hehua Hu, Xiong Liu, Binrong Luo, Yuhua Liu, Huiyong Xu, Liping Duan*. Toxicity of a molluscicide candidate PPU07 against Oncomelania hupensis (Gredler, 1881) and local fish in field evaluation. Chemosphere 2019,222, 56-61.

[2] Shuwen Wang, Kaizhi Gu, Zhiqian Guo,* Chenxu Yan, Tingyuan Yang, Zhuo Chen, He Tian, and Wei-Hong Zhu*. Self-Assembly of a Monochromophore-Based Polymer Enables Unprecedented Ratiometric Tracing of Hypoxia. Advanced Materials 2019,31 (3), 1805735.

[3]Zhuo Chen#*, Tingyuan Yang#, Weisi Wang, Junmin Yao, Shaomin Han, Yi Tao, Rui Wang* and Liping Duan*. Synthesis and biological evaluation of carbazole aminoalcohols as antitumor agents.ChemistrySelect, 2018, 3 (44), 12630-12638.

[4]Zhuo Chen, Lin-jiang Tong, Bai-you Tang, Hong-yan Liu, Xin Wang, Tao Zhang, Xian-wen Cao, Yi Chen, Hong-lin Li, Xu-hong Qian, Yu-fang Xu*, Hua Xie* and Jian Ding*. C11, a novel fibroblast growth factor receptor 1 (FGFR1) inhibitor, suppresses breast cancer metastasis and angiogenesis, Acta Pharmacologica Sinica, 2018, https://doi.org/10.1038/s41401-018-0191-7.

[5]Zhuo Chen, Yufang Xu, Xuhong Qian*,Naphthalimides and analogues as antitumor agents: A review on molecular design, bioactivity and mechanism of action, Chinese Chemical Letters, 2018, https://doi.org/10.1016/j.cclet.2018.09.020

[6] Chong Qin,Yang Hu,Bing Zhou,Ester Fernandez-Salas,Chao-Yie Yang, Liu Liu,Donna McEachern,Sally Przybranowski,Mi Wang,Jeanne Stuckey, Jennifer Meagher,Longchuan Bai,Zhuo Chen,Mei Lin,Jiuling Yang, Fuming Xu,Jiantao Hu,Weiguo Xiang,Liyue Huang,Siwei Li,Bo Wen,Duxin Sun, and Shaomeng Wang*. Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression, Journal of Medicinal Chemistry, 2018, 61, 6685-6704.

[7]Bing Zhou#,Jiantao Hu#,Fuming Xu#,Zhuo Chen#,Longchuan Bai#,Ester Fernandez-Salas#,Mei Lin#,Liu Liu,Chao-Yie Yang,Yujun Zhao, Donna McEachern,Sally Przybranowski,Bo Wen,Duxin Sun,and Shaomeng Wang*. Discovery of a Small-Molecule Degrader of Bromodomain and ExtraTerminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression. Journal of Medicinal Chemistry, 2018, 61, 462–481

[8] Zhuo Chen, and Honglin Li*. Novel Drugs Targeting the Epigenome. Current Pharmacology Reports, 2017, 3, 268-285.

[9] Yongjia Hao, Jiankun Lyu, Rong Qu, Deheng Sun, Zhenjiang Zhao, Zhuo Chen, Jian Ding, Hua Xie, Yufang Xu & Honglin Li. Structure-Guided Design of C4-alkyl-1,4-dihydro-2H-pyrimido[4,5-d][1,3]oxazin-2-ones as Potent and Mutant-Selective Epidermal Growth Factor Receptor (EGFR) L858R/T790M Inhibitors, Scientific Reports, 2017, DOI:10.1038/s41598-017-04184-9

[10] Weisi Wang, Qiang Li, Yufen Wei, Jian Xue, Xiao Sun, Yang Yu,Zhuo Chen,Shizhu Li, and Liping Duan*. Novel carbazole aminoalcohols as inhibitors of b-hematin formation: Antiplasmodial and antischistosomal activities. International Journal for Parasitology: Drugs and Drug Resistance, 2017, 7, 191-199.

[11] Weisi Wang, Xiao Sun, Deheng Sun, Shizhu Li, Yang Yu, Tingyuan Yang, Junmin Yao,Zhuo Chen,* and Liping Duan*. Carbazole aminoalcohols induce antiproliferation and apoptosis of human tumor cells by inhibiting topoisomerase I. ChemMedChem, 2016, 11, 2675 – 2681.

[12] Yongjia Hao, Xia Wang, Tao Zhang, Deheng Sun, Yi Tong, Yuqiong Xu, Haiyang Chen, Linjiang Tong, Lili Zhu, Zhenjiang Zhao, Zhuo Chen, Jian Ding, Hua Xie,*, Yufang Xu, * and Honglin Li*. Discovery and Structural Optimization of N5-Substituted 6,7-dioxo-6,7- dihydropteridines as Potent and Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors Against L858R/T790M Resistance Mutation. Journal of Medicinal Chemistry, 2016, 59, 7111-7124

[13] Deheng Sun, Yu Yang, Jiankun Lyu, Wei Zhou, Wenlin Song, Zhenjiang Zhao, Zhuo Chen,* Yufang Xu,* and Honglin Li*. Discovery and Rational Design of Pteridin-7(8H)-one-Based Inhibitors Targeting FMS-like Tyrosine Kinase 3 (FLT3) and Its Mutants. Journal of Medicinal Chemistry, 2016, 59, 6187–6200

[14] Wenlin Song, Shiliang Li, Yi Tong, Jiawei Wang, Lina Quan, Zhuo Chen, Zhenjiang Zhao, Yufang Xu, Lili Zhu*, Xuhong Qian*, Honglin Li*. Structure-based Design of Potent Human Dihydroorotate Dehydrogenase Inhibitors as Anticancer Agents. MedChemComm, 2016, 7, 1441-1448

[15] Qian Sun, Deheng Sun, Lun Song, Zhuo Chen, Zhaoyang Chen, Weibing Zhang*, and Junhong Qian*. Highly Selective Fluorescent Turn-On Probe for Protein Thiols in Biotin Receptor-Positive Cancer Cells. Analytical Chemistry, 2016, 88, 3400–3405

[16] Shaoying Tan, Deheng Sun, Jiankun Lyu, Xiao Sun, Fangshu Wu, Qiang Li, Yiqi Yang, Jianxu Liu, Xin Wang, Zhuo Chen*, Honglin Li*, Xuhong Qian, Yufang Xu*. Antiproliferative and apoptosis-inducing activities of novel naphthalimide–cyclam conjugates through dual topoisomerase (topo) I/II inhibition. Bioorganic & Medicinal Chemistry, 2015, 23, 5672–5680

[17] Qian Sun, Haiyu Tian, Haoran Qu, Deheng Sun,Zhuo Chen, Liping Duan, Weibing Zhang* and Junhong Qian*. Discrimination between streptavidin and avidin with fluorescent affinity-based probes. Analyst, 2015, 140, 4648-4653

[18] Yi Xiao,* Fengyu Liu, Zhuo Chen, Weipin Zhu, Yufang Xu and Xuhong Qian*. Discovery of a novel family of polycyclic aromatic molecules with unique reactivity and members valuable for fluorescent sensing and medicinal chemistry. Chemical Communication, 2015, 51, 6480-6488.

[19] Shaoying Tan, Kun Han, Qiang Li, Linjiang Tong, Yiqi Yang, Zhuo Chen*, Xie Hua*, Jian Ding, Xuhong Qian and Yufang Xu*. Novel metal complexes of naphthalimide-cyclam conjugates as potential multi-target receptor tyrosine kinase (RTK) inhibitors: Synthesis and biological evaluation. European Journal of Medicinal Chemistry, 2014, 85, 207-214.

[20] Shaoying Tan, Hong Yin, Zhuo Chen*, Xuhong Qian, Yufang Xu*. Oxo-heterocyclic fused naphthalimides as antitumor agents: Synthesis and biological evaluation. European Journal of Medicinal Chemistry, 2013, 62, 130-138.

[21] Zhuo Chen, Le Han, Minghao Xu, Yufang Xu*, Xuhong Qian*. Rationally designed multitarget anticancer agents. Current Medicinal Chemistry, 2013, 20, 1694-1714.

[22] Xin Wang, Zhuo Chen*, Linjiang Tong, Shaoying Tan, Wei Zhou, Ting Peng, Kun Han, Jian Ding, Hua Xie*, and Yufang Xu*. Naphthalimides Exhibit in vitro Antiproliferative and Antiangiogenic Activities by Inhibiting both Topoisomerase II (Topo II) and Receptor Tyrosine Kinases (RTKs). European Journal of Medicinal Chemistry, 2013, 65, 477-486

[23] Zhuo Chen, Xin Wang, Weiping Zhu, Xianwen Cao, Linjiang Tong, Honglin Li, Hua Xie*, Yufang Xu*, Shaoying Tan, Dong Kuang, Jian Ding, Xuhong Qian*, Acenaphtho [1,2-b]pyrrole Derivatives as Potent and Selective FGFR1 Inhibitors: Design, Synthesis and Biological Evaluation. Journal of Medicinal Chemistry, 2011, 54, 3732-3745. The amendment was published online 2014. (Journal of Medicinal Chemistry, 2014, 57, 1621−1624.)

[24] Bing Lin, Zhuo Chen, Yufang Xu, Huanying Zhang, Jianwen Liu*, Xuhong Qian, 7-b, a Novel Amonafide Analogue, Cause Growth Inhibition and Apoptosis in Raji Cells via a ROS-Mediated Mitochondrial Pathway. Leukemia Research, 2011, 35, 646-656.

[25] Hua Xie, Liping Lin, Linjiang Tong, Yong Jiang, Mingyue Zheng, Zhuo Chen, Xiaoyan Jiang, Xiaowei Zhang, Xiaowei Ren, Wenchao Qu, Yang Yang, Hua Wan, Yi Chen, Jianping Zuo, Hualiang Jiang, Meiyu Geng, Jian Ding*, AST1306, a Novel Irreversible Inhibitor of the Epidermal Growth Factor Receptor 1 and 2, Exhibits Antitumor Activity Both In Vitro and In Vivo. PLoS ONE, 2011, 6(7): e21487

[26] Zhuo Chen, Xin Liang, Huanying Zhang, Hua Xie, Jianwen Liu, Yufang Xu*, Weiping Zhu, Yi Wang, Xin Wang, Shaoying Tan, Dong Kuang, Xuhong Qian*. A New Class of Naphthalimide-based Antitumor Agents that Inhibit Topoisomerase II (Topo II) and Induce Lysosomal Membrane Permeabilization (LMP) and Apoptosis. Journal of Medicinal Chemistry, 2010, 53, 2589-2600.

专利

[1] LI HONGLIN[CN]; XU YUFANG[CN]; ZHAO ZHENJIANG[CN]; ZHOU WEI[CN]; XU YUQIONG[CN]; SUN DEHENG[CN]; WANG XIA[CN]; CHEN ZHUO[CN]；国际专利；Use of pteridinone derivative serving as EGFR inhibitor；公开号: 澳大利亚公开AU2016272057(A1)；公开日: 2018-01-25；

[2] LI HONGLIN[CN]; XU YUFANG[CN]; ZHAO ZHENJIANG[CN]; ZHOU WEI[CN]; XU YUQIONG[CN]; SUN DEHENG[CN]; WANG XIA[CN]; CHEN ZHUO[CN]；国际专利；Use of pteridinone derivative serving as EGFR inhibitor；公开号: 欧洲公开EP3312180(A1)；公开日: 2018-04-25。

[3] LI HONGLIN[CN]; XU YUFANG[CN]; ZHAO ZHENJIANG[CN]; ZHOU WEI[CN]; XU YUQIONG[CN]; SUN DEHENG[CN]; WANG XIA[CN]; CHEN ZHUO[CN]；国际专利；Use of pteridinone derivative serving as EGFR inhibitor；公开号: 美国公开US2018148454(A1)；公开日: 2018-05-31。

[4] LI HONGLIN[CN]; XU YUFANG[CN]; ZHAO ZHENJIANG[CN]; ZHOU WEI[CN]; XU YUQIONG[CN]; SUN DEHENG[CN]; WANG XIA[CN]; CHEN ZHUO[CN]；国际专利；Use of pteridinone derivative serving as EGFR inhibitor；公开号: 日本公开 JP2018516278(A)；公开日: 2018-06-21；

[5] LI HONGLIN[CN]; XU YUFANG[CN]; ZHAO ZHENJIANG[CN]; ZHOU WEI[CN]; XU YUQIONG[CN]; SUN DEHENG[CN]; WANG XIA[CN]; CHEN ZHUO[CN]；国际专利；Use of pteridinone derivative serving as EGFR inhibitor；公开号: 韩国公开KR20180021743(A)；公开日: 2018-03-05。

[6] 李洪林，陈卓，赵振江，齐甜甜，杨婷媛，宋文琳，韩乐，孙德恒；中国专利；噻唑衍生物在治疗非淋巴细胞性白血病中的应用；公开号: CN108721283A；公开日: 2018.11.02。

[7] 李洪林，陈卓，赵振江；中国专利；来氟米特和特立氟胺在白血病治疗；公开号: CN108721280A；公开日: 2018.11.02。

[8] 李洪林，徐玉芳，赵振江，周伟，徐玉琼，孙德恒，王霞，陈卓；中国专利；蝶啶酮衍生物作为EGFR抑制剂的应用；公开号: CN107922417A；公开日: 2018.04.17。

[9] 李洪林，徐玉芳，陈卓，孙德恒，吕剑昆，赵振江，宋文琳，周伟，杨宇；中国专利；作为FLT3抑制剂的蝶啶酮衍生物及应用；公开号: CN107151249A；公开日: 2017.09.12。

[10] 李洪林，徐玉芳，谢华，郝永佳，陈卓，孙德恒，吕剑昆，徐玉琼，童依，陈海洋，赵振江，丁健；中国专利；作为EGFR抑制剂的嘧啶并[4,5-d][1,3]噁嗪-2-酮衍生物及其应用；公开号 : CN107129506A；公开日 : 2017.09.05。

[11] 李洪林，徐玉芳，陈卓，赵振江，吕剑昆，孙德恒，杨宇，周伟；中国专利；蝶啶酮衍生物作为FLT3抑制剂的应用；公开（公告）号 : CN106467540A；公开（公告）日 : 2017.03.01。

[12] 徐玉芳，李洪林，赵振江，朱丽丽，许明豪，吴方舒，朱俊生，王佳炜，李诗良，陈卓；中国专利；检测二氢乳清酸脱氢酶的化合物；公开号 : CN106279141A；公开日 : 2017.01.04；PCT申请号：PCT/CN2016/085367。

[13] 李洪林，徐玉芳，赵振江，周伟，徐玉琼，孙德恒，王霞，陈卓；中国专利；蝶啶酮衍生物作为EGFR抑制剂的应用；公开（公告）号 : CN106279173A；公开（公告）日 : 2017.01.04；PCT申请号：PCT/CN2016/083945

[14] 钱旭红，徐玉芳，陈卓，朱维平，王新，谭绍英，旷东，谢华；中国专利，8-氧-8H-苊并[1,2-b]吡咯衍生物，申请号：200910056554.2，公开号：CN101633637。

[15] 徐玉芳，陈卓，钱旭红，朱维平，王新，谭绍英，旷东，刘建文，梁欣；中国专利,  萘酰亚胺衍生物，申请号：200910056555.7，公开号：CN101633640。

[16] 钱旭红，朱维平，徐玉芳，张佩琢，徐晓勇，肖义，陈卓，段春晓；中国专利，一种荧光标记试剂，申请号：200510030078.9，公开号：CN1940563。

[17] 钱旭红，刘燕，徐玉芳，李君辉，孔祥明，陈卓，肖义，张元兴；中国专利，萘类衍生物及其在乏氧体系中的应用，申请号：CN200410017346.9，公开号：CN1563005。