陳卓，副研究員，碩士生導(dǎo)師

地址：梅隴路130號實驗18樓516室

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

研究方向：抗腫瘤新藥研發(fā)

個人簡歷：

陳卓，博士，華東理工大學(xué)藥學(xué)院副研究員，主要從事抗腫瘤新藥活性評價及機制研究。本項目中主要負(fù)責(zé)候選藥物的體內(nèi)外藥效評價。申請人近年來致力于抗腫瘤候選新藥的研究和開發(fā)，熟悉國內(nèi)外相關(guān)研究領(lǐng)域發(fā)展現(xiàn)狀與動態(tài)，積累了豐富的研究經(jīng)驗。已在Journal of Medicinal Chemistry, European Journal of Medicinal Chemistry, Chemmedchem, Chemical Communication等國際SCI期刊發(fā)表論文26篇，SCI他引200余次，單篇最高他引50余次（Journal of Medicinal Chemistry, 2010）。迄今為止，申請中國發(fā)明專利8項，國際PCT專利2項。作為項目負(fù)責(zé)人承擔(dān)國家自然科學(xué)基金、上海市自然科學(xué)基金等項目。

學(xué)習(xí)及研究經(jīng)歷：

2010年6月，畢業(yè)于華東理工大學(xué)藥物化學(xué)專業(yè)，獲醫(yī)學(xué)博士學(xué)位；

2010年7月-2012年10月，中國科學(xué)院上海藥物研究所腫瘤藥理研究室博士后，研究內(nèi)容：1）靶向FGFR的小分子抑制劑抗腫瘤活性評價及機制研究，2）不可逆EGFR酪氨酸激酶抑制劑艾力替尼臨床前藥效評價；

2015年9月-2016年9月，國家留學(xué)基金委公派密歇根大學(xué)訪問學(xué)者，研究內(nèi)容：1）靶向LSD1新型小分子抑制劑抗急性粒細(xì)胞白血病 (AML)及小細(xì)胞肺癌（SCLC）活性評價及作用機制研究，2）BET 蛋白降解誘導(dǎo)新藥作用機制研究及藥效評價。

2012年11月至今，華東理工大學(xué)藥學(xué)院副研究員，研究內(nèi)容：1）靶向FLT3-ITD突變候選新藥抗AML藥效評價及作用機制研究，2）靶向EGFR-T790突變第三代候選新藥抗非小細(xì)胞肺癌（NSCLC）藥效評價及作用機制研究；

論文及專利情況

論文

[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.

專利

[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]；國際專利；Use of pteridinone derivative serving as EGFR inhibitor；公開號: 澳大利亞公開AU2016272057(A1)；公開日: 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]；國際專利；Use of pteridinone derivative serving as EGFR inhibitor；公開號: 歐洲公開EP3312180(A1)；公開日: 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]；國際專利；Use of pteridinone derivative serving as EGFR inhibitor；公開號: 美國公開US2018148454(A1)；公開日: 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]；國際專利；Use of pteridinone derivative serving as EGFR inhibitor；公開號: 日本公開 JP2018516278(A)；公開日: 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]；國際專利；Use of pteridinone derivative serving as EGFR inhibitor；公開號: 韓國公開KR20180021743(A)；公開日: 2018-03-05。

[6] 李洪林，陳卓，趙振江，齊甜甜，楊婷媛，宋文琳，韓樂，孫德恒；中國專利；噻唑衍生物在治療非淋巴細(xì)胞性白血病中的應(yīng)用；公開號: CN108721283A；公開日: 2018.11.02。

[7] 李洪林，陳卓，趙振江；中國專利；來氟米特和特立氟胺在白血病治療；公開號: CN108721280A；公開日: 2018.11.02。

[8] 李洪林，徐玉芳，趙振江，周偉，徐玉瓊，孫德恒，王霞，陳卓；中國專利；蝶啶酮衍生物作為EGFR抑制劑的應(yīng)用；公開號: CN107922417A；公開日: 2018.04.17。

[9] 李洪林，徐玉芳，陳卓，孫德恒，呂劍昆，趙振江，宋文琳，周偉，楊宇；中國專利；作為FLT3抑制劑的蝶啶酮衍生物及應(yīng)用；公開號: CN107151249A；公開日: 2017.09.12。

[10] 李洪林，徐玉芳，謝華，郝永佳，陳卓，孫德恒，呂劍昆，徐玉瓊，童依，陳海洋，趙振江，丁健；中國專利；作為EGFR抑制劑的嘧啶并[4,5-d][1,3]噁嗪-2-酮衍生物及其應(yīng)用；公開號 : CN107129506A；公開日 : 2017.09.05。

[11] 李洪林，徐玉芳，陳卓，趙振江，呂劍昆，孫德恒，楊宇，周偉；中國專利；蝶啶酮衍生物作為FLT3抑制劑的應(yīng)用；公開（公告）號 : CN106467540A；公開（公告）日 : 2017.03.01。

[12] 徐玉芳，李洪林，趙振江，朱麗麗，許明豪，吳方舒，朱俊生，王佳煒，李詩良，陳卓；中國專利；檢測二氫乳清酸脫氫酶的化合物；公開號 : CN106279141A；公開日 : 2017.01.04；PCT申請?zhí)枺?/span>PCT/CN2016/085367。

[13] 李洪林，徐玉芳，趙振江，周偉，徐玉瓊，孫德恒，王霞，陳卓；中國專利；蝶啶酮衍生物作為EGFR抑制劑的應(yīng)用；公開（公告）號 : CN106279173A；公開（公告）日 : 2017.01.04；PCT申請?zhí)枺?/span>PCT/CN2016/083945

[14] 錢旭紅，徐玉芳，陳卓，朱維平，王新，譚紹英，曠東，謝華；中國專利，8-氧-8H-苊并[1,2-b]吡咯衍生物，申請?zhí)枺?/span>200910056554.2，公開號：CN101633637。

[15] 徐玉芳，陳卓，錢旭紅，朱維平，王新，譚紹英，曠東，劉建文，梁欣；中國專利,  萘酰亞胺衍生物，申請?zhí)枺?/span>200910056555.7，公開號：CN101633640。

[16] 錢旭紅，朱維平，徐玉芳，張佩琢，徐曉勇，肖義，陳卓，段春曉；中國專利，一種熒光標(biāo)記試劑，申請?zhí)枺?/span>200510030078.9，公開號：CN1940563。

[17] 錢旭紅，劉燕，徐玉芳，李君輝，孔祥明，陳卓，肖義，張元興；中國專利，萘類衍生物及其在乏氧體系中的應(yīng)用，申請?zhí)枺?/span>CN200410017346.9，公開號：CN1563005。