【个人资料】 | |
| ·姓名：苟少华 ·性别：男 ·民族：汉 ·职称：教授 ·学历：博士 ·联系电话：025 52091139 ·电子信箱：sgou@seu.edu.cn ·课题组网址： |
【研究方向】 | |
靶向抗肿瘤药物和心脑血管药物设计与筛选 金属抗肿瘤药物研究 药物及其中间体工艺的研发 | |
【学习与工作经历】 | |
1980-1990 南京大学化学系，先后获得理学学士、硕士、博士学位 1992-1993 英国谢菲尔德大学开展博士后研究 1995-1996 奥地利维也纳工业大学进行客座研究 1990-2007 南京大学，曾担任化学化工学院副院长和配位化学国家重点实验室副主任，1998年晋升为教授。 2008-迄今 东南大学化学化工学院工作，现担任东南大学药物研究中心主任， 江苏省生物药物高技术研究重点实验室主任。 现为国家新药审评中心咨询专家、江苏省化学化工学会理事、江苏省高新企业评审专家。长期从事药物化学和配位化学方面的基础研究以及药物开发等方面的研发工作。 | |
【科研项目】 | |
先后主持和参加完成了包括“十一五”、“十二五”国家“重大新药创制”专项课题和平台建设项目，国家自然科学基金委青年基金、面上项目和重点项目，教育部和江苏省人才项目，江苏省自然科学基金和科技支撑项目以及江苏省重大基础设施建设项目等30余项，并主持完成企业委托项目30余项。 | |
【论文及获奖】 | |
在Nature Commun., JACS, Adv. Func. Materials, Coord. Chem. Rev.，Chem. Sci., Small, Acta Pharmcologic Sinica B, J. Med. Chem., Cancer Lett., J. Materials Chem. B, Eur. J. Med. Chem., Chem. Commun., Inorg. Chem., Chem-Eur. J., Bioconjugate Chem., Acta Pharmcologic Sinica, Biochem. Pharmacology等国内外刊物上发表论文300余篇。获授权发明专利30多项，其中许可实施多项，作为第一发明人获得美国、欧洲和日本专利各2项。 近20多年来，与国内企业合作，研发药物与制备医药中间体及精细化工产品，有十几个产品已实现产业化，相关产品已产生了几十亿元销售收入。 1995年获中国化学会“青年化学”奖、国家教委“资助优秀年轻教师基金”，1996年获江苏省首届“江苏青年科学家”奖、被评为江苏省优秀青年骨干教师，1997年被江苏省列为333工程培养对象，2000年获国家教育部青年骨干教师研究基金，2002年被教育部评为全国高等学校优秀骨干教师，2007年被评为江苏省“333高层次人才培养工程”首批中青年科学技术带头人、获第一届“中国百篇最具影响优秀国际学术论文”奖，2008年获江苏省“六大人才高峰”高层次人才项目资助，2014年获中华全国工商业联合会科技进步奖一等奖，2016年获中华全国工商业联合会科技进步奖一等奖，2018年获江苏省教育科学研究成果奖二等奖（高校自然科学类），2019年获日内瓦国际发明银奖。 近年来发表的主要论文： 2024年 1.Discovery of a potent and selective cell division cycle 7 inhibitor from 6-(3-fluoropyridin-4-yl)thieno[3,2-d]pyrimidin-4(3H)-one derivatives as an orally active antitumor agent. Mingwei Fu, Min Ge, Wanxiang Yang, Chunchen Fu, Xiaowei Li, Yuanjiang Wang,* Shaohua Gou* Acta Pharmaceutica Sinica B, 2024,14(2),893-896. DOI:10.1016/j.apsb.2023.11.026 2.A electron-accepting half-sandwich iridium(III) complex for the treatment of hypoxic tumors via synergetic chemo- and phototherapy. Yuliang Yang, Y Gao, Jian Zhao*, Shaohua Gou* Inorg. Chem. Frontiers, 2024, 11, 436-450. DOI:10.1039/d3qi02047a 3.Multi-targeting HDAC inhibitors containing a RAS/RAF protein interfering unit. Yuanjiang Wang, Jianluo Zhang, Kun Li, Shengjin Xia, and Shaohua Gou* J. Med. Chem., 2024, 67(3), 2066-2082. DOI:10.1021/acs.jmedchem.3c01941 4.Discovery of N-(4-((6-(3,5-dimethoxyphenyl)-9H-purine derivatives as irreversible covalent FGFR inhibitors. Yuanjiang Wang, Yanchang Pan, Zhaodan Lv, Shaohua Gou* Eur. J. Med. Chem., 2024, 271, 116415. DOI:10.1016/j.ejmech.2024.116415 2023年 1.Circumventing acquired drug resistance through a CK2-targeted combination via attenuating endogenous AhR-TLS-promoted genomic instability in human colorectal cancer cells. Feihong Chen, Zhiwei Wang, Yuanjiang Wang, Shaohua Gou* Food Chem. Toxicol., 2023, 176, 113774. DOI:10.1016/j.fct.2023.113774 2.Hybrids of carbonic anhydrase and cyclooxygenase inhibitors attenuate cardiac hypoxic inflammatory injuries. Wen Zhou, Chunping Wang, Bin Zhang, Shaohua Gou* Eur. J. Pharmaco., 2023, 950, 175751. DOI:10.1016/j.ejphar.2023.175751 3.Realizing NIR-triggered type-I PDT and PTT via maximizing electronic exchange energy of perylene diimide-based photosensitizers. Jian Zhao#, Rong Huang#, Ya Gao, Jiadong Xu, Yanyan Sun, Jiayuan Bao, Lei Fang*, Shaohua Gou* ACS MaterialsLett., 2023, 5,1752–1759. DOI:10.1021/acsmaterialslett.3c00436 4.Design of near-infrared-triggered metallo-photosensitizers via a self-assembly-induced vibronic decoupling strategy Jian Zhao, Ya Gao, Rong Huang, Chen Chi, Yanyan Sun, Gang Xu*, Xing-Hua Xia*, Shaohua Gou* J. Am. Chem. Soc., 2023, 145, 11633-11642. DOI:10.1021/jacs.3c01645 5.Naphthalene diimides functionalized half-Sandwich Ru(II) complexes as mitochondria-targeted anticancer and antimetastatic Agents. Yuliang Yang, Xiaofeng Zou, Yanyan Sun, Feihong Chen, Jian Zhao*, Shaohua Gou* Inorg. Chem., 2023, 62 (24) , 9649-9660. DOI:10.1021/acs.inorgchem.3c01125 6.Study on the anticancer potency of Ru(II)/Ir(III) complexes via DNA damage and poly(ADP-ribose) polymerase 1 inhibition. Yuliang Yang, Ya Gao, Yanyan Sun, Jian Zhao*, Shaohua Gou * J. Med. Chem., 2023, 66(19), 13731-13745. DOI:10.1021/acs.jmedchem.3c01156 7.Blockade of chemo-resistance to 5-FU by a CK2-targeted combination via attenuating endogenous AhR-TLS-promoted genomic instability in human colorectal cancer cells. Zhiwei Wang, Feihong Chen, Yuanjiang Wang, Shaohua Gou* Toxicol. App. Pharmacol., 2023, 475, 116647. DOI:10.1016/j.taap.2023.116647 8.Design, synthesis, and biological evaluation of a series of benzofuran [3,2-D]pyrimidine-4(1H)-ketone derivatives containing thiosemicarbazone analogs as novel PRAP-1 inhibitors. Yuanjiang Wang, Kun Li, Wenqing Xu, Shaohua Gou* Bioorg. Chem., 2023, 139, 106759. DOI:10.1016/j.bioorg.2023.106759 9.Discovery of efficient hypoxia-targeted NO donor compounds to alleviate hypoxia cardiac disease. Wanxiang Yang, Wen Zhou, Shaohua Gou* J. Med. Chem., 2023, 66(23), 15977-15989.DOI:10.1021/acs.jmedchem.3c01421 10.A self-assembly-induced exciton delocalization strategy for converting a perylene diimide derivative from a type-II toType-I photosensitizer. Lei Fang, Rong Huang, Wenqi Gong, Yuanhui Ji, Yanyan Sun, Shaohua Gou*, Jian Zhao* Small, 2023, 2307414.DOI: 10.1002/smll.202307414 2022年 1.A supramolecular photosensitizer derived from an arene-Ru(II) complex self-assembly for NIR activated photodynamic and photothermal therapy Gang Xu, Chengwei Li, Chen Chi, Luyan Wu, Yanyan Sun, Jian Zhao*, Xing-Hua Xia*, Shaohua Gou* Nature Comm., 2022, 13(1), 3064. 2.Boosting phototherapy efficacy of NIR-absorbing ruthenium (II) complex via supramolecular engineering Zhimei Wang, Chengwei Li, Huang, S, Ma, X, Yanyan, Jian Zhao*, Shaohua* Materials Today Nano, 2022, 18, 100220. Chengwei Li, Ya Gao, Rong Huang, Lei Fang*, Yanyan Sun, Yuliang Yang,Shaohua Gou*,Jian Zhao* ACS MaterialsLett., 2022, 4(4) , pp.657-664. 4.A hypoxia-activated NO donor for the treatment of myocardial hypoxia injury Wen Zhou, Wanxiang Yang, Keyu Fan, Wuyang Hua, Shaohua Gou* Chem. Sci., 2022,13, 3549-3555. 5.Platinum(IV) prodrugs with cancer stem cell inhibitory effects on lung cancer for overcoming drug resistance Xinyi Wang, Zhikun Liu, YuanjiangWang*, Shaohua Gou* J. Med. Chem., 2022, 65(11), 7933-7945. 6. Hypoxia-activated prodrugs with dual COX-2/CA inhibitory effects on attenuating cardiac inflammation under hypoxia Wen Zhou, Chunping Wang, Zhikun Liu, Shaohua Gou* J. Med. Chem., 2022, 65(19), 13436-13451. 7.Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway Qingqing Liu,Bin Zhang, Yuanjiang Wang, Xinyi Wang, Shaohua Gou * Eur. J. Med. Chem., 2022, 229, 114058. 8.Design, synthesis and anticancer evaluation of selective 2,4-disubstituted pyrimidine CDK9 inhibitors Zichen Xu, Bin Zhang, Zhikun Liu, Shaohua Gou* Eur. J. Med. Chem., 2022, 244, 114875. 9.Design, synthesis and biological evaluation of antitumor platinum(II) agents conjugated with non-steroidal anti-inflammatory drug species Ju Zang, Bin Zhang, Yuanjiang Wang, Xinyi Wang, Shaohua Gou* Bioorg. Chem., 2022, 120, 105633.
Zichen Xu, Yongzhi Yu, Jian Zhao, Zhixin Liao, Yanyan Sun, Shaohua Gou* Inorg. Chem., 2022, 61, 20346-20357. 2021年 1.Novel CK2 specific Pt(II) compound reverses cisplatin-mediated resistance by inhibiting cancer cell stemness and suppressing DNA damage repair in NSCLC treatments Yuanjiang Wang, Xinyi Wang, Gang Xu, Shaohua Gou* J. Med. Chem., 2021, 64(7), 4163-4178. 2. Discovery of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine derivatives as highly selective CK2 inhibitors with potent cancer cell stemness inhibition Yuanjiang Wang, Zhaodan Lv, Feihong Chen, XingWang, Shaohua Gou* J. Med. Chem., 2021,64(8), 5082-5098. 3. Discoveryof 6-(7-nitro-2,1,3-benzoxadiazol-4-ylthio)hexanol derivatives as glutathione transferase inhibitors with favorable selectivity and tolerated toxicity Qingqing Liu, Zhikun Liu, Wuyang Hua, ShaohuaGou* J. Med. Chem., 2021, 64(3), 1701-1702. 4. Conjugatesderived from lapatinib derivatives with cancer cell stemness inhibitors effectively reversed drug resistance in triple- negative breast cancer. Yuanjiang Wang, Zhaodan Lv, Feihong Chen, Xing Wang,Shaohua Gou* J. Med. Chem., 2021, 64(17), 12877-12892. 5. Blood-brain barrier permeable and NO-releasing multifunctional nanoparticles for Alzheimer’s diseasetreatment: Targeting NO/cGMP/CREB signaling pathways. Zhikun Liua, Qingqing Liu,Bin Zhang, Qiao Liu, Lei Fang*, Shaohua Gou* J. Med. Chem., 2021,64(18), 13853-13872. 6. ROS-Responsive and multifunctional anti-Alzheimer prodrugs: Tacrine-ibuprofen hybrids via a phenylboronate linker Zhikun Liu, Bin Zhang, Shengjin Xia, Lei Fang *, Shaohua Gou * Eur. J. Med. Chem., 2021, 212, 112997. 7. Design, synthesis and biological evaluation of sulfamoylphenyl-quinazoline derivatives as potentia lEGFR/CAIX dual inhibitors Bin Zhang, Zhikun Liu, Shengjin Xia, Qingqing Liu, Shaohua Gou * Eur. J. Med. Chem., 2021, 216, 113300. Jian Zhao, Kaiwen Yan, Gang Xu, Qiang Zhao,Chenjie Xu*, Shaohua Gou* Adv. Func. Materials, 2021, 31(11), 2008325. 9. A light-controlled multi-step drug release nanosystem targeting tumor hypoxia for synergistic cancer therapy. Bin Zhang, Zichen Xu, Wen Zhou, Zhikun Liu, Jian Zhao*, Shaohua Gou* Chem. Sci., 2021, 12, 11810–11820. 10 The introduction of immunosuppressor (TDO inhibitor) significantly improved theefficacy of irinotecan in treating hepatocellular carcinoma Qingqing Liu, Shixian Hua, XinyiWang, Feihong Chen*, Shaohua Gou* Cancer Immunology Immunotherapy, 21, 70, 497-508. 11. Breakdown of chemo-immune resistance by a TDO2-targeted Pt(IV) prodrug via attenuating endogenous Kyn-AhR-AQP4 metabolic circuity andTLS-promoted genomic instability Feihong Chen, Gang Xu, Wenyuan Tian, Shaohua Gou* Biochem. Pharmacology, 2021, 114785. 2020年 1. Platinum-based modification of styrylbenzylsulfonesas multifunctional antitumor agents: Targeting the RAS-RAF pathway, enhancing antitumor activity and overcoming multidrug resistance Zhikun Liu, Meng Wang, Hengshan Wang, Lei Fang*, Shaohua Gou* J. Med. Chem., 2020,63, 186-204. 2. Targeting RAS-RAF pathway significantly improves antitumor activity of Rigosertib- derived platinum(IV) complexes and overcome cisplatin resistance Zhikun Liu, Meng Wang, Hengshan Wang, Lei Fang*, Shaohua Gou* Eur. J. Med. Chem., 2020, 194, 12269. 3. Dual-functional conjugates improving cancer immunochemotherapy by inhibiting tubulin polymerization and indoleamine-2,3 -dioxygenase Shixian Hua, Feihong Chen, Xinyi Wang, Shaohua Gou* Eur. J. Med. Chem., 2020, 189, 112041 4. Iridium (III) complexes derived polymeric micelles with low dark toxicity and strong NIR excitation for phototherapy and chemotherapy Jian Zhao, Xinzhong Zhang, LeiFang*, Chuanzhu Gao, Chenjie Xu*, Shaohua Gou* Small, 2020, 16(14), 2000363. 5. Enhancing photodynamic therapy efficacy of upconversion-based nanoparticles conjugated with a long-lived triplet excited state iridium(III)-naphthalimide complex: toward highly enhanced hypoxia-inducible factor-1 Jian Zhao, Shuchen Sun, Xiaoyan Li, Wenjing Zhang,* Shaohua Gou* ACS Appl. Bio Mater. 2020, 3, 252−262. 6. Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3- dioxygenase Shixian Hua ,Feihong Chen, Shaohua Gou* Eur. J. Med. Chem., 2020, 187, 111949. 7. Design of a tris-heteroleptic Ru(II) complex with red-light excitation and remarkably improved photobiological activity Shuang Li, JianZhao*, Xinyi Wang, Gang Xu, Shaohua Gou*, Qiang Zhao* Inorg. Chem., 2020, 59(15), 11193-11204. 2019年 1. Construction of dual stimuli-responsive platinum(IV) hybrids with NQO1 targeting ability and overcoming cisplatin resistance Lei Fang, Xiaodong Qin, Jian Zhao, Shaohua Gou* Inorg. Chem., 2019, 58, 2291-2200. 2. Dinuclear organoruthenium complexes exhibit antiproliferative activity through DNA damage and ROS-mediated ER stress pathway JianZhao, Shuang Li, Xinyi Wang, Gang Xu, Shaohua Gou* Inorg. Chem., 2019, 58, 2208-2217. 3. Multifunctional platinum(IV) complexes as immuno stimulatory agents to promote cancer immunochemotherapy by inhibiting tryptophan-2,3-dioxygenase Shixian Hua, Feihong Chen,Gang Xu, Shaohua Gou* Eur. J. Med. Chem., 2019, 169, 29-41. 4. SHR-A1403, a c-Met antibody-drug conjugate, exerts encouraging anti-tumor activity in c-Met-overexpressed models Changyong Yang, Lei Wang, Xing Sun, Mi Tang, Haitian Quan, Lianshan Zhang, Liguang Lou*, Shaohua Gou* Acta Pharmcologic Sinica, 2019, 40(7),971-979. 5. Promoting antitumor efficacy by suppressing hypoxia via nano self-assembly of two irinotecan-based dual drug conjugates owning a HIF-1a inhibitor Bin Zhang, Xiaochao Huang, Hengshan Wang*, Shaohua Gou* J. Materials Chem. B, 2019, 7, 5352 - 5362. 2018年 1. Pt(IV) complexes conjugating with chalcone analogue as inhibitors of microtubule polymerizationexhibited selective inhibition in humancancer cells. Xiaochao Huang, Rizhen Huang, Zhimei Wang, Lingxue Li, Shaohua Gou*, Zhixin Liao, Hengshan Wang* Eur. J. Med. Chem., 2018, 146, 435-450. 2. Dual-targeting antitumor hybrids derived from Pt(IV) species and millepachine analogues Xiaochao Huang, Shixian Hua, Rizhen Huang, Zhikun Liu, Shaohua Gou*, Zhimei Wang, Zhixin Liao, Hengshan Wang* Eur. J. Med. Chem., 2018, 148, 1-25. 3. Theranostic Pt(IV) conjugatewith target selectivity for androgen receptor Xiaodong Qin, Lei Fang, Jian Zhao, Shaohua Gou* Inorg. Chem., 2018, 57(9),5019-5029. 4. Pt(IV)prodrugs containing microtubulin inhibitors displayed potent antitumor activityand ability to overcome cisplatin resistance Lingxue Li, Xiaochao Huang, Rizhen Huang, Shaohua Gou*, Zhimei Wang, Hengshan Wang* Eur. J. Med. Chem., 2018, 156, 666-679 . 5. Hypoxia-targeting organometallic Ru(II) arene complexes with enhanced anticancer activity in hypoxic cancer cells Jian Zhao, Wanchun Li, Shaohua Gou*, Shuang Li, Shengqiu Lin, Qianhui Wei, Gang Xu* Inorg. Chem., 2018, 57, 8396-8403. | |
