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Design,synthesis and antitumor evaluation of a new series of N-substi-tuted-thiourea derivatives

Acta Pharmacologica Sinica 2006年第9期27卷 1259-1271页

作者： Jian LI~2 Jin-zhi TAN~2 Li-li CHEN~2 Jian ZHANG~2 Xu SHEN~(2,3)Chang-lin MEI~(4,6)Li-li FU~4 Li-ping LIN~5 Jian DING~5 Bing XIONG~2 Xi-shan XIONG~4 Hong LIU~(2,6)Xiao-min LUO~(2,6)Hua-liang JIANG~(2,3)2 Drug Discovery and Design Centre,State Key Laboratory of Drug Research,shanghai institute of materia medica,shanghai institutes for Biological Sciences,Chinese Academy of Sciences,shanghai 201203.china 3 School of Pharmacy.East china University of Science and Technology,shanghai 200237,china 4 division of Nephrology,Department of Internal Medicine,Changzheng Hospital,Second Military medical University,shanghai 200003,china 5 division of antitumor pharmacology,shanghai institute of materia medica,shanghai 201203.china 2Drug Discovery and Design Centre State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Shanghai Institutes for Biological Sciences Chinese Academy of Sciences Shanghai 201203 China 2Drug Discovery and Design Centre State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Shanghai Institutes for Biological Sciences Chinese Academy of Sciences Shanghai 201203 China 2Drug Discovery and Design Centre State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Shanghai Institutes for Biological Sciences Chinese Academy of Sciences Shanghai 201203 China 2Drug Discovery and Design Centre State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Shanghai Institutes for Biological Sciences Chinese Academy of Sciences Shanghai 201203 China 3School of Pharmacy East China University of Science and Technology Shanghai 200237 China 3School of Pharmacy East China University of Science and Technology Shanghai 200237 China 4division of Nephrology Department of Internal Medicine Changzheng Hospital Second Military Medical University Shanghai 200003 China 5division of antitumor pharmacology Shanghai Institute of Materia Medica Shanghai 201203 China 5division of antitumor pharmacology Shanghai Institute of Materia Medica Shanghai 201203 China 2Drug Discovery and Design Centre State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Shanghai Institutes for Biological Sciences Chinese Academy of Sciences Shanghai 201203 China 4division of Nephrology Department of Internal Medicine Changzheng Hospital Second Military Medical University Shanghai 200003 China 2Drug Discovery and Design Centre State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Shanghai Institutes for Biological Sciences Chinese Academy of Sciences Shanghai 201203 China 2Drug Discovery and Design Centre State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Shanghai Institutes for Bi

Aim:To design and synthesize a novel class of protein tyrosine kinase inhibitors,featuring the N-(2-oxo-1,2-dihydroquinolin-3-yl-methyl)-thiourea ***:First,compounds 1 and 2 were identified using the virtual screeningapproach in conjunction with binding assay based on surface plasmon ***,3 regions of compounds 1 and 2 were selected for chemical *** compounds were characterized potent inhibitory activities toward thehuman lung adenocarcinoma cell line SPAC ***:Forty new compounds(1-2,3a-g,4a-w,and 5a-l)were designed,synthesized and *** com-pounds(1,3e,41,4w,5a,and 5b)were found to show promising inhibitory activityagainst the SPAC1 tumor cell *** inhibitory activity of compound 5aincreases approximately 10 times more than that of the original compound ***:This study provides a promising new template with potential antitu-mot activity.

关键词： N-substituted-thiourea derivatives antitumor SPAC1 tyrosine kinase inhibitor virtual screening

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Salvicine,a novel topoisomerase Ⅱ inhibitor,exerts its potent anticancer activity by ROS generation

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Acta Pharmacologica Sinica 2007年第9期28卷 1460-1465页

作者： Ling-hua MENG Jian DING division of antitumor pharmacology,State Key laboratory of Drug Research,shanghai institute of materia medica,Chinese Academy of Sciences,shanghai 201203.china division of antitumor pharmacology State Key laboratory of Drug Research Shanghai Institute of Materia Medica Chinese Academy of Sciences Shanghai China

Salvicine is a novel diterpenoid quinone compound obtained by structural modi-fication of a natural product lead isolated from a Chinese herb with potent growthinhibitory activity against a wide spectrum of human tumor cells in vitro and inmice bearing human tumor xenografts. Salvicine has also been found to have aprofound cytotoxic effect on multidrug-resisitant (MDR) cells. Moreover, Salvicinesignificantly reduced the lung metastatic foci of MDA-MB-435 orthotopicxenograft. Recent studies demonstrated that salvicine is a novel non-intercalativetopoisomerase II (Topo II) poison by binding to the ATPase domain, promotingDNA-Topo II binding and inhibiting Topo II-mediated DNA relegation and ATPhydrolysis. Further studies have indicated that salcivine-elicited ROS plays acentral role in salvicine-induced cellular response including Topo II inhibition,DNA damage, circumventing MDR and tumor cell adhesion inhibition.

关键词： Salvicine is a novel diterpenoid quinone compound obtained by structural modi-fication of a natural product lead isolated from a Chinese herb with potent growthinhibitory activity against a wide spectrum of human tumor cells in vitro and inmice

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Design,synthesis,antitumor evaluations and molecular modeling studies of novel 3,5-substituted indolin-2-one derivatives

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Acta Pharmacologica Sinica 2007年第1期28卷 140-152页

作者： Hai-hong LI~2 Xiu-hua ZHANG~3 Jin-zhi TAN~2 Li-li CHEN~2 Hong LIU~(2,5) Xiao-min LUO~(2,5) Xu SHEN~(2,4) Li-ping LIN~(3,5) Kai-xian CHEN~2 Jian DING~3 Hua-liang JIANG~(2,4)2 Center for Drug Discovery and Design,State Key Laboratory of Drug Research,shanghai institute of materia medica,shanghai institutes for Biological Sciences,and Graduate School,Chinese Academy of Sciences,shanghai 201203.china 3 division of Anti-tumor pharmacology,shanghai institute of materia medica,shanghai institutes for Biological Sciences,Chinese Academy of Sciences,shanghai 201203.china 4 School of Pharmacy,East china University of Science and Technology,shanghai 200237,china CenterforDrugDiscoveryandDesign StateKeyLaboratoryofDrugResearchShanghaiInstituteofMateriaMedicaShanghaiInstitutesforBiologicalSciencesandGraduateSchoolChineseAcademyofSciencesShanghai201203China

Aim:To design and synthesize a novel class of antitumor agents,featuring the 3,5-substituted indolin-2-one ***:Based on enzyme binding fea-tures of（Z）-SU5402,introducing a β-pyrrole group at the 3-position of the indolin-2-one core,a series of novel 3,5-substituted indolin-2-ones were designed *** human carcinoma cell lines of A-43l,A-549,MDA-MB-468,and Autosomal Dominant Polycystic Kidney disease were chosen for the cellproliferation ***:Twenty new compounds（1a-t）with E configurationhave been designed,synthesized and *** structural features weredetermined by nuclear magnetic resonance（NMR）spectra,low-and high-resolu-tion mass spectra,and confirmed by X-ray *** the enzymeassay showed a weak inhibition effect against the epidermal growth factor receptor,vascular endothelial growth factor receptor,fibroblast growth factor receptor andplatelet-derived growth factor receptor tyrosine kinases,the cell-based antitumoractivity was *** 1 g and lh showed higher inhibitory activitytoward the A-549 and MDA-MB-468 cell lines with IC50of 0.065-9.4 μmol/***:This study provides a new template for further development ofpotent antitumor drugs.

关键词： protein-tyrosine kinase indolin-2-one antitumor drug screening assays drug design molecular models

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治疗高血压藥物的研究 Ⅵ.国产蘿芙木中水溶性生物鹼的藥理作用

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生理学报 1959年第1期 54-63页

作者： division OF pharmacology, institute OF materia medica, ACADEMIA SINICA(shanghai) 中国科学院药物研究所药理组上海

用蘿芙木屬(Rauwolfia)植物的生物鹼来治疗高血压已受到普遍的重视;其中以Reserpine最受注意,它有降低血压作用,并有特殊的鎮靜效能。我国广东、广西、云南諸省出产蘿芙木植物均为Rauwolfia verticillata(Lour.)Baill.,它的化学和藥理... 详细信息

用蘿芙木屬(Rauwolfia)植物的生物鹼来治疗高血压已受到普遍的重视;其中以Reserpine最受注意,它有降低血压作用,并有特殊的鎮靜效能。我国广东、广西、云南諸省出产蘿芙木植物均为Rauwolfia verticillata(Lour.)Baill.,它的化学和藥理均有报导。临床正拟試用国产蘿芙木治疗高血压。刘鑄晋等用离子交换剂获得蘿芙木全鹼,本文是研究它的毒性、降压及中樞鎮靜作用,以便推荐它到临床試用。

关键词：高血压皮下注射升压反应肾上腺素肾上腺能α-受体兴奋药小白鼠水溶性

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Synthesis and SAR Studies of Phenanthroindolizidine and Phenanthroquinolizidine Alkaloids as Potent antitumor Agents

Synthesis and SAR Studies of Phenanthroindolizidine and Phen...

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2011年全国药物化学学术会议——药物的源头创新

作者： Ziwen Wang~a,Meng Wu~a,Zheng Li~a,Lei Wang~a,Gui fang Han~a,Fazhong Chen~a,Yu xiu Liu~a, Kai liang Wang~b,Ao Zhang ~(*,b),Linghua Meng~c,Qing min Wang~(*,a) a:State Key Laboratory of Elemento-Organic Chemistry,Research institute of Elemento-Organic Chemistry,Nankai University,Tianjin 300071,People’s Republic of china b:division of Anti-tumor pharmacology,State Key Laboratory of Drug Research,shanghai institute of materia medica(SIMM), Chinese Academy of Sciences,shanghai 201203.china c:Synthetic Organic & Medicinal Chemistry Laboratory(SOMCL),shanghai institute of materia medica(SIMM),Chinese Academy of Sciences, shanghai 201203.china.

A series of phenanthroindolizidine and phenanthroquinolizidine alkaloids and their (13aS,14S)-14-amino-derivatives(1-44) were prepared and first systematically evaluated for their anti-tumor activities against A549 an... 详细信息

关键词： phenanthroindolizidine phenanthroquinolizidine anti-tumor activity blood-brain barrier

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Antihepatoma effect of alpha-fetoprotein antisense phosphorothioate oligodeoxyribonucleotides in vitro and in mice

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World Journal of Gastroenterology 2001年第3期7卷 345-351页

作者： Xing Wang Wang~1 Jin Hui Yuan~1 Ru Gang Zhang~1 Li Xia Guo~1 Yong Xie~2 Hong Xie~1 ~1Department of Biotherapy,shanghai institute of Cell Biology,Chinese Academy of Sciences,shanghai 200031,china ~2Department of Biology,Hong Kong University of Science and Technology,chinaDr.Xing Wang Wang earned Ph.D.from shanghai institute of materia medical,Chinese Academy of Sciences in 1997.Now a professor at shanghai institute of Cell Biology,Chinese Academy of Sciences. Department of Biotherapy Shanghai Institute of Cell Biology Chinese Academy of Sciences 320 Yue-Yang Road Shanghai 200031 China.

AIM: To evaluate antihepatoma effect of antisense phosphorothioate oligodeoxyribonucleotides (S-ODNs) targeted to alpha-fetoprotein (AFP) genes in vitro and in nude mice. METHODS: AFP gene expression was examined by immunocytochemical method or enzyme-linked immunosorbent assay. Effect of S-ODNs on SMMC-7721 human hepatoma cell growth in vitro was determined using microculture tetrazolium assay. In vitro antitumor activities of S-ODNs were monitored by measuring tumor weight differences in treated and control mice bearing SMMC-7721 xenografts. Induction of cell apoptosis was evaluated by fluorescence-activated cell sorter (FACS) analysis. RESULTS: Antisense S-ODN treatment led to reduced AFP gene expression. Specific antisense S-ODNs, but not control S-ODNs, inhibited the growth of hepatoma cells in vitro. In vitro, only antisense S-ODNs exhibited obvious antitumor activities. FACS analysis revealed that the growth inhibition by antisense S-ODNs was associated with their cell apoptosis induction. CONCLUSION: Antisense S-ODNs targeted to AFP genes inhibit the growth of human hepatoma cells and solid hepatoma, which is related to their cell apoptosis induction.

关键词： Animals Apoptosis Carcinoma, Hepatocellular Gene Expression Gene Therapy Humans In Vitro Liver Neoplasms Male Mice Mice, Inbred BALB C Mice, Nude Neoplasm Transplantation Oligodeoxyribonucleotides, Antisense Research Support, Non-U.S. Gov't Transplantation, Heterologous Tumor Cells, Cultured alpha-Fetoproteins

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AST-6,a novel irreversible inhibitor of the epidermal growth factor receptor 1 and 2,inhibits tumor growth both in vitro and in vivo

AST-6,a novel irreversible inhibitor of the epidermal growth...

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中国药理学会第十次全国学术会议

作者： XIE Hua~(1,*),LIN Li-pin~1,TONG Lin-jiang~1,JIANG Yong~3,ZHENG Ming-yue~2,WANG Yi~1,ZHANG Xiao-wei~1, GENG Mei-yu~1,JIANG Hua-liang~2,GUO Jian-hui~(3,*),DING Jian~(1,*) (1.division of antitumor pharmacology,2.Drug Discovery and Design Center,shanghai institute of materia medica, Chinese Academy of Sciences,shanghai 201203,P.R.china 3.Allist Pharmaceuticals,shanghai 201203,P.R.china)

Despite the initial response to the reversible ErbB-family inhibitors,cancer patients almost invariably develop *** evidence demonstrated that irreversible ErbB-family inhibitors were significantly active to override this ***,we found a novel quinazoline compound,AST-6,selectively inhibited enzymatic activities of wild type EGFR and ErbB2,and EGFR resistant ***,AST-6 functions as an irreversible in-

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Thiosemicarbazones derivatives design,synthesis and their anti-cancer activity study

Thiosemicarbazones derivatives design,synthesis and their an...

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第六届全国化学生物学学术会议

作者： Hong Liu,He Huang,Qin Chen,Linghua Meng,Jian Ding,Hualiang Jiang division of Drug Discovery and Design Center and Anti-tumor pharmacology,State Key Laboratory of Drug Research,shanghai institute of materia medica,Chinese Academy of Sciences,555 Zu Chong Zhi Road,Zhangjiang Hi-Tech Park,shanghai 201203,P.R.china

＜正＞Thiosemicarbazones are a class of iron chelators that have shown potent anti-cancer activities,some of which are under preclinical or clinical *** synthesized a class of novel thiosemicarbazone derivatives which...

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天然产物来源的抗肿瘤药物的发现和研究(英文)

天然产物来源的抗肿瘤药物的发现和研究(英文)

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第四届中国肿瘤学术大会暨第五届海峡两岸肿瘤学术会议

作者： Ding Jian division of Anti-Tumor pharmacology, State Key Laboratory of Drug Research, shanghai institute of materia medica, Chinese Academy of Sciences, shanghai, china.

＜正＞Natural Product is a very important resource for anticancer lead *** of the most promising research areas of shanghai institute of materia medica （SIMM） is novel anticancer agent discovery from Traditional Chinese *** is a natural alkaloid isolated from Camptotheca *** developed its derivative 10-hydroxycamptothecin in 1970s and it is still widely used in ***, we synthesized a novel amphoteric 9-substituted camptothecin, Chimmitecan, which confers unproved anti-cancer pharmacological profiles both in vitro and in ***, a natural product derivative from Salvia prionitis, is a new topoisomerase II *** also showed prominent anti-multidrug resistance effects and transcription factor c-Jun played a principal role in exerting this *** acid B got from Chinese plant Pseudolarix *** caused depolymerization of tubulin by binding to a novel site, and abrogated secretion of VEGF due to reducing hypoxia-inducible factor la protein by promoting proteasome pathway, which may responsible for its powerful anti-angiogenic effect

关键词： natural product Camptothecin Salvicine Chimmitecan Pseudolarix acid B

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Curcumin induces DNA damage and ATM/ATR-independent cell cycle arrest in colorectal carcinoma HCT 116 cells

Curcumin induces DNA damage and ATM/ATR-independent cell cyc...

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2011医学科学前沿论坛第十二届全国肿瘤药理与化疗学术...

作者： Jin-Jian Lu~(a,b),Yu-Jun Cai~(a,*),Jian Ding~(a,*) a division of Anti-tumor pharmacology,State Key Laboratory of Drug Research,shanghai institute of materia Mcdica,Chinese Academy of Science,shanghai 201203,P R.china b ''College of Life Sciences,Zhejiang Chinese medical University,Hangzhou,Zhejiang Province,310053,E R.china

＜正＞Curcumin（CUR） is a polyphenol derived from the plant Curcuma longa and displays potential anti-cancer *** of the mechanisms stems from its ability to induce cancer cell cycle arrest followed by suppression of cell proliferation. Herein,we reported that CUR significantly mediated DNA damage and S and G2/M phase arrest in colorectal carcinoma HCT116 *** etoposide（VP16）,a topoisomeraseⅡinhibitor,mediated cell cycle arrest,CUR-mediated G2/M phase arrest was hardly reversed by caffeine（CAFF）,an inhibitor of activated ataxia-telangiectasia-mutated （ATM）/ATM-and Rad3-related（ATR）,indicating that ATM and ATR signaling pathways are not involved in CUR-mediated cell cycle arrest in HCT116 ***,we demonstrated that CUR mediated mitosis arrest in HCT116 cells by using mitotic protein monoclonal antibody-2（MPM-2） as a mitosis marker and binds to tubulin using the surface plasmon resonance（SPR） *** findings provide new mechanisms of cell proliferation inhibition mediated by CUR in HCT116 cells.

关键词： curcumin DNA damage caffeine S phase arrest mitosis arrest tubulin

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