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

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

作者： Ling-hua MENG Jian DING division of antitumor pharmacol.gy,State Key laboratory of Drug Research,shanghai institute of materia medica,Chinese Academy of Sciences,shanghai 201203.china division of antitumor pharmacol.gy 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 and antitumor evaluation of a new series of N-substi-tuted-thiourea derivatives

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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 pharmacol.gy,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 pharmacol.gy Shanghai Institute of Materia Medica Shanghai 201203 China 5division of antitumor pharmacol.gy 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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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 pharmacol.gy,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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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 pharmacol.gy,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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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 pharmacol.gy,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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