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中文摘要：
本项目应用基因组学、蛋白组学和生物信息学的最新研究成果，以具有抗肿瘤活性的先导化合物为纽带，整合多学科的优势，研究新的作用机理，发现新的肿瘤靶向分子或候选药物。通过本项目的实施，确定了4个新的分子靶向抗肿瘤候选药物，其中广谱酪氨酸激酶抑制剂AL3810和拓扑异构酶抑制剂希明替康已完成全部临床前研究；mTOR抑制剂Y31和乙酰肝素酶抑制剂JG6处于临床前研究阶段。4个候选新药都具有自主知识产权，全部获得国家重大专项"重大新药创制"资助；针对PI3K/mTOR信号传导通路、c-met激酶、PARP1等抗肿瘤新分子靶点，发现了一批新型的抗肿瘤先导化合物，申请中国专利19项，国际专利 3项；在抗肿瘤药物作用机制、新化合物发现、构效关系研究以及分子标志物探寻等方面，有一系列新发现，发表SCI学术论文59 篇，其中40余篇影响因子大于3；"拓扑异构酶II新型抑制剂沙尔威辛的抗肿瘤分子机制"获2009年国家自然科学二等奖；研究团队的学术水平，创新意识和团队合作精神得到提升；学术带头人丁健研究员2009年当选为中国工程院院士，培养了一批青年科研人才，包括32名博士，10名硕士，3名博士后。
结论摘要：
英文主题词molecularly targeted; anticancer drugs; tyrokine kinase, PI3K/mTOR
成果综合统计
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期刊论文
Salvicine triggers DNA double-strand breaks and apoptosis by GSH-depletion-driven H2O2 generation an
Increased accumulation of hypoxia-inducible factor-1 alpha with reduced transcriptional activity med
Echinoside A, a new marine-derived anticancer saponin, targets topoisomerase2 alpha by unique interf
WJD008, a Dual Phosphatidylinositol 3-Kinase (PI3K)/Mammalian Target of Rapamycin Inhibitor, Prevent
Structure Determination of Grandifotane A from Khaya grandifoliola by NMR, X-ray Diffraction, and EC
Synthesis of N-11-anchoring biotinylated artemisinin derivatives and their preliminary biological as
MFTZ-1 reduces constitutive and inducible HIF-1 alpha accumulation and VEGF secretion independent of
Efficient synthesis of triarylmethanes via bisarylation of aryl aldehydes with arenes catalyzed by s
Identification of p27/KIP1 expression level as a candidate biomarker of response to rapalogs therapy
Dihydroartemisinin accelerates c-MYC oncoprotein degradation and induces apoptosis in c-MYC-overexpr
c-Jun Protects Hypoxia-Inducible Factor-1 alpha from Degradation via Its Oxygen-Dependent Degradatio
Direct Palladium-Catalyzed Arylations of Aryl Bromides with 2/9-Substituted Pyrimido[5,4-b]indolizin
Design and Synthesis of Novel C14-Hydroxyl Substituted Triptolide Derivatives as Potential Selective
GA3, a new gambogic acid derivative, exhibits potent antitumor activities in vitro via apoptosis-inv
S9, a Novel Anticancer Agent, Exerts Its Anti-Proliferative Activity by Interfering with Both PI3K-A
Harrisotones A-E, five novel prenylated polyketides with a rare spirocyclic skeleton from Harrisonia
Simple Cyclohexanediamine-Derived Primary Amine Thiourea Catalyzed Highly Enantioselective Conjugate
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