药物设计方法与抗肿瘤靶向药物研究
81325021
2013
H3407.药物设计与药物信息
杨胜勇
国家杰出青年科学基金
教授
四川大学
200万元
药物设计方法;药效团模型;从头设计;打分函数;抗肿瘤靶向药物
2014-01至2017-12
- 中英文摘要
- 结题摘要
- 结题报告
- 项目成果
- 项目参与人
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| 序号 | 标题 | 类型 | 作者 |
|---|---|---|---|
| 1 | Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors | 期刊论文 | Xing-Dong Lin;Hui-Wen Yang;Shuang Ma;Wei-Wei Li;Chun-Hui Zhang;Wen-Jing Wang;Rong Xiang;Lin-Li Li;Sheng-Yong Yang |
| 2 | Design, Synthesis and Biological Evaluation of 1-Benzyl-1H-pyrazole Derivatives as Receptor Interacting Protein 1 Kinase Inhibitors | 期刊论文 | Zou Chan();Xiong Yu;Huang Lu-Yi;Song Chun-Li;Wu Xiao-Ai;Li Lin-Li();Yang Sheng-Yong() |
| 3 | A prediction model of drug-induced ototoxicity developed by an optimal support vector machine (SVM) method | 期刊论文 | Shu Zhou;Guo-Bo Li;Lu-Yi Huang;Huan-Zhang Xie;Ying-Lan Zhao;Yu-Zong Chen;Lin-Li Li;Sheng-Yong Yang |
| 4 | SKLB188 inhibits the growth of head and neck squamous cell carcinoma by suppressing EGFR signalling | 期刊论文 | Barzegar M;Ma S;Zhang C;Chen X;Gu Y;Shang C;Jiang X;Yang J;Nathan CA;Yang S;Huang S |
| 5 | Discovery of pyrazolo[1,5-a]pyrimidine-3-carbonitrile derivatives as a new class of histone lysine demethylase 4D (KDM4D) inhibitors | 期刊论文 | Fang Zhen();Wang Tian-Qi;Li Hui;Zhang Guo;Wu Xiao-Ai;Yang Li;Peng Yu-Lan;Zou Jun;Li Lin-Li;Xiang Rong();Yang Sheng-Yong() |
| 6 | SKLB-677, an FLT3 and Wnt/beta-catenin signaling inhibitor, displays potent activity in models of FLT3-driven AML | 期刊论文 | Ma Shuang;Yang Ling-Ling;Niu Ting;Cheng Chuan;Zhong Lei;Zheng Ming-Wu;Xiong Yu;Li Lin-Li;Xiang Rong;Chen Li-Juan;Zhou Qiao;Wei Yu-Quan;Yang Sheng-Yong |
| 7 | Discovery of KDM5A Inhibitors: Homology Modeling, Virtual Screening and Structure-Activity Relationship Analysis | 期刊论文 | Wu Xiao-Ai();Fang Zhen;Yang Bo;Zhong Lei;Yang Qiu-Yuan;Zhang Chun-Hui;Huang Shen-Zhen;Xiang Rong;Suzuki Takayoshi;Li Lin-Li();Yang Sheng-Yong() |
| 8 | Discovery of Potent and Selective Inhibitors of Cdc2-Like Kinase 1 (CLK1) as a New Class of Autophagy Inducers | 期刊论文 | Sun Qi-Zheng;Lin Gui-Feng;Li Lin-Li;Jin Xi-Ting;Huang Lu-Yi;Zhang Guo;Yang Wei;Chen Kai;Xiang Rong;Chen Chong;Wei Yu-Quan;Lu Guang-Wen;Yang Sheng-Yong |
| 9 | From Lead to Drug Candidate: Optimization of 3-(Phenylethyny1)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as Agents for the Treatment of Triple Negative Breast Cancer | 期刊论文 | Zhang, Chun-Hui; Chen, Kai; Jiao, Yan; Li, Lin-Li; Li, Ya-Ping; Zhang, Rong-Jie; Zheng, Ming-Wu; Zhong, Lei; Huang, Shen-Zhen; Song, Chun-Li; Lin, Wan-Ting; Yang, Jiao; Xiang, Rong; Peng, Bing; Han, Jun-Hong; Lu, Guang-Wen; Wei, Yu-Quan; Yang, Sheng-Yong |
| 10 | Discovery of New SIRT2 Inhibitors by Utilizing a Consensus Docking/Scoring Strategy and Structure-Activity Relationship Analysis | 期刊论文 | Huang Shen-Zhen();Song Chun-Li();Wang Xiang;Zhang Guo;Wang Yan-Lin;Jiang Xiao-Juan;Sun Qi-Zheng;Huang Lu-Yi;Xiang Rong;Hu Yi-Guo;Li Lin-Li();Yang Sheng-Yong() |
| 11 | A preclinical evaluation of a novel multikinase inhibitor, SKLB-329, as a therapeutic agent against hepatocellular carcinoma | 期刊论文 | Zhong Lei;Fu Xiao-Yu;Zou Chan;Yang Ling-Ling;Zhou Shu;Yang Jiao;Tang Yun;Cheng Chuan;Li Lin-Li;Xiang Rong;Chen Li-Juan;Chen Yu-Zong;Wei Yu-Quan;Yang Sheng-Yong |
| 12 | Preclinical Evaluation of a Novel Orally Available SRC/Raf/VEGFR2 Inhibitor, SKLB646, in the Treatment of Triple-Negative Breast Cancer | 期刊论文 | Zheng Ming-Wu;Zhang Chun-Hui;Chen Kai;Huang Mei;Li Ya-Ping;Lin Wan-Ting;Zhang Rong-Jie;Zhong Lei;Xiang Rong;Li Lin-Li;Liu Xin-Yu;Wei Yu-Quan;Yang Sheng-Yong |
| 13 | Drug Discovery against Psoriasis: Identification of a New Potent FMS-like Tyrosine Kinase 3 (FLT3) Inhibitor, 1-(4-((1H-Pyrazolo[3,4-d]pyrimidin-4-yl)oxy)-3-fluorophenyl)-3-(5-(tert- butyl)isoxazol-3-yl)urea, That Showed Potent Activity in a Psoriatic Animal Model | 期刊论文 | Li Guo-Bo;Ma Shuang;Yang Ling-Ling;Ji Sen;Fang Zhen;Zhang Guo;Wang Li-Jiao;Zhong Jie-Min;Xiong Yu;Wang Jiang-Hong;Huang Shen-Zhen;Li Lin-Li;Xiang Rong;Niu Dawen;Chen Ying-Chun;Yang Sheng-Yong |
| 14 | Discovery of selective protein arginine methyltransferase 5 inhibitors and biological evaluations | 期刊论文 | Ji Sen();Ma Shuang();Wang Wen-Jing();Huang Shen-Zhen;Wang Tian-Qi;Xiang Rong;Hu Yi-Guo;Chen Qiang;Li Lin-Li();Yang Sheng-Yong() |
| 15 | TS-Chemscore, a Target-Specific Scoring Function, Significantly Improves the Performance of Scoring in Virtual Screening | 期刊论文 | Wang Wen-Jing;Huang Qi;Zou Jun;Li Lin-Li;Yang Sheng-Yong |
| 16 | LEADOPT: An automatic tool for structure-based lead optimization, and its application in structural optimizations of VEGFR2 and SYK inhibitors | 期刊论文 | Guo-Bo Li;Sen Ji;Ling-Ling Yang;Rong-Jie Zhang;Kai Chen;Lei Zhong;Shuang Ma;Sheng-Yong Yang |
| 17 | Discovery and structure-activity analysis of 4-((5-nitropyrimidin-4-yl)amino)benzimidamide derivatives as novel protein arginine methyltransferase 1 (PRMT1) inhibitors | 期刊论文 | Yu Xu-Ri;Tang Yun;Wang Wen-Jing;Ji Sen;Ma Shuang;Zhong Lei;Zhang Chun-Hui;Yang Jiao;Wu Xiao-Ai;Fu Zheng-Yan;Li Lin-Li;Yang Sheng-Yong |
| 18 | Preclinical pharmacodynamic evaluation of drug candidate SKLB-178 in the treatment of non-small cell lung cancer | 期刊论文 | Zhong, Lei，Yang, Jiao，Cao, Zhixing，Chen, Xin，Hu, Yiguo，Li, Linli，Yang, Shengyong |
| 19 | 原创小分子靶向药物设计合成新方法及其在药物发现中的应用 | 奖励 | 杨胜勇 |
| 20 | A Preclinical Evaluation of SKLB261, a Multikinase Inhibitor of EGFR/Src/VEGFR2, as a Therapeutic Agent against Pancreatic Cancer | 期刊论文 | Youli Pan;Mingwu Zheng;Lei Zhong;Jiao Yang;Shu Zhou;Ya Qin;Rong Xiang;Yuzong Chen;Shengyong Yang |
| 21 | Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer | 期刊论文 | Zhang, Chun-Hui，Zheng, Ming-Wu，Li, Ya-Ping，Lin, Xing-Dong，Huang, Mei，Zhong, Lei，Li, Guo-Bo，Zhang, Rong-Jie，Lin, Wan-Ting，Jiao, Yan，Wu, Xiao-Ai，Yang, Jiao，Xiang, Rong，Chen, Li-Juan，Zhao, Ying-Lan，Cheng, Wei，Wei, Yu-Quan，Yang, Sheng-Yong |
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