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SKLB1206, a novel orally available multikinase inhibitor targeting EGFR activating and T790M mutants, ErbB2, ErbB4, and VEGFR2, displays potent antitumor activity both in vitro and in vivo.
Pan Y, Xu Y, Feng S, Luo S, Zheng R, Yang J, Wang L, Zhong L, Yang HY, Wang BL, Yu Y, Liu J, Cao Z, Wang X, Ji P, Wang Z, Chen X, Zhang S, Wei YQ, Yang SY. Pan Y, et al. Among authors: yang sy, yang hy, yang j. Mol Cancer Ther. 2012 Apr;11(4):952-62. doi: 10.1158/1535-7163.MCT-11-0679. Epub 2012 Feb 8. Mol Cancer Ther. 2012. PMID: 22319204
Discovery of the novel potent and selective FLT3 inhibitor 1-{5-[7-(3- morpholinopropoxy)quinazolin-4-ylthio]-[1,3,4]thiadiazol-2-yl}-3-p-tolylurea and its anti-acute myeloid leukemia (AML) activities in vitro and in vivo.
Li WW, Wang XY, Zheng RL, Yan HX, Cao ZX, Zhong L, Wang ZR, Ji P, Yang LL, Wang LJ, Xu Y, Liu JJ, Yang J, Zhang CH, Ma S, Feng S, Sun QZ, Wei YQ, Yang SY. Li WW, et al. Among authors: yang sy, yang ll, yang j. J Med Chem. 2012 Apr 26;55(8):3852-66. doi: 10.1021/jm300042x. Epub 2012 Apr 6. J Med Chem. 2012. PMID: 22452518
Structural optimization and structure-activity relationships of N2-(4-(4-Methylpiperazin-1-yl)phenyl)-N8-phenyl-9H-purine-2,8-diamine derivatives, a new class of reversible kinase inhibitors targeting both EGFR-activating and resistance mutations.
Yang J, Wang LJ, Liu JJ, Zhong L, Zheng RL, Xu Y, Ji P, Zhang CH, Wang WJ, Lin XD, Li LL, Wei YQ, Yang SY. Yang J, et al. Among authors: yang sy. J Med Chem. 2012 Dec 13;55(23):10685-99. doi: 10.1021/jm301365e. Epub 2012 Nov 16. J Med Chem. 2012. PMID: 23116168
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.
Zhang CH, Zheng MW, Li YP, Lin XD, Huang M, Zhong L, Li GB, Zhang RJ, Lin WT, Jiao Y, Wu XA, Yang J, Xiang R, Chen LJ, Zhao YL, Cheng W, Wei YQ, Yang SY. Zhang CH, et al. Among authors: yang sy, yang j. J Med Chem. 2015 May 14;58(9):3957-74. doi: 10.1021/acs.jmedchem.5b00270. Epub 2015 Apr 16. J Med Chem. 2015. PMID: 25835317
From Lead to Drug Candidate: Optimization of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as Agents for the Treatment of Triple Negative Breast Cancer.
Zhang CH, Chen K, Jiao Y, Li LL, Li YP, Zhang RJ, Zheng MW, Zhong L, Huang SZ, Song CL, Lin WT, Yang J, Xiang R, Peng B, Han JH, Lu GW, Wei YQ, Yang SY. Zhang CH, et al. Among authors: yang sy, yang j. J Med Chem. 2016 Nov 10;59(21):9788-9805. doi: 10.1021/acs.jmedchem.6b00943. Epub 2016 Oct 26. J Med Chem. 2016. PMID: 27739679
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