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Your search keyword '"Yongqin Wan"' showing total 2 results
Start Over Author "Yongqin Wan" Journal journal of medicinal chemistry
2 results on '"Yongqin Wan"'

1. Synthesis, Structure–Activity Relationships, and in Vivo Efficacy of the Novel Potent and Selective Anaplastic Lymphoma Kinase (ALK) Inhibitor 5-Chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) Currently in Phase 1 and Phase 2 Clinical Trials

Author

Young Kim, Tove Tuntland, H. Martin Seidel, Thomas H. Marsilje, Nanxin Li, Wei Pei, You-Qun He, Xiaoming Cui, Wendy Richmond, Markus Warmuth, Auzon Steffy, Alex Aycinena, Sungjoon Kim, W. Perry Gordon, Donald S. Karanewsky, AnneMarie Culazzo Pferdekamper, Jin Yunho, Jonathan Chang, Ruo Steensma, Jennifer L. Harris, Bo Liu, Sean B. Joseph, Yelena Sarkisova, Christian C. Lee, Todd Groessl, Bei Chen, Wenshuo Lu, Chopiuk Greg, Tao Jiang, Kevin Johnson, Tetsuo Uno, Pierre-Yves Michellys, Jiqing Jiang, Andrew Phimister, Allen G. Li, Nathanael S. Gray, Badry Bursulaya, Frank Sun, Yongqin Wan, and Jie Li

Subjects
Pyrimidine, Brigatinib, Ceritinib, Chemistry, medicine.drug_class, Rational design, Pharmacology, ALK inhibitor, chemistry.chemical_compound, In vivo, hemic and lymphatic diseases, Drug Discovery, medicine, Molecular Medicine, Anaplastic lymphoma kinase, Structure–activity relationship, medicine.drug
Abstract

The synthesis, preclinical profile, and in vivo efficacy in rat xenograft models of the novel and selective anaplastic lymphoma kinase inhibitor 15b (LDK378) are described. In this initial report, preliminary structure–activity relationships (SARs) are described as well as the rational design strategy employed to overcome the development deficiencies of the first generation ALK inhibitor 4 (TAE684). Compound 15b is currently in phase 1 and phase 2 clinical trials with substantial antitumor activity being observed in ALK-positive cancer patients.

Published
2013

2. Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials

Author

Thomas H, Marsilje, Wei, Pei, Bei, Chen, Wenshuo, Lu, Tetsuo, Uno, Yunho, Jin, Tao, Jiang, Sungjoon, Kim, Nanxin, Li, Markus, Warmuth, Yelena, Sarkisova, Frank, Sun, Auzon, Steffy, AnneMarie C, Pferdekamper, Allen G, Li, Sean B, Joseph, Young, Kim, Bo, Liu, Tove, Tuntland, Xiaoming, Cui, Nathanael S, Gray, Ruo, Steensma, Yongqin, Wan, Jiqing, Jiang, Greg, Chopiuk, Jie, Li, W Perry, Gordon, Wendy, Richmond, Kevin, Johnson, Jonathan, Chang, Todd, Groessl, You-Qun, He, Andrew, Phimister, Alex, Aycinena, Christian C, Lee, Badry, Bursulaya, Donald S, Karanewsky, H Martin, Seidel, Jennifer L, Harris, and Pierre-Yves, Michellys

Subjects
Male, Clinical Trials, Phase I as Topic, Receptor Protein-Tyrosine Kinases, Xenograft Model Antitumor Assays, Rats, Macaca fascicularis, Structure-Activity Relationship, Clinical Trials, Phase II as Topic, Dogs, Pyrimidines, Neoplasms, Animals, Humans, Anaplastic Lymphoma Kinase, Sulfones, Protein Kinase Inhibitors
Abstract

The synthesis, preclinical profile, and in vivo efficacy in rat xenograft models of the novel and selective anaplastic lymphoma kinase inhibitor 15b (LDK378) are described. In this initial report, preliminary structure-activity relationships (SARs) are described as well as the rational design strategy employed to overcome the development deficiencies of the first generation ALK inhibitor 4 (TAE684). Compound 15b is currently in phase 1 and phase 2 clinical trials with substantial antitumor activity being observed in ALK-positive cancer patients.

Published
2013

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