Hon-Chung Tsui
Schering-Plough
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Publication
Featured researches published by Hon-Chung Tsui.
Bioorganic & Medicinal Chemistry Letters | 2010
Dong Xiao; Cheng Wang; Anandan Palani; Hon-Chung Tsui; Gregory Reichard; Sunil Paliwal; Neng-Yang Shih; Robert Aslanian; Ruth Duffy; Jean Lachowicz; Geoffrey B. Varty; Cynthia Morgan; Fei Liu; Amin Nomeir
Modification of prototype NK(1) antagonist 2 resulted in the synthesis of a series of simple amides 6 and retroamides 9. These compounds were shown to be potent and orally active NK(1) antagonists.
Bioorganic & Medicinal Chemistry Letters | 2008
Sunil Paliwal; Gregory A. Reichard; Sapna Shah; Michelle Laci Wrobleski; Cheng Wang; Carmine Stengone; Hon-Chung Tsui; Dong Xiao; Ruth A. Duffy; Jean E. Lachowicz; Amin A. Nomeir; Geoffrey B. Varty; Neng-Yang Shih
Strategic replacement of the nitrogen of the lead compound 1 in the original cyclic urea series with a carbon resulted in the discovery of a novel, potent and orally more efficacious gamma-lactam series of selective NK(1) antagonists. Optimization of the lactam series culminated in the identification of compounds with high binding affinity and excellent oral CNS activity.
Bioorganic & Medicinal Chemistry Letters | 2018
Sobhana Babu Boga; Abdul-Basit Alhassan; Alan Cooper; Ronald J. Doll; Neng-Yang Shih; Gerald W. Shipps; Yongqi Deng; Hugh Zhu; Yang Nan; Robert Sun; Liang Zhu; Jagdish Desai; Kiran Muppalla; Xiaolei Gao; James Wang; Xin Yao; Joseph Kelly; Subrahmanyam Gudipati; Sunil Paliwal; Hon-Chung Tsui; Tong Wang; Bradley Sherborne; Li Xiao; Alan Hruza; Alexei V. Buevich; Li-Kang Zhang; David Hesk; Ahmed A. Samatar; Donna Carr; Brian Long
Compound 5 (SCH772984) was identified as a potent inhibitor of ERK1/2 with excellent selectivity against a panel of kinases (0/231 kinases tested @ 100 nM) and good cell proliferation activity, but suffered from poor PK (rat AUC PK @10 mpk = 0 μM h; F% = 0) which precluded further development. In an effort to identify novel ERK inhibitors with improved PK properties with respect to 5, a systematic exploration of sterics and composition at the 3-position of the pyrrolidine led to the discovery of a novel 3(S)-thiomethyl pyrrolidine analog 28 with vastly improved PK (rat AUC PK @10 mpk = 26 μM h; F% = 70).
ACS Medicinal Chemistry Letters | 2018
Sobhana Babu Boga; Yongqi Deng; Liang Zhu; Yang Nan; Alan Cooper; Gerald W. Shipps; Ronald J. Doll; Neng-Yang Shih; Hugh Zhu; Robert Sun; Tong Wang; Sunil Paliwal; Hon-Chung Tsui; Xiaolei Gao; Xin Yao; Jagdish Desai; James Wang; Abdul Basit Alhassan; Joseph Kelly; Kiran Muppalla; Subrahmanyam Gudipati; Li-Kang Zhang; Alexei V. Buevich; David Hesk; Donna Carr; Priya Dayananth; Stuart Black; Hong Mei; Kathleen Cox; Bradley Sherborne
The emergence and evolution of new immunological cancer therapies has sparked a rapidly growing interest in discovering novel pathways to treat cancer. Toward this aim, a novel series of pyrrolidine derivatives (compound 5) were identified as potent inhibitors of ERK1/2 with excellent kinase selectivity and dual mechanism of action but suffered from poor pharmacokinetics (PK). The challenge of PK was overcome by the discovery of a novel 3(S)-thiomethyl pyrrolidine analog 7. Lead optimization through focused structure-activity relationship led to the discovery of a clinical candidate MK-8353 suitable for twice daily oral dosing as a potential new cancer therapeutic.
Archive | 2006
Alan B. Cooper; Yongqi Deng; Gerald W. Shipps; Neng-Yang Shih; Hugh Y. Zhu; Robert Sun; Joseph M. Kelly; Ronald J. Doll; Yang Nan; Tong Wang; Jagdish A. Desai; James Wang; Youhao Dong; Vincent S. Madison; Li Xiao; Alan Hruza; M. Arshad Siddiqui; Ahmed A. Samatar; Sunil Paliwal; Hon-Chung Tsui; Azim A. Celebi; Yiji Wu; Sobhana Babu Boga
Bioorganic & Medicinal Chemistry Letters | 2006
Michelle Laci Wrobleski; Gregory A. Reichard; Sunil Paliwal; Sapna Shah; Hon-Chung Tsui; Ruth A. Duffy; Jean E. Lachowicz; Cynthia A. Morgan; Geoffrey B. Varty; Neng-Yang Shih
Archive | 2008
Robert Sun; Alan B. Cooper; Yongqi Deng; Tong Wang; Yang Nan; Hugh Y. Zhu; Sobhana Babu Boga; Xiaolei Gao; Joseph M. Kelly; Sunil Paliwal; Hon-Chung Tsui; Ronald J. Doll; Neng-Yang Shih
Archive | 2008
Alan Cooper; Yongqi Deng; Gerald W. Shipps; Neng-Yang Shih; Hugh Zhu; Joseph Kelly; Ronald J. Doll; Yang Nan; Jagdish Desai; James Wang; Sunil Paliwal; Hon-Chung Tsui; Sobhana Babu Boga; Abdul-Basit Alhassan; Xiaolei Gao; Liang Zhu
Archive | 2002
Sunil Paliwal; Gregory A. Reichard; Cheng Wang; Dong Xiao; Hon-Chung Tsui; Neng-Yang Shih; Juan D. Arredondo; Michelle Laci Wrobleski; Anandan Palani
Archive | 2002
Sunil Paliwal; Gregory A. Reichard; Cheng Wang; Dong Xiao; Hon-Chung Tsui; Neng-Yang Shih; Juan D. Arredondo; Michelle Laci Wrobleski; Anandan Palani