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Synthesis of the novel elemonic acid derivatives as Pin1 inhibitors.
Li, Xiaojing; Li, Lei; Zhou, Qingtong; Zhang, Na; Zhang, Shuzhi; Zhao, Rui; Liu, Dan; Jing, Yongkui; Zhao, Linxiang.
Afiliação
  • Li X; Key Laboratory of Structure-Based Drug Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
  • Li L; Department of Pharmacology, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
  • Zhou Q; Key Laboratory of Structure-Based Drug Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
  • Zhang N; Key Laboratory of Structure-Based Drug Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
  • Zhang S; Key Laboratory of Structure-Based Drug Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
  • Zhao R; Key Laboratory of Structure-Based Drug Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
  • Liu D; Key Laboratory of Structure-Based Drug Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
  • Jing Y; Department of Medicine, Mount Sinai School of Medicine, New York, NY 10029, USA. Electronic address: yongkui.jing@mssm.edu.
  • Zhao L; Key Laboratory of Structure-Based Drug Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, PR China. Electronic address: linxiang.zhao@vip.sina.com.
Bioorg Med Chem Lett ; 24(24): 5612-5615, 2014 Dec 15.
Article em En | MEDLINE | ID: mdl-25466185
A novel series of elemonic acid derivatives were synthesized and evaluated for their inhibitory activity on Pin1. Five compounds displayed significantly improved ability to inhibit Pin1 activity at micromolar levels. Compound 10 with 2-carboxylmethylene was the most active one with an IC50 value of 0.57 µM. The docking models of Pin1 support that introduction of an acidic group to elemonic acid enhance the Pin1 inhibitory activity.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Triterpenos / Peptidilprolil Isomerase / Inibidores Enzimáticos Limite: Humans Idioma: En Ano de publicação: 2014 Tipo de documento: Article
Texto completo
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Triterpenos / Peptidilprolil Isomerase / Inibidores Enzimáticos Limite: Humans Idioma: En Ano de publicação: 2014 Tipo de documento: Article