Your browser doesn't support javascript.
loading
Design, synthesis and antiproliferative effect of 17ß-amide derivatives of 2-methoxyestradiol and their studies on pharmacokinetics.
Shi, Xiufang; Wang, Zhihao; Xu, Feng; Lu, Xiang; Yao, Haifeng; Wu, Dandan; Sun, Shuaijun; Nie, Ruifang; Gao, Shuo; Li, Panpan; Xia, Liwen; Zhang, Zhenzhong; Wang, Cong.
Afiliación
  • Shi X; School of Pharmaceutical Sciences, and Institute of Drug Discovery & Development, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan 450001, China; Key Laboratory of Technology of Drug Preparation (Zhengzhou University), Ministry of Education of China, China; Key Laboratory of Henan Provin
  • Wang Z; School of Pharmaceutical Sciences, and Institute of Drug Discovery & Development, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan 450001, China; Key Laboratory of Technology of Drug Preparation (Zhengzhou University), Ministry of Education of China, China; Key Laboratory of Henan Provin
  • Xu F; School of Pharmaceutical Sciences, and Institute of Drug Discovery & Development, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan 450001, China; Key Laboratory of Technology of Drug Preparation (Zhengzhou University), Ministry of Education of China, China; Key Laboratory of Henan Provin
  • Lu X; School of Pharmaceutical Sciences, and Institute of Drug Discovery & Development, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan 450001, China; Key Laboratory of Technology of Drug Preparation (Zhengzhou University), Ministry of Education of China, China; Key Laboratory of Henan Provin
  • Yao H; School of Pharmaceutical Sciences, and Institute of Drug Discovery & Development, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan 450001, China; Key Laboratory of Technology of Drug Preparation (Zhengzhou University), Ministry of Education of China, China; Key Laboratory of Henan Provin
  • Wu D; School of Pharmaceutical Sciences, and Institute of Drug Discovery & Development, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan 450001, China; Key Laboratory of Technology of Drug Preparation (Zhengzhou University), Ministry of Education of China, China; Key Laboratory of Henan Provin
  • Sun S; School of Pharmaceutical Sciences, and Institute of Drug Discovery & Development, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan 450001, China; Key Laboratory of Technology of Drug Preparation (Zhengzhou University), Ministry of Education of China, China; Key Laboratory of Henan Provin
  • Nie R; School of Pharmaceutical Sciences, and Institute of Drug Discovery & Development, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan 450001, China; Key Laboratory of Technology of Drug Preparation (Zhengzhou University), Ministry of Education of China, China; Key Laboratory of Henan Provin
  • Gao S; School of Pharmaceutical Sciences, and Institute of Drug Discovery & Development, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan 450001, China; Key Laboratory of Technology of Drug Preparation (Zhengzhou University), Ministry of Education of China, China; Key Laboratory of Henan Provin
  • Li P; School of Pharmaceutical Sciences, and Institute of Drug Discovery & Development, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan 450001, China; Key Laboratory of Technology of Drug Preparation (Zhengzhou University), Ministry of Education of China, China; Key Laboratory of Henan Provin
  • Xia L; School of Pharmaceutical Sciences, and Institute of Drug Discovery & Development, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan 450001, China; Key Laboratory of Technology of Drug Preparation (Zhengzhou University), Ministry of Education of China, China; Key Laboratory of Henan Provin
  • Zhang Z; School of Pharmaceutical Sciences, and Institute of Drug Discovery & Development, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan 450001, China; Key Laboratory of Technology of Drug Preparation (Zhengzhou University), Ministry of Education of China, China; Key Laboratory of Henan Provin
  • Wang C; School of Pharmaceutical Sciences, and Institute of Drug Discovery & Development, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan 450001, China; Key Laboratory of Technology of Drug Preparation (Zhengzhou University), Ministry of Education of China, China; Key Laboratory of Henan Provin
Steroids ; 128: 6-14, 2017 12.
Article en En | MEDLINE | ID: mdl-29031938
ABSTRACT
A series of 17ß-amide-2-methoxyestradiol compounds were synthesized with an aim to enhance the antiproliferative effect of 2-methoxyestradiol. The antiproliferative activity of 2-methoxyestradiol analogs against human cancer cells was investigated. 2-methoxy-3-benzyloxy-17ß-chloroacetamide-1,3,5(10)-triene (5e) and 2-methoxy-3-hydroxy-17ß-butyramide-1,3,5(10)-triene (6c) had comparable or better antitumor activity than 2-methoxyestradiol. The elimination half-life of 6c (t1/2ß=240.93min) is ten times longer than 2-ME and the area under the curve was seven times (AUC0-tmin=2068.20±315.74µgmL-1min) higher than 2-ME, respectively. Whereas 5e had similar pharmacokinetic behavior with 2-ME (t1/2ß=22.28min) with a t1/2ß of 29.5 min. 6c had higher blood concentration, longer actuation duration and better suppression rate against S180 mouse ascites tumor than 2-methoxyestradiol.
Asunto(s)
Palabras clave
Texto completo
Añadir a Mi BVS
Imprimir
XML
PubMed Links
Buscar en Google

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Proliferación Celular / Estradiol / Neoplasias Tipo de estudio: Prognostic_studies Límite: Animals / Humans Idioma: En Revista: Steroids Año: 2017 Tipo del documento: Article
Texto completo
Añadir a Mi BVS
Imprimir
XML
PubMed Links
Buscar en Google

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Proliferación Celular / Estradiol / Neoplasias Tipo de estudio: Prognostic_studies Límite: Animals / Humans Idioma: En Revista: Steroids Año: 2017 Tipo del documento: Article