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Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors.
Zhang, Ji-Quan; Luo, Yong-Jie; Xiong, Yan-Shi; Yu, Yang; Tu, Zheng-Chao; Long, Zi-Jie; Lai, Xiao-Ju; Chen, Hui-Xuan; Luo, Yu; Weng, Jiang; Lu, Gui.
Afiliação
  • Zhang JQ; Institute of Medicinal Chemistry, School of Pharmaceutical Sciences, Sun Yat-sen University , Guangzhou, 510006, PR China.
  • Luo YJ; College of Pharmacy, Guizhou Medical University , Guiyang, 550004, PR China.
  • Xiong YS; Institute of Medicinal Chemistry, School of Pharmaceutical Sciences, Sun Yat-sen University , Guangzhou, 510006, PR China.
  • Yu Y; Institute of Medicinal Chemistry, School of Pharmaceutical Sciences, Sun Yat-sen University , Guangzhou, 510006, PR China.
  • Tu ZC; Institute of Medicinal Chemistry, School of Pharmaceutical Sciences, Sun Yat-sen University , Guangzhou, 510006, PR China.
  • Long ZJ; Guangzhou Institute of Biomedicine and Health, Chinese Academy of Sciences , Guangzhou, 510530, PR China.
  • Lai XJ; Department of Hematology, The Third Affiliated Hospital, Sun Yat-sen University , Guangzhou, 510260, PR China.
  • Chen HX; State Key Laboratory of Oncology in South China, Cancer Center, Sun Yat-sen University , Guangzhou, 510060, PR China.
  • Luo Y; Institute of Medicinal Chemistry, School of Pharmaceutical Sciences, Sun Yat-sen University , Guangzhou, 510006, PR China.
  • Weng J; Institute of Medicinal Chemistry, School of Pharmaceutical Sciences, Sun Yat-sen University , Guangzhou, 510006, PR China.
  • Lu G; Institute of Medicinal Chemistry, School of Pharmaceutical Sciences, Sun Yat-sen University , Guangzhou, 510006, PR China.
J Med Chem ; 59(15): 7268-74, 2016 08 11.
Article em En | MEDLINE | ID: mdl-27427973
ABSTRACT
Three series of substituted pyrimidines were designed and synthesized. All target compounds were screened for kinase inhibitory activities against PI3Kα, and most IC50 values were found within the nanomolar range. Compounds 5d and 5p displayed comparable activities relative to the positive control 5a. 5p also showed a significant isozyme selectivity (PI3Kß/α). Furthermore, the cytotoxicities of these pyrimidines against human cancer cell lines were evaluated and the in vivo anticancer effect of 5d was also tested.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Pirimidinas / Desenho de Fármacos / Inibidores de Proteínas Quinases / Inibidores de Fosfoinositídeo-3 Quinase / Antineoplásicos Limite: Humans Idioma: En Revista: J Med Chem Assunto da revista: QUIMICA Ano de publicação: 2016 Tipo de documento: Article
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Pirimidinas / Desenho de Fármacos / Inibidores de Proteínas Quinases / Inibidores de Fosfoinositídeo-3 Quinase / Antineoplásicos Limite: Humans Idioma: En Revista: J Med Chem Assunto da revista: QUIMICA Ano de publicação: 2016 Tipo de documento: Article