2. Academic Validation
  3. Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors

Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors

  • J Med Chem. 2016 Aug 11;59(15):7268-74. doi: 10.1021/acs.jmedchem.6b00235.
Ji-Quan Zhang 1 2,  Yong-Jie Luo 1,  Yan-Shi Xiong 1,  Yang Yu 1,  Zheng-Chao Tu 3,  Zi-Jie Long 4,  Xiao-Ju Lai 5,  Hui-Xuan Chen 1,  Yu Luo 1,  Jiang Weng 1,  Gui Lu 1 6
Affiliations

Affiliations

  • 1 Institute of Medicinal Chemistry, School of Pharmaceutical Sciences, Sun Yat-sen University , Guangzhou, 510006, PR China.
  • 2 College of Pharmacy, Guizhou Medical University , Guiyang, 550004, PR China.
  • 3 Guangzhou Institute of Biomedicine and Health, Chinese Academy of Sciences , Guangzhou, 510530, PR China.
  • 4 Department of Hematology, The Third Affiliated Hospital, Sun Yat-sen University , Guangzhou, 510260, PR China.
  • 5 State Key Laboratory of Oncology in South China, Cancer Center, Sun Yat-sen University , Guangzhou, 510060, PR China.
  • 6 Institute of Human Virology, Sun Yat-sen University , Guangzhou, 510080, PR China.
PMID: 27427973 DOI: 10.1021/acs.jmedchem.6b00235
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 (PI3Kβ/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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