Design, Synthesis and Biological Evaluation of Novel 1,3,5-triazines Derivatives as Potent Antitumor AgentsZhixu Zhou, Yalu Zhang, Ning Yan, Yude Wang and Tiemin Sun*
Key Laboratory of Structure-Based Drug Design and Discovery, Shenyang Pharmaceutical University, Shenyang, PR China
- *Corresponding Author:
- Tiemin Sun
Key Laboratory of Structure-Based Drug Design and Discovery
Shenyang Pharmaceutical University
Shenyang, PR China
E-mail: [email protected]
Received date: July 21, 2015; Accepted date: August 07, 2015; Published date: August 11, 2015
Citation: Zhou Z, Zhang Y, Yan N, Wang Y, Sun T (2015) Design, Synthesis and Biological Evaluation of Novel 1,3,5-triazines Derivatives as Potent Antitumor Agents. Med chem 5:345-350 doi: 10.4172/2161-0444.1000284
Copyright: © 2015 Zhou Z, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.
A series of 1,3,5-triazines derivatives were designed, synthesized and evaluated their biological activity. The preliminary investigation showed that most compounds displayed good to excellent potency against seven tested cancer cell lines as compared with ZSTK474. Compounds 5a, 7a and 7d were further examined for their inhibitory activity against PI3Kα kinase. The most promising compound 7d (PI3Kα half-maximal inhibitory concentration [IC50] = 10.56 nM) showed remarkable cytotoxicityagainst H1975, A549, PC9, HCT116, BT549, CNE2 and SW480 cell lines with IC50 values of 2.83 μM, 4.62 μM, 0.29 μM, 3.92 μM, 0.56 μM, 3.53 μM and 1.27 μM, respectively. The structure-activity relationships (SARs) analyses will guide us to further refine the structure of 1,3,5-triazines derivatives to achieve optimumanticancer activity.