1. Discovery of 6-chloro-2-(propylthio)-8,9-dihydro-7H-purines containing a carboxamide moiety as potential selective anti-lung cancer agents.
- Author
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Zhao, Tao-Qian, Zhao, Yuan-Di, Liu, Xin-Yang, Wang, Bo, Li, Zhong-Hua, He, Zhang-Xu, Zhang, Xin-Hui, Liang, Jian-Jia, Ma, Li-Ying, and Liu, Hong-Min
- Subjects
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PURINES , *CELL lines , *LUNG cancer , *STRUCTURE-activity relationship in pharmacology , *INTRINSIC factor (Physiology) , *PHYSIOLOGY , *THERAPEUTICS - Abstract
A new series of 6-chloro-2-(propylthio)-8,9-dihydro-7H-purine-8-caboxamide derivatives were designed, synthesized, and further evaluated for their antiproliferative activities on four human cancer cell lines (A549, MGC803, PC-3 and TE-1). The structure-activity relationships (SARs) studies were conducted through the variation in the two regions, which including position 8 and 9, of purine core. One of the compounds, 8 , containing a terminal piperazine appendage with a carboxamide moiety at position 8 and phenyl group at position 9 of 6-chloro-8,9-dihydro-7H-purine core, showed the most potent antiproliferative activity and good selectivity between cancer and normal cells (IC 50 values of 2.80 μM against A549 and 303.03 μM against GES-1, respectively). In addition, compound 8 could inhibit the colony formation and migration of A549 cells in a concentration-dependent manner, as well as induce the apoptosis possibly through the intrinsic pathway. [ABSTRACT FROM AUTHOR]
- Published
- 2018
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