1. Synthesis and preliminary antiproliferative activity of new pteridin-7(8H)-one derivatives.
- Author
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Li, Zhong-Hua, Zhao, Tao-Qian, Liu, Xue-Qi, Zhao, Bing, Wang, Chao, Geng, Peng-Fei, Cao, Ya-Quan, Fu, Dong-Jun, Yu, Bin, Liu, Hong-Min, and Jiang, Li-Ping
- Subjects
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PTERIDINES , *CELL cycle , *STRUCTURE-activity relationships , *PURINES , *HETEROCYCLIC compounds , *CELL proliferation - Abstract
Pteridines are an important class of heterocyclic compounds with diverse biological activities. Here, we report a series of pteridin-7(8 H )-one derivatives and their antiproliferative activities toward MKN-45, MGC-803, EC-109, and H1650. Structure-activity relationship studies showed that compound 12 exerted the most potent antiproliferative activity against MKN-45 and MGC-803 with the IC 50 values of 4.32 and 7.01 μM, respectively. Besides, compound 12 induced morphological changes and apoptosis of MKN-45 cells, increased expression of Bax, down-regulated expression of Bcl-2 and caused cleavage of caspase-3/9. Additionally, we first reported the construction of the novel bicyclic 8,9-dihydro-7 H -purine-8-carboxylate scaffold through the competitive 5-endo cyclization reaction with two C-N bonds and a chiral carbon center established. [ABSTRACT FROM AUTHOR]
- Published
- 2018
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