European Journal of Medicinal Chemistry p. 1396 - 1405 (2018)
Update date:2022-08-05
Topics:
Li, Zhong-Hua
Zhao, Tao-Qian
Liu, Xue-Qi
Zhao, Bing
Wang, Chao
Geng, Peng-Fei
Cao, Ya-Quan
Fu, Dong-Jun
Jiang, Li-Ping
Yu, Bin
Liu, Hong-Min
Pteridines are an important class of heterocyclic compounds with diverse biological activities. Here, we report a series of pteridin-7(8H)-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 IC50 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-7H-purine-8-carboxylate scaffold through the competitive 5-endo cyclization reaction with two C-N bonds and a chiral carbon center established.
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