Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 76, Issue -, Pages -Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2022.129020
Keywords
Pyrido[34-d]pyrimidine derivatives; Antitumor activity; Proliferation; Apoptosis
Categories
Funding
- Natural Science Foundation of Henan Province
- National Natural Science Foundation of China
- China Postdoctoral Science Foundation
- [212300410392]
- [81903447]
- [81703328]
- [2021 M692943]
- [2020 M672249]
- [2022 T150465]
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In this study, 29 pyrido[3,4-d]pyrimidine compounds were designed and synthesized, and compound 30 showed the best anti-tumor activity against MGC803 cells. Mechanistic studies revealed that compound 30 inhibited cell migration and induced apoptosis. Compound 30 might be a potential lead agent for the treatment of human gastric cancers.
In order to find high-efficiency and low-toxic anti-tumor drugs, 29 pyrido[3,4-d]pyrimidine compounds were designed, synthesized and evaluated by MTT assay in vitro. The results presented that most of the compounds had good antitumor activities, among which compound 30 had the best anti-tumor activity on MGC803 cells (IC50 = 0.59 mu M). Mechanistic studies exhibited that compound 30 inhibited migration of MGC803 and induced apoptosis. It was proved that compound 30 up-regulated expression of Bid and PARP, down-regulated expression of CycD1 by western blot experiments. This study indicated that compound 30 might be served as a lead agent for the treatment of human gastric cancers.
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