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Synthesis of Novel Analogs of Thieno[2,3-d] Pyrimidin-4(3H)-ones as Selective Inhibitors of Cancer Cell Growth

College of Life Sciences, Shanghai Normal University, Shanghai 201418, China
Key Laboratory of Plant Resources and Chemistry of Arid Zone, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi 830011, China
University of Chinese Academy of Sciences, Beijing 100049, China
Authors to whom correspondence should be addressed.
Biomolecules 2019, 9(10), 631;
Received: 21 September 2019 / Revised: 16 October 2019 / Accepted: 17 October 2019 / Published: 21 October 2019
(This article belongs to the Special Issue Bioactives from Marine Products)
New 2,3-disubstituted thieno[2,3-d]pyrimidin-4(3H)-ones were synthesized via a one-pot reaction from 2H-thieno[2,3-d] [1,3]oxazine-2,4(1H)-diones, aromatic aldehydes, and benzylamine or 4-hydroxylbezylamine. The obtained compounds were tested in vitro for cancer cell growth inhibition. Compound 19 can inhibit all four types of tested cancer cells, i.e., MCF-7, A549, PC-9, and PC-3 cells. Most of the compounds inhibited the proliferation of A549 and MCF-7 cells. Compound 15 exhibited the strongest anti-proliferative effect against A549 cell lines with IC50 values of 0.94 μM, and with no toxicity to normal human liver cells. Its potency was further proved by cell clone formation assay, Hoechst 33258 staining, and evaluation on the effects of apoptosis-related proteins. View Full-Text
Keywords: thienopyrimidine; thieno[2,3-d] pyrimidinone; anticancer thienopyrimidine; thieno[2,3-d] pyrimidinone; anticancer
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Zhang, S.; Liu, F.; Hou, X.; Cao, J.; Dai, X.; Yu, J.; Huang, G. Synthesis of Novel Analogs of Thieno[2,3-d] Pyrimidin-4(3H)-ones as Selective Inhibitors of Cancer Cell Growth. Biomolecules 2019, 9, 631.

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