77373-43-4Relevant academic research and scientific papers
Design, synthesis, and biological evaluation of C-2 substituted 3H-thieno[2,3-d]pyrimidin-4-one derivatives as novel FGFR1 inhibitors
Guo, Ping,Xie, Zixin,Zhang, Huan,Zhang, Zaikui,Han, Chao,Cheng, Donghua,Lin, Dan,Zhang, Yuan,Wang, Xuebao,Guo, Xin,Ye, Faqing
, p. 753 - 760 (2017/12/28)
Background: Thienopyrimidinone is a newly designed, selective fibroblast growth factor receptor 1 (FGFR1) inhibitor with an excellent anticancer effect. Objective: The goal of the present study was to design and synthesize better FGFR1 inhibitors through modifications of the lead compound thienopyrimidinone. Methods: In the present study, a series of C-2 substituted derivatives of thienopyrimidinone, namely L1–L16, were synthesized, and their inhibitory effects on FGFR1 were evaluated. The anti-proliferative activities of these compounds were assessed by MTT assay. Results: Among the novel derivatives, L11 was found to exert remarkable FGFR1 inhibitory activity (79.93% at 10 M) and anti-proliferative activity, with IC50 values of 2.1, 2.5, and 3.5 M in the FGFR1-overexpressing cell lines, H460, HT-1197, and B16F10, respectively. Conclusion: Our newly synthesized thienopyrimidinone derivatives may be candidate FGFR1 inhibitors for future development as novel anticancer agents.
NEW DISPERSE DYE WITH POTENT ANTICANCER ACTIVITY
-
Page/Page column 1, (2012/09/22)
New yellow disperse dye of 2-cinnamyl-5,6,7,8- tetrahydro[l]benzothieno[2,3-d]pyrimidine-4(3H)-one with a first medical application as anticancer showing potent activity against different cancer cell lines and low cytotoxicity to melanocytes (normal skin) which will be helpful in treatment of cancer specially melanoma due to dye stability on the skin.
Reaction of Nitriles under Acidic Conditions. Part I. A General Method of Synthesis of Condensed Pyrimidines
Dave, K. G.,Shishoo, G. J.,Devani, M. B.,Kalyanaraman, R.,Ananthan, S.,et. al.
, p. 1497 - 1500 (2007/10/02)
Nitriles are known to give rise to salts of different compositions with halogen acids.Many of the reactions undergone by nitriles under the influence of halogen acids are, in many cases, assumed to proceed via the intermediate formation of highly reactive
