129006-34-4Relevant academic research and scientific papers
Phenyl and Diaryl Ureas with Thiazolo[5,4-d]pyrimidine Scaffold as Angiogenesis Inhibitors: Design, Synthesis and Biological Evaluation
Xue, Wen-Jun,Deng, Ya-Hui,Yan, Zhong-Hui,Liu, Ji-Ping,Liu, Yu,Sun, Li-Ping
, (2019/04/03)
Angiogenesis is crucial for tumor growth and inhibition of angiogenesis has been regarded as a promising approach for cancer therapy. Vascular endothelial growth factor receptor-2 (VEGFR-2) is an important factor in angiogenesis. In this work, a novel series of thiazolo[5,4-d]pyrimidine derivatives inhibiting angiogenesis were rationally designed and synthesized. Their inhibitory activities against human umbilical vein endothelial cells (HUVEC) were investigated in vitro. 1-(4-Fluorophenyl)-3-{4-[(5-methyl-2-phenyl[1,3]thiazolo[5,4-d]pyrimidin-7-yl)amino]phenyl}urea (19b) and 1-(3-Fluorophenyl)-3-{4-[(5-methyl-2-phenyl[1,3]thiazolo[5,4-d]pyrimidin-7-yl)amino]phenyl}urea (19g) exhibited the most potent inhibitory effect on HUVEC proliferation (IC50=12.8 and 5.3 μm, respectively). Compound 19g could inhibit the migration of human umbilical vein endothelial cells. These results support the further investigation of these compounds as potent anticancer agents.
Facile synthesis of 2,5,7-trisubstituted oxazolo[5,4-d]pyrimidines via copper-catalyzed intramolecular C-O bond formation
Xu, Dan,Sun, Li-Ping,You, Qi-Dong
experimental part, p. 4248 - 4251 (2012/07/14)
A novel and convenient synthesis of 2,5,7-trisubstituted oxazolo[5,4-d]pyrimidines was presented. The key step involved an intramolecular C-O cross-coupling of the ortho-halopyrimidine amide via a copper (I)-mediated cyclization reaction, which provided t
Purines. X. Reactivities of methyl groups on 9-phenylpurines: Condensation with an aldehyde or an ester, and oxidation with selenium dioxide
Tanji,Satoh,Higashino
, p. 227 - 229 (2007/10/02)
The condensation of a methyl group at the 6- or 8-position on the 9H-purine ring with benzaldehyde and ethyl benzoate in the presence of sodium hydride occurred to give the styryl- (4a, b) and phenacyl-9H-purines (5a, b and 6a,b). Conversion of the methyl
PURINES. IX. REACTION OF 9-PHENYL-9H-PURINE-2-CARBONITRILES WITH GRIGNARD REAGENTS
Tanji, Ken-ichi,Higashino, Takeo
, p. 435 - 440 (2007/10/02)
The palladium-catalyzed cross-coupling reaction of 2- and 6-chloro-9-phenyl-9H-purines with potassium cyanide proceeded to give 9-phenyl-9H-purine-2- (3a-c) and -6-carbonitriles (4a-c).The conversion of the cyano group at the 2-position into the correspon
