In 2017,Molecules included an article by Xu, Shan; Sun, Chengyu; Chen, Chen; Zheng, Pengwu; Zhou, Yong; Zhou, Hongying; Zhu, Wufu. Application of 1158763-55-3. The article was titled 《Synthesis and biological evaluation of novel 8-morpholinoimidazo[1,2-a]pyrazine derivatives bearing phenylpyridine/phenylpyrimidine-carboxamides》. The information in the text is summarized as follows:
Three series of novel 8-morpholinoimidazo[1,2-a]pyrazine derivatives bearing phenylpyridine/phenylpyrimidine-carboxamides I [R = H, 4-Me, 3-F, etc.], II and III [R1 = H, 4-Me, 4-OMe, etc.] were designed and synthesized. All the compounds were evaluated for their IC50 values against three cancer cell lines (A549, PC-3 and MCF-7). Most of the target compounds exhibited moderate cytotoxicity against the three cancer cell lines. Two selected compounds III [R1 = 4-Me, 4-OMe] were further tested for their activity against PI3Kα kinase, and the results indicated that compound III [R1 = 4-OMe] showed inhibitory activity against PI3Kα kinase with an IC50 value of 1.25 μM. Structure-activity relationships (SARs) and pharmacol. results indicated that the replacement of the thiopyranopyrimidine with an imidazopyrazine was beneficial for the activity and the position of aryl group had a significant influence to the activity of these compounds The compounds II in which an aryl group substituted at the C-4 position of the pyridine ring were more active than I substituted at the C-5 position. Moreover, the cytotoxicity of compounds III bearing phenylpyrimidine-carboxamides was better than that of the compounds I and II bearing phenylpyridine-carboxamides. Furthermore, the substituents on the benzene ring also had a significant impact on the cytotoxicity and the pharmacol. results showed that electron donating groups were beneficial to the cytotoxicity. The results came from multiple reactions, including the reaction of 5-(3-Fluorophenyl)picolinic acid(cas: 1158763-55-3Application of 1158763-55-3)
5-(3-Fluorophenyl)picolinic acid(cas: 1158763-55-3) belongs to pyridine derivatives. The ring atoms in the pyridine molecule are sp2-hybridized. The nitrogen is involved in the π-bonding aromatic system using its unhybridized p orbital. Application of 1158763-55-3 Pyridine has a conjugated system of six π electrons that are delocalized over the ring.