51069-75-1Relevant articles and documents
Synthesis and biological evaluation of harmirins, novel harmine–coumarin hybrids as potential anticancer agents
Beus, Maja,Kralj, Marijeta,Pavi?, Kristina,Poje, Goran,Raji?, Zrinka,Uzelac, Lidija
, (2021/11/08)
As cancer remains one of the major health burdens worldwide, novel agents, due to the development of resistance, are needed. In this work, we designed and synthesized harmirins, which are hybrid compounds comprising harmine and coumarin scaffolds, evaluat
Efficient Synthesis of Pyrido[3,2-c[coumarins via Silver Nitrate Catalyzed Cycloisomerization and Application to the First Synthesis of Polyneomarline C
Han, Young Taek,Yoon, Jeong A
supporting information, p. 4611 - 4618 (2019/12/11)
Herein, we report an efficient method for the synthesis of the pyrido[3,2-c[coumarin scaffold, one of the privileged heterocycle-fused coumarin scaffolds, via a AgNO 3-catalyzed cycloisomerization of 4-(propynylamino)coumarins obtained from div
Synthesis and biological evaluation of novel phosphoramidate derivatives of coumarin as chitin synthase inhibitors and antifungal agents
Ji, Qinggang,Ge, Zhiqiang,Ge, Zhixing,Chen, Kaizhi,Wu, Hualong,Liu, Xiaofei,Huang, Yanrong,Yuan, Lvjiang,Yang, Xiaolan,Liao, Fei
, p. 166 - 176 (2015/12/04)
A series of novel phosphoramidate derivatives of coumarin have been designed and synthesized as chitin synthase (CHS) inhibitors. All the synthesized compounds have been screened for their chitin synthase inhibition activity and antimicrobial activity in vitro. The bioactive assay manifested that most of the target compounds exhibited good efficacy against CHS and a variety of clinically important fungal pathogens. In particular, compound 7t with IC50 of 0.08 mM against CHS displayed stronger efficiency than the reference Polyoxin B with IC50 of 0.16 mM. In addition, the apparent Ki values of compound 7t was 0.096 mM while the Km of Chitin synthase prepared from Candida tropicalis was 3.86 mM for UDP-Nacetylglucosamine, and the result of the Ki showed that the compounds was a non-competitive inhibitor of the CHS. As far as the antifungal activity is concerned, compounds 7o, 7r and 7t were highly active against Aspergillus flavus with MIC values in the range of 1 μg/mL to 2 μg/Ml while the results of antibacterial screening showed that these compounds have negligible actions to the tested bacteria. These results indicated that the design of these compounds as antifungal agents was rational.