12239-58-6Relevant articles and documents
Microwave-promoted one-pot syntheses of coumarin dyes
Nourmohammadian, Farahnaz,Gholami, Mahnaz Davoodzadeh
, p. 901 - 909 (2010)
To one pot synthesis of coumarins with benzimidazol or benzoxazol moieties, three different microwave irradiations based procedures are reported here which take place within a few minutes. In spite of fairly well yield of the products using solvent free procedures, 25-30% further yields were achieved within 3 minutes at 110C using 2mL n-pentanol as solvent.
Synthesis and anti-angiogenesis activity of coumarin derivatives
Lee, Seokjoon,Sivakumar, Krishnamoorthy,Shin, Woon-Seob,Xie, Fang,Wang, Qian
, p. 4596 - 4599 (2006)
A series of 7-diethylaminocoumarin compounds were synthesized and the cytotoxicities were tested against human umbilical vein endothelial cell (HUVEC) and some cancer cells. We found that the introduction of cyano groups at the 4-position will promote the bioactivity. In particular, compounds 9 and 10 strongly inhibited the proliferation of various cancer cell lines, and 12 and 15 showed a high selectivity for HUVEC. Therefore, these coumarin molecules can be utilized as lead compounds to develop potential nontoxic angiogenesis inhibitors and small molecular ligands to target HUVEC.
Facile synthesis and fluorescent properties of coumarin-7 and its isomer 4-(2-benzimidazolyl)-7-(diethylamino)coumarin
Wang, Xiaolong,Yang, Fang,Xue, Ziyan,Wang, Xiaoqiang,Chen, Chen
, p. 213 - 215 (2015)
Coumarin-7 and its isomer 4-(2-benzimidazolyl)-7-(diethylamino)coumarin were synthesised using condensation of the corresponding formylcoumarin with o-phenylenediamine as the key step. Moreover, absorption and fluorescence emission spectra of these two coumarins were recorded.
Development of benzimidazole derivatives to inhibit HIV-1 replication through protecting APOBEC3G protein
Pan, Ting,He, Xin,Chen, Bing,Chen, Hui,Geng, Guannan,Luo, Haihua,Zhang, Hui,Bai, Chuan
, p. 500 - 513 (2015/04/14)
Human APOBEC3G (apolipoprotein B mRNA-editing enzyme, catalytic polypeptide-like 3G, A3G) is a potent restriction factor against human immunodeficiency virus type 1 (HIV-1) by inducing hypermutation of G to A in viral genome after its incorporation into virions. HIV-1 Vif (Virion Infectivity Factor) counteracts A3G by inducing ubiquitination and proteasomal degradation of A3G protein. Vif-A3G axis therefore is a promising therapeutic target of HIV-1. Here we report the screening, synthesis and SAR studies of benzimidazole derivatives as potent inhibitors against HIV-1 replication via protecting A3G protein. Based on the steep SAR of the benzimidazole scaffold, we identified compound 14 and 26 which provided the best potency, with IC50 values of 3.45 nM and 58.03 nM respectively in the anti-HIV-1 replication assay in H9 cells. Compound 14 and 26 also afforded protective effects on A3G protein level. Both compounds have been proved to be safe in acute toxicological studies. Taken together, we suggest that these two benzimidazole derivatives can be further developed as a new category of anti-HIV-1 leads.
