428853-17-2Relevant academic research and scientific papers
Discovery of new potent protein arginine methyltransferase 5 (PRMT5) inhibitors by assembly of key pharmacophores from known inhibitors
Zhu, Kongkai,Song, Jia-Li,Tao, Hong-Rui,Cheng, Zhi-Qiang,Jiang, Cheng-Shi,Zhang, Hua
supporting information, p. 3693 - 3699 (2018/10/24)
Protein arginine methyltransferase 5 (PRMT5) is an epigenetics related enzyme that has been validated as a promising therapeutic target for human cancer. Up to now, two small molecule PRMT5 inhibitors has been put into phase I clinical trial. In the prese
Synthesis, evaluation and molecular modelling studies of some novel 3-(3,4-dihydroisoquinolin-2(1H)-yl)-N-(substitutedphenyl)propanamides as HIV-1 non-nucleoside reverse transcriptase inhibitors
Murugesan,Ganguly, Swastika,Maga, Giovanni
experimental part, p. 169 - 176 (2010/11/17)
A novel series of fifteen 3-(3,4-dihydroisoquinolin-2(1H)-yl)-N- (substituted phenyl) propanamides 3(a-o) were synthesized by reacting the corresponding 3-chloro-N-(aryl) propanamides 2(a-o) with 1,2,3,4- tetrahydroisoquinoline 1 in acetonitrile. The compounds have been characterized on the basis of elemental analysis and spectral data. All the compounds were evaluated for their HIV-1 RT inhibitory activity. Among the synthesized compounds, 3-(3,4-dihydroisoquinolin-2(1H)-yl)-N-o-tolyl propanamide 3d and 3-(3,4-dihydroisoquinolin-2(1H)-yl)-N-(2,4,6-tribromophenyl)propanamide 3f were identified as significant inhibitors of HIV-1 reverse transcriptase with 56% and 43% residual RT activity respectively at the final concentration of 40 μM when compared with the standard drug Efavirenz. Docking studies with HIV-1 RT (PDB ID 1rt2) were also performed in order to investigate the binding pattern of these compounds. Indian Academy of Sciences.
