134903-48-3Relevant articles and documents
Synthesis, antimycobacterial and anticancer activity of novel indole-based thiosemicarbazones
Mashayekhi, Vida,Haj Mohammad Ebrahim Tehrani, Kamaleddin,Azerang, Parisa,Sardari, Soroush,Kobarfard, Farzad
, (2021/09/08)
Based on the structural elements of bioactive indole-based compounds, a series of novel 1-substituted indole-3-carboxaldehyde thiosemicarbazones were synthesized as potential antimycobacterial and anticancer agents. The derivatives were prepared via a two
B-ring modified aurones as promising allosteric inhibitors of hepatitis C virus RNA-dependent RNA polymerase
Meguellati, Amel,Ahmed-Belkacem, Abdelhakim,Yi, Wei,Haudecoeur, Romain,Crouillère, Marie,Brillet, Rozenn,Pawlotsky, Jean-Michel,Boumendjel, Ahcène,Peuchmaur, Marine
, p. 579 - 592 (2014/06/09)
Following our recent report showing the potential of naturally occurring aurones (2-benzylidenebenzofuran-3(2H)-ones) as anti-hepatitis C virus (HCV) agents, efforts were continued in order to refine the structural requirements for the inhibitory effect on HCV RNA-dependent RNA polymerase (RdRp). In this study, we targeted the B-ring moiety of aurones with the aim to improve structural features associated with higher inhibition of the targeted polymerase. In vitro evaluation of the RdRp inhibitory activity of the 37 newly synthesized compounds pointed out that the replacement of the B-ring with an N-substituted indole moiety induced the highest inhibitory effect. Of these, compounds 31, 40 and 41 were found to be the most active (IC50 = 2.3-2.4 μM). Docking experiments performed with the most active compounds revealed that the allosteric thumb pocket I of RdRp is the binding pocket for aurone analogues.
Intramolecular photochemical cross-coupling reactions of 3-acyl-2-haloindoles and 2-chloropyrrole-3-carbaldehydes with substituted benzenes
Lu, Shen-Ci,Zhang, Xi-Xia,Shi, Zong-Jun,Ren, Yu-Wei,Li, Bing,Zhang, Wei
supporting information; experimental part, p. 2839 - 2844 (2010/03/24)
Highly efficient syntheses of indolo[2,1-a]isoquinolines, indolo[2,1-a][2]benzazepines, pyrrolo[2,1-a]isoquinolines and pyrrolo[1,2-a]benzazepines in excellent yields have been achieved by the intramolecular photochemical cross-coupling reactions of 3-acyl-2-halo-N- (ω-arylalkyl)indoles and 2-chloro-N-(ω-arylalkyl)pyrrole-3- carbaldehydes in acetone. A new heterocyclic ring system - pyrrolo[1,2-d][1,4] benzoxazepine - has also been constructed for the first time in this work by the photocyclization of 2-chloro-N-(2-phenoxyethyl)pyrrole-3-carbaldehyde.