146552-66-1Relevant articles and documents
Solution-Phase Synthesis of Backbone-Constrained Cationic Peptoid Hexamers with Antibacterial and Anti-Biofilm Activities
Charbonnel, Nicolas,Faure, Sophie,Forestier, Christiane,Roy, Olivier,Shyam, Radhe,Taillefumier, Claude
supporting information, p. 5813 - 5822 (2021/11/17)
Abstract: Submonomer synthesis in solution and block-coupling protocols were combined to prepare amphiphilic peptoid hexamers. The amphipathic character arises from the use of hydrophobic aliphatic tert-butyl side-chains imposing the cis-amide backbone co
Design, synthesis and anticancer profile of new 4-(1H-benzo[d]imidazol-1-yl)pyrimidin-2-amine-linked sulfonamide derivatives with V600EBRAF inhibitory effect
Abdel-Maksoud, Mohammed S.,Mohamed, Ahmed A. B.,Hassan, Rasha M.,Abdelgawad, Mohamed A.,Chilingaryan, Garri,Selim, Samy,Abdel-Bakky, Mohamed S.,Al-Sanea, Mohammad M.
, (2021/10/01)
A new series of 4-(1H-benzo[d]imidazol-1-yl)pyrimidin-2-amine linked sulfonamide derivatives 12a–n was designed and synthesized according to the structure of well-established V600EBRAF inhibitors. The terminal sulfonamide moiety was linked to the pyrimidine ring via either ethylamine or propylamine bridge. The designed series was tested at fixed concentration (1 μM) against V600EBRAF, finding that 12e, 12i and 12l exhibited the strongest inhibitory activity among all target compounds and 12l had the lowest IC50 of 0.49 μM. They were further screened on NCI 60 cancer cell lines to reveal that 12e showed the most significant growth inhibition against multiple cancer cell lines. Therefore, cell cycle analysis of 12e was conducted to investigate the effect on cell cycle progression. Finally, virtual docking studies was performed to gain insights for the plausible binding modes of vemurafenib, 12i, 12e and 12l.
Imidazothiazole-based potent inhibitors of V600E-B-RAF kinase with promising anti-melanoma activity: biological and computational studies
Anbar, Hanan S.,El-Gamal, Mohammed I.,Jeon, Hong R.,Kwon, Dow,Lee, Bong S.,Oh, Chang-Hyun,Tarazi, Hamadeh
, p. 1712 - 1726 (2020/10/02)
A series of imidazothiazole derivatives possessing potential activity against melanoma cells were investigated for molecular mechanism of action. The target compounds were tested against V600E-B-RAF and RAF1 kinases. Compound 1zb is the most potent agains
