4857-06-1Relevant articles and documents
Design, Synthesis, Cytotoxicity, and Molecular Docking Studies of New Benzimidazole Hybrids as Possible Anticancer Agents
Mishra, Shashank Shekher,Sharma, C. S.
, p. 21 - 29 (2021/08/12)
In the course of efforts to develop new anticancer agents, benzimidazole-based morpholine, thiomorpholine, and piperazine hybrid compounds were designed and synthesized. The structures of the synthesized compounds were confirmed by Proton nuclear magnetic resonance, Carbon-13 NMR, and mass spectroscopy. The title compounds were screened for cytotoxicity against breast and lung cancer cell lines. Compound 6c was found most active against lung cancer cell line with IC50 value of 2.11 μM and compound 10c was found most active against breast cancer cell line with IC50 of 2.23 μM. The molecular docking analysis was also carried out to explore binding pattern of compound with the target protein. All synthesized compounds showed excellent binding affinity toward target protein. Therefore, these findings will be helpful in future drug design of more potent anticancer agents.
Substituted benzimidazoles as modulators of Ras signaling
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Page/Page column 103-104, (2019/12/25)
Benzimidazole compounds that increase the rate of SOS-mediated nucleotide exchange on Ras by binding to a functionally relevant, chemically tractable pocket on the SOS protein, as part of the Ras:SOS:Ras complex.
From Cells to Mice to Target: Characterization of NEU-1053 (SB-443342) and Its Analogues for Treatment of Human African Trypanosomiasis
Devine, William G.,Diaz-Gonzalez, Rosario,Ceballos-Perez, Gloria,Rojas, Domingo,Satoh, Takashi,Tear, Westley,Ranade, Ranae M.,Barros-álvarez, Ximena,Hol, Wim G. J.,Buckner, Frederick S.,Navarro, Miguel,Pollastri, Michael P.
, p. 225 - 236 (2017/04/21)
Human African trypanosomiasis is a neglected tropical disease that is lethal if left untreated. Existing therapeutics have limited efficacy and severe associated toxicities. 2-(2-(((3-((1H-Benzo[d]imidazol-2-yl)amino)propyl)amino)methyl)-4,6-dichloro-1H-indol-1-yl)ethan-1-ol (NEU-1053) has recently been identified from a high-throughput screen of >42,000 compounds as a highly potent and fast-acting trypanocidal agent capable of curing a bloodstream infection of Trypanosoma brucei in mice. We have designed a library of analogues to probe the structure-activity relationship and improve the predicted central nervous system (CNS) exposure of NEU-1053. We report the activity of these inhibitors of T. brucei, the efficacy of NEU-1053 in a murine CNS model of infection, and identification of the target of NEU-1053 via X-ray crystallography.