96103-60-5Relevant academic research and scientific papers
Kinetic Target-Guided Synthesis of Small-Molecule G-Quadruplex Stabilizers
Dobia?, Juraj,Dvo?áková, Hana,Hubálek, Martin,Kozák, Jaroslav,Pomeislová, Alice,Reyes-Gutiérrez, Paul E.,Teply, Filip,Veverka, Václav,Vrzal, Luká?
, p. 1236 - 1250 (2020/12/31)
The formation of a G-quadruplex motif in the promoter region of the c-MYC protooncogene prevents its expression. Accordingly, G-quadruplex stabilization by a suitable ligand may be a viable approach for anticancer therapy. In our study, we used the 4-(4-m
N-aryl-2-aminobenzimidazoles: Novel, efficacious, antimalarial lead compounds
Ramachandran, Sreekanth,Hameed P., Shahul,Srivastava, Abhishek,Shanbhag, Gajanan,Morayya, Sapna,Rautela, Nikhil,Awasthy, Disha,Kavanagh, Stefan,Bharath, Sowmya,Reddy, Jitendar,Panduga, Vijender,Prabhakar,Saralaya, Ramanatha,Nanduri, Robert,Raichurkar, Anandkumar,Menasinakai, Sreenivasaiah,Achar, Vijayashree,Jiménez-Díaz, María Belén,Martínez, María Santos,Angulo-Barturen, I?igo,Ferrer, Santiago,Sanz, Laura María,Gamo, Francisco Javier,Duffy, Sandra,Avery, Vicky M.,Waterson, David,Lee, Marcus C. S.,Coburn-Flynn, Olivia,Fidock, David A.,Iyer, Pravin S.,Narayanan, Shridhar,Hosagrahara, Vinayak,Sambandamurthy, Vasan K.
, p. 6642 - 6652 (2014/10/15)
From the phenotypic screening of the AstraZeneca corporate compound collection, N-aryl-2-aminobenzimidazoles have emerged as novel hits against the asexual blood stage of Plasmodium falciparum (Pf). Medicinal chemistry optimization of the potency against Pf and ADME properties resulted in the identification of 12 as a lead molecule. Compound 12 was efficacious in the P. berghei (Pb) model of malaria. This compound displayed an excellent pharmacokinetic profile with a long half-life (19 h) in rat blood. This profile led to an extended survival of animals for over 30 days following a dose of 50 mg/kg in the Pb malaria model. Compound 12 retains its potency against a panel of Pf isolates with known mechanisms of resistance. The fast killing observed in the in vitro parasite reduction ratio (PRR) assay coupled with the extended survival highlights the promise of this novel chemical class for the treatment of malaria.
Benzimidazole derivatives as new serotonin 5-HT6 receptor antagonists. Molecular mechanisms of receptor inactivation
De La Fuente, Tania,Martín-Fontecha, Mar,Sallander, Jessica,Benhamú, Bellinda,Campillo, Mercedes,Medina, Rocío A.,Pellissier, Lucie P.,Claeysen, Sylvie,Dumuis, Aline,Pardo, Leonardo,López-Rodríguez, María L.
experimental part, p. 1357 - 1369 (2010/08/20)
On the basis of our previously described pharmacophore model for serotonin 5-HT6 receptor (5-HT6R) antagonists, we have designed, synthesized, and pharmacologically characterized a series of benzimidazole derivatives 1-20 that repres
CELL TARGETING CONJUGATES
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Page/Page column 43-44, (2008/06/13)
The present invention relates to cell targeting conjugates and in particular, but not exclusively, to methods of their use in selectively eliminating and in selectively imaging target cells. The invention also relates to processes for production of the conjugates and to intermediate compounds that may be used in production of a specific class of cell targeting conjugates. In one embodiment there is provided a cell targeting conjugate comprising the following components that are covalently conjugated via a linker that is degradable within the target cells: i) a DNA minor groove binding ligand incorporating an effective Auger electron-emitting and/or gamma-emitting and/or positron-emitting atom or photoactive moiety; ii) a target cell specific protein or peptide that is capable of internalisation by target cells.
DERIVATIVES OF 5(6)-AMINOBENZIMIDAZOLE
Kuznetsov, V. A.,Garabadzhiu, A. V.,Ginzburg, O. F.
, p. 576 - 580 (2007/10/02)
A series of triamines were obtained by the amination of 2-nitro-5-chloroaminobenzene and reduction of the obtained compounds.In reaction with the esters of aromatic acids the products were converted into derivatives of 5(6)-aminobenzimidazole.
