5805-52-7Relevant academic research and scientific papers
Structure-based design of novel benzimidazole derivatives as PIN1 inhibitors
Wang, Shuxiang,Guan, Lihong,Zang, Jie,Xing, Kun,Zhang, Jian,Liu, Dan,Zhao, Linxiang
, (2019/04/08)
Peptidyl-prolyl cis/trans isomerase Pin1 plays a key role in amplifying and translating multiple oncogenic signaling pathways during oncogenesis. The blockade of Pin1 provided a unique way of disrupting multiple oncogenic pathways and inducing apoptosis. Aiming to develop potent Pin1 inhibitors, a series of benzimidazole derivatives were designed and synthesized. Among the derivatives, compounds 6h and 13g showed the most potent Pin1 inhibitory activity with IC50 values of 0.64 and 0.37 μM, respectively. In vitro antiproliferative assay demonstrated that compounds 6d, 6g, 6h, 6n, 6o and 7c exhibited moderate antiproliferative activity against human prostate cancer PC-3 cells. Taken together, these unique benzimidazole derivatives exhibited great potential to be further explored as potent Pin1 inhibitors with improved potency.
1,2-dis-substituted benzimidazole derivative and application thereof
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Paragraph 0133-0135, (2017/07/19)
The invention belongs to the technical field of medicines, and particularly relates to a 1,2-dis-substituted benzimidazole derivative and pharmaceutically acceptable salt thereof, a preparation method of the derivative, a medicine composition with the derivative serving as an active component, and application of the derivative in preparation of a Pin1 inhibitor and preparation of a medicine for treating and/or preventing various cancers. The 1,2-dis-substituted benzimidazole derivative and the pharmaceutically acceptable salt thereof are as shown in the general formula I, and definitions of all substituents are described in claims and the specification. (Refer to Specification).
18 beta-glycyrrhetinic acid derivative and application thereof
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Paragraph 0132; 0133; 0134, (2017/09/18)
The invention relates to the technical field of medicines, in particular to an 18 beta-glycyrrhetinic acid derivative with Pin1 inhibitory activity and pharmacologically-acceptable salt thereof, a preparation method of the derivative, a pharmaceutical composition taking the derivative as an active ingredient and application of the derivative to the preparation of a Pin1 inhibitor and the preparation of a drug for treating and/or preventing various cancers. The derivative shown in a general formula I or the pharmacologically-acceptable salt thereof has the following structure, wherein R, X, Y and n are stated in the claims and the descriptions.
Phototransformation of benzimidazole and thiabendazole inside cucurbit[8]uril
Smitka, Jaroslav,Lemos, Americo,Porel, Mintu,Jockusch, Steffen,Belderrain, Tomas R.,Tesarova, Eva,Da Silva, Jose P.
, p. 310 - 315 (2014/02/14)
The phototransformation of benzimidazole (BZ) and of the benzimidazole pesticide thiabendazole (TBZ) was investigated in aqueous solution in the absence and presence of the supramolecular host cucurbit[8]uril (CB8). ESI-MS and NMR reveal that both compoun
Photochemistry, of Heterocyclics. III. Photolysis of Various 2-Substituted Benzimidazoles
Crank, George,Mursyidi, Achmad
, p. 775 - 784 (2007/10/02)
A variety of 2-substituted benzimidazoles have been irradiated with ultraviolet light to determine the effects of substituents on the photochemical behaviour of the benzimidazole ring system.Benzimidazol-2-amine gave -2'amine and -2'-amine, showing that this derivative behaves in the same way as benzimidazole. 2-Chlorobenzimidazole loses chlorine forming a dimeric species and benzimidazol-2(3H)-one, which is itself inert to photolysis. 2-Trichloromethylbenzimidazole also loses chlorine to form a variety of products depending on the solvent. 2-Trifluoromethylbenzimidazole does not lose fluorine but forms a dimer and also undergoes imidazole ring cleavage.Benzimidazole-2-thiol also undergoes imidazole ring cleavage with loss of sulfur.The 2-phenyl group stabilizes the benzimidazole ring system to photolysis as does the 2-thiazolyl group; however, the latter suffers thiazole ring cleavage.
