19018-24-7Relevant articles and documents
Design and structure-activity relationships anticandidosic of diazaheteroaryl functionalized by Micha?l acceptors
Aboudramane, Kone,Doumade, Zon,Drissa, Sissouma,Jean-Paul, N'Guessan D.,Mahama, Ouattara,Mamidou, Koné Witabouna,Songuigama, Coulibaly
, p. 117 - 133 (2022/02/14)
Benzimidazole and imidazopyridine heterocycles associated with Micha?l acceptors have shown strong anticandidosic potential in our previous work. After a decade of research, we have designed, synthesized and evaluated the anticandidosic activities of seve
Preparation method of thiabendazole intermediate
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Paragraph 0034-0035, (2020/12/31)
The invention provides a preparation method of a thiabendazole intermediate. The method uses a raw material containing o-phenylenediamine to prepare the thiabendazole intermediate shown as a formula (1), and comprises the following steps: in an acidic environment, carrying out condensation reaction on the raw material containing o-phenylenediamine to obtain a crude product 1; carrying out halogenation reaction on the crude product 1 to obtain a crude product 2; and carrying out decarboxylation reaction on the crude product 2, and purifying to obtain the thiabendazole intermediate. According tothe invention, the method is low in raw material cost, simple in synthetic route, inapplicable to catalysts, recyclable in solvent, almost zero in emission of three wastes, mild in reaction condition, simple to operate and suitable for modern industrial production, and the influence on the environment is avoided, and the yield is as high as 80% or above. R is Cl or Br.
Design, synthesis, and biological evaluation of aromatic amide-substituted benzimidazole-derived chalcones. The effect of upregulating TP53 protein expression
Han, Chun,Jing, Xiaobi,Li, Mengyao,Su, Feng,Wang, Zhijun,Wu, Lintao,Wu, Xi,Yang, Yuting
, (2020/03/17)
A series of benzimidazole-derived chalcones containing aromatic amide substituent were designed and synthesized. All of the chalcone compounds were tested for their in vitro antitumor activity against human cancer cell lines (HCT116, HepG2, A549, and CRL-5908). The antiproliferative activity of compounds 3, 6, 9, 14, 15, 16 against HCT116 cells was significantly better than that that of 5-Fluorouracil (IC50: 94.63 μM). The antitumor activity of these compounds showed obvious differences between the wild type HCT116 and mutant HCT116 (TP53-/-) cells. A preliminary mechanistic study suggested that these compounds act by upregulating the expression of TP53 protein in tumor cells without inhibiting the MDM2-TP53 interaction.