• Title/Summary/Keyword: benzimidazole

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The Antitumor Potentials of Benzimidazole Anthelmintics as Repurposing Drugs

  • Deok-Soo Son;Eun-Sook Lee;Samuel E. Adunyah
    • IMMUNE NETWORK
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    • v.20 no.4
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    • pp.29.1-29.20
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    • 2020
  • The development of refractory tumor cells limits therapeutic efficacy in cancer by activating mechanisms that promote cellular proliferation, migration, invasion, metastasis, and survival. Benzimidazole anthelmintics have broad-spectrum action to remove parasites both in human and veterinary medicine. In addition to being antiparasitic agents, benzimidazole anthelmintics are known to exert anticancer activities, such as the disruption of microtubule polymerization, the induction of apoptosis, cell cycle (G2/M) arrest, anti-angiogenesis, and blockage of glucose transport. These antitumorigenic effects even extend to cancer cells resistant to approved therapies and when in combination with conventional therapeutics, enhance anticancer efficacy and hold promise as adjuvants. Above all, these anthelmintics may offer a broad, safe spectrum to treat cancer, as demonstrated by their long history of use as antiparasitic agents. The present review summarizes central literature regarding the anticancer effects of benzimidazole anthelmintics, including albendazole, parbendazole, fenbendazole, mebendazole, oxibendazole, oxfendazole, ricobendazole, and flubendazole in cancer cell lines, animal tumor models, and clinical trials. This review provides valuable information on how to improve the quality of life in patients with cancers by increasing the treatment options and decreasing side effects from conventional therapy.

Synthesis, Antinicrobial and Molluscicidal Activities of New Benzimidazole Derivatives

  • Nofal, Z.M.;Fanmy, H.H.;Mohamed, H.S.
    • Archives of Pharmacal Research
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    • v.25 no.1
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    • pp.28-38
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    • 2002
  • A series of Schiff's benzimidazole bases, thiosemicarbazides were synthesized, azole ring systems as 1,3,4-triazole, 1,3,4-oxadiazole were prepared. 1-Methylbenzimidazole incorporated to substituted dithio-carbamate, thiophenol, diethylamine via acetamido group were synthesized. A series of pyrimidinobenzimidazoles, triazinobenz-imidazoles, and 2-(acetonylamino)-1-methyl-benzimidazole were prepared. The antimicrobial and molluscicidal activities of some newly prepared compounds were carried out.

Synthesis and SAR of Benzimidazole Derivatives Containing Oxycyclic Pyridine as a Gastric $H^+/K^+$-ATPase Inhibitors

  • Jo, Seong Un;Gang, Seong Gyu;Kim, Seong Su;Jeon, Hae Gyeong;Choe, Jong Gwon;Yeom, Eul Geon
    • Bulletin of the Korean Chemical Society
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    • v.22 no.11
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    • pp.1217-1223
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    • 2001
  • A series of benzimidazole derivatives containing oxycyclic pyridine was prepared and evaluated for their gastric H+ /K+ -ATPase inhibitory activity. Several of the synthesized compound exhibited potent antisecretion in pylorus-ligated rats when administered intradoudenally. Their inhibitory activities were equivalent or comparable to omeprazole.

Reactions in Surfactant Solutions(V): Dephosphorylation of p-Nitrophenyldiphenylphosphinate by Benzimidazole Catalyzed with Ethyltri-n-octylammonium Bromide

  • 홍영석;이정근;김현묵
    • Bulletin of the Korean Chemical Society
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    • v.18 no.12
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    • pp.1260-1264
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    • 1997
  • The phase-transfer reagent (PTC), ethyl tri-n-octylammonium bromide (ETABr), strongly catalyzes the reaction of p-nitrophenyldiphenylphosphinate (p-NPDPIN) with benzimidazole (BI) and its anion (BI-). In ETABr solutions, the dephosphorylation reactions exhibit higer than first order kinetics with respect to the nucleophile, BI, and ETABr, suggesting that reactions are occuring in small aggregates of the three species including the substrate, whereas the reaction of p-NPDPIN with OH- is not catalyzed by ETABr. This behavior for the drastic rate-enhancement of the dephosphorylation is refered as 'aggregation complex model' for reactions of hydrophobic organic phosphinates with benzimidazole in hydrophobic quarternary ammonium salt solutions.

Synthesis and Study of Antibacterial and Antifungal Activities of Novel 2-[[(Benzoxazole/benzimidazole-2-yl)sulfanyl]acetylamino]thiazoles

  • Kaplancikli, Zafer-Asim;Gulhan, Turan-Zitouni;Revial, Gilbert;Guven, Kiymet
    • Archives of Pharmacal Research
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    • v.27 no.11
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    • pp.1081-1085
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    • 2004
  • Several 2-[[(benzoxazole/benzimidazole-2-yl)sulfanyl]acetylamino]thiazoles derivatives were synthesized by reacting 4-substituted-2-(chloroacetylamino)thiazoles with benzoxazole/benzimidazole-2-thioles in acetone and in the presence of $K_2CO_3$. The chemical structures of the compounds were elucidated by IR, $^1H-NMR$, and $FAB^{+}-MS$ spectral data. Their antimicrobial activities against Micrococcus luteus (NRLL B-4375), Bacillus cereus (NRRL B-3711), Proteus vulgaris (NRRL B-123), Salmonella typhimurium (NRRL B-4420), Staphylococcus aureus (NRRL B-767), Escherichia coli (NRRL B-3704), Candida albicans and Candida globrata (isolates obtained from Osmangazi Uni. Fac.of Medicine) were investigated and in this investigation, a significant level of activity was illustrated.