title: Synthesis, in vitro and in vivo antitumor and antiviral activity of novel 1-substituted benzimidazole derivatives.
abstract: A novel series of 5-nitro-1H-benzimidazole derivatives substituted at position 1 by heterocyclic rings was synthesized. Cytotoxicity and antiviral activity of the new compounds were tested. Compound 3 was more active than doxorubicin against A-549, HCT-116 and MCF-7. However, compound 3 showed no activity against human liver carcinoma Hep G-2 cell line. Compounds 9 and 17b (E) showed potency near to doxorubicin against the four cell lines. The acute toxicity of compound 9 on liver cancer induced in rats was determined in vivo. Interestingly, it showed restoration activity of liver function and pathology towards normal as compared to the cancer-bearing rats induced by DENA. Compounds 17a (Z), 17b (E) and 18a (Z) were the most promising compounds for their antiviral activity against rotavirus Wa strain.
authors.affiliation: a Department of Chemistry of Natural and Microbial Products .
authors.forename: Yasser M
authors.initials: YM
authors.lastname: Shaker
authors.forename: Mohamed A
authors.initials: MA
authors.lastname: Omar
authors.forename: Khaled
authors.initials: K
authors.lastname: Mahmoud
authors.forename: Salwa M
authors.initials: SM
authors.lastname: Elhallouty
authors.forename: Waled M
authors.initials: WM
authors.lastname: El-Senousy
authors.forename: Mamdouh M
authors.initials: MM
authors.lastname: Ali
authors.forename: Abeer E
authors.initials: AE
authors.lastname: Mahmoud
authors.forename: Abeer H
authors.initials: AH
authors.lastname: Abdel-Halim
authors.forename: Saeed M
authors.initials: SM
authors.lastname: Soliman
authors.forename: Hoda I
authors.initials: HI
authors.lastname: El Diwani
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000998:Antiviral Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001562:Benzimidazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009374:Neoplasms, Experimental / Q000188:drug therapy / Q000473:pathology; D051381:Rats; D012401:Rotavirus / Q000187:drug effects*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D000998:Antiviral Agents; D001562:Benzimidazoles; C031000:benzimidazole
keywords: Antitumor; antiviral; benzimidazoles; cytotoxicity