Synthesis, antitumor evaluation and DNA binding studies of novel amidino-benzimidazolyl substituted derivatives of furyl-phenyl- and thienyl-phenyl-acrylates, naphthofurans and naphthothiophenes

Novel biologically active nitro and amino substituted benzimidazo[1,2-a]quinolines

“…The growth inhibition activity was assessed as described previously [ 7,8,15,16,20 ]. The panel cell lines were inoculated onto a series of standard 96-well microtiter plates on day 0, at 1×10 4 to 3×10 4 cells/mL, depending on the doubling times of a specific cell line.…”

“…2,3,4 The benzimidazole unit which has a structural similarity with purine, is also the key building block for a variety of derivatives that are known to play crucial roles in the functions of a number of biologically important molecules. Besides, benzimidazoles represent the major backbone of numerous of synthetic medical and biochemical agents possessing different chemical and pharmacological features which impart them diverse biological properties like anticancer, 5,6,7 antiviral, 8,9 antibacterial, 10,11 antifungal, 12 antihistaminic 13 and anticonvulsant activity. 14 As a part of our continuing search for potential anticancer agents related to benzimidazole derivatives, we have recently reported on the synthesis, cytostatic evaluation, DNA/RNA interaction study and proteomic profiling of a series of amidino-substituted heterocyclic benzimidazoles and benzimidazo [1,2-a]quinolines.…”

Novel synthetic bisbenzimidazole that targets angiogenesis in Ehrlich ascites carcinoma bearing mice

“…[5][6][7] Multiple previous reports have suggested that benzimidazoles to be very good cytotoxic agents against different types of cancer cell lines. 8 Recently bisbenzimidazole conjugates have been reported to target mitochondria in cancer cells and induce their antiproliferative activity by caspase dependent apoptosis. 9 In addition, bisbenzimidazoles bind to minor groove of the DNA to instigate its anti-proliferative effect and many DNA minor groove binders have entered clinical trials in cancer treatment.…”

Synthesis of Novel 2-Butyl-1H-Benzo [4, 5] Imidazo [1, 2-A] Imidazo [4, 5-E] Pyridine-5-Carbonitrile Derivatives and Evaluation of Their Anticancer Activity

“…Therefore there is a need for new class of anticancer agents in treating the cancer. Among the other heterocyclic pharmacophores, imidazoles,pyridines and benzimidazoles are the most promising heterocyclic moieties, which have active templates in treating various diseases including various cancers [3][4][5][6][9][10][11] .…”

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AbSTRACTA series of new 2-butyl-1H-benzo [4,5]imidazo [1,2-a]imidazo [4,5-e]pyridine-5-carbonitrile derivatives were synthesized by the self cyclisation of (E)-2-(1H-benzo[d]imidazol-2-yl)-3-(2-butyl-4-chloro-1H-imidazol-5-yl)acrylonitrile in the presence of piperidine as catalyst, which in turn were prepared by the condensation of substituted N-alkyl 2-butyl-4-chloro-1H-imidazole-5-carbaldehydes with 2-cyanomethylbenzimidazole in the presence of catalytic amount of L-proline in ethanol or by using piperidine as a base. Newly synthesized compounds which incorporate a variety of N-substituent moieties were characterized by spectral data and screened for anticancer activity against MCF-7 breast cancer cell line.

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