Literature DB >> 7658451

Synthesis and evaluation of terbenzimidazoles as topoisomerase I inhibitors.

Q Sun1, B Gatto, C Yu, A Liu, L F Liu, E J LaVoie.   

Abstract

The synthesis and pharmacological activity of a series of terbenzimidazoles are described. The ability of these derivatives to induce DNA cleavage in the presence of topoisomerase I was evaluated in vitro. These analogs were also assayed for their cytotoxicity in RPMI 8402 cells and the camptothecin-resistant CPT-K5 cells. In addition the potential for these compounds to serve as substrates for MDR1 was also determined. Several terbenzimidazoles exhibited similar cytotoxicity against variants of human tumor cells that either overexpress MDR1 or are camptothecin-resistant.

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Year:  1995        PMID： 7658451     DOI： 10.1021/jm00018a024

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  6 in total

1.  A terbenzimidazole that preferentially binds and conformationally alters structurally distinct DNA duplex domains: a potential mechanism for topoisomerase I poisoning.

Authors:  D S Pilch; Z Xu; Q Sun; E J LaVoie; L F Liu; K J Breslauer
Journal:  Proc Natl Acad Sci U S A       Date:  1997-12-09       Impact factor: 11.205

2.  Topoisomerase I-mediated DNA cleavage induced by the minor groove-directed binding of bibenzimidazoles to a distal site.

Authors:  Qasim A Khan; Daniel S Pilch
Journal:  J Mol Biol       Date:  2006-10-13       Impact factor: 5.469

3.  Primary anti-proliferative activity evaluation of 1-(quinolizidin-1'-yl)methyl- and 1-(ω-tert-amino)alkyl-substituted 2-phenyl-, 2-benzyl- and 2-[(benzotriazol-1/2-yl)methyl]benzimidazoles on human cancer cell lines.

Authors:  Michele Tonelli; Bruno Tasso; Lorenzo Mina; Giuseppe Paglietti; Vito Boido; Fabio Sparatore
Journal:  Mol Divers       Date:  2013-04-13       Impact factor: 2.943

4.  3,4-dimethoxyphenyl bis-benzimidazole, a novel DNA topoisomerase inhibitor that preferentially targets Escherichia coli topoisomerase I.

Authors:  Sandhya Bansal; Devapriya Sinha; Manish Singh; Bokun Cheng; Yuk-Ching Tse-Dinh; Vibha Tandon
Journal:  J Antimicrob Chemother       Date:  2012-09-03       Impact factor: 5.790

5.  Molecular characterization of recombinant Pneumocystis carinii topoisomerase I: differential interactions with human topoisomerase I poisons and pentamidine.

Authors:  Rukiyah T van Dross; Marilyn M Sanders
Journal:  Antimicrob Agents Chemother       Date:  2002-07       Impact factor: 5.191

6.  Preparation of Tyrian purple (6,6'-dibromoindigo): past and present.

Authors:  Joel L Wolk; Aryeh A Frimer
Journal:  Molecules       Date:  2010-08-10       Impact factor: 4.411
  6 in total

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