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9. Synthesis of Analogues of Bis-benzimidazoles as Novel DNA Minor
Groove Binders
Y. Opoku-Boahen1* and J. Mann2
1Chemistry
Department, University of Cape Coast, Cape Coast, Ghana. Email:
yawoboahen@yahoo.com
2McClay Chair of Biological Chemistry, School of
Chemistry, Queens University of Belfast, David Keir Building,
Belfast, BT 9 5AG, N. Ireland.
Abstract:
The syntheses of three analogues of symmetric
bisbenzimidazoles, their binding to the minor groove of DNA
and cytotoxicity have been studied. The bisbenzimidazoloes
were evaluated against the anticancer drug Hoechst 33258 in
four human ovarian cancer cell lines: A2780, A2780cisR,
CHI, and SKOV-3. The compounds were cytotoxic with activity
significantly greater than that shown by the clinically used
drug Hoechst 33258. The compounds were found to bind to the
minor groove of DNA with AT sequence selectivity.
Keywords: Bisbenzimidazoles, cytotoxicity, cancer cell
lines, DNA
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