DNA Binding Compounds. VII. Synthesis, Characterization and DNA Binding Capacity of 1,2-Dicarba-closo-dodecaborane Bibenzimidazoles Related to the DNA Minor Groove Binder Hoechst 33258

1999 ◽  
Vol 52 (4) ◽  
pp. 291 ◽  
Author(s):  
Stuart A. Bateman ◽  
David P. Kelly ◽  
Jonathan M. White ◽  
Roger F. Martin

A series of bibenzimidazole derivatives based on the known DNA minor groove binder Hoechst 33258 have been prepared to include a 1,2-dicarba-closo-dodecaborane cage for potential use in boron neutron capture therapy (BNCT). The carborane derivatives (5){(7) were chosen to reduce the steric inhibition of minor groove DNA binding displayed by the previously prepared carborane ligand (4). The synthesis and preliminary DNA binding studies of these bibenzimidazole derivatives are presented herein.

1998 ◽  
Vol 51 (3) ◽  
pp. 243 ◽  
Author(s):  
Christopher I. Clark ◽  
David P. Kelly ◽  
Roger F. Martin ◽  
Jonathan M. White ◽  
Pavel Lobachevsky

2-[2′-(4′′-Ethoxyphenyl)-1H-indol-6′-yl]-5-(4′′′-methylpiperazin-1′′′-yl)-1H-benzimidazole (1) has been synthesized from 2-(4′-ethoxyphenyl)-1H-indole-6-carbaldehyde (4b) and 4-(4′-methylpiperazin-1′-yl)benzene-1,2-diamine (3b). The aldehyde (4b) was prepared in five steps by using a modified Leimgruber–Batcho indole synthesis. Evaluation of (1) as a DNA ligand is described.


2009 ◽  
Vol 57 (5) ◽  
pp. 481-486 ◽  
Author(s):  
Himanshu Ojha ◽  
Bhaskar Mohan Murari ◽  
Sneh Anand ◽  
Mohd Imtaiyaz Hassan ◽  
Faizan Ahmad ◽  
...  

ChemInform ◽  
2010 ◽  
Vol 28 (18) ◽  
pp. no-no
Author(s):  
S. FRAU ◽  
J. BERNADOU ◽  
B. MEUNIER

1994 ◽  
Vol 47 (2) ◽  
pp. 247 ◽  
Author(s):  
DP Kelly ◽  
SA Bateman ◽  
RF Martin ◽  
ME Reum ◽  
M Rose ◽  
...  

The synthesis and characterization of four novel boron-containing bibenzimidazoles related to the DNA minor groove binder Hoechst 33258 are reported. Such compounds, particularly their 1�B-enriched forms, have potential as agents for boron neutron capture therapy which is used in the treatment of cancers.


2015 ◽  
Vol 2 (2) ◽  
pp. 41
Author(s):  
G. A. Belitsky ◽  
K. I. Kirsanov ◽  
E. A. Lesovaya ◽  
M. G. Yakubovskaya

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