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1ftd

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[[Image:1ftd.gif|left|200px]]
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{{Seed}}
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{{STRUCTURE_1ftd| PDB=1ftd | SCENE= }}
{{STRUCTURE_1ftd| PDB=1ftd | SCENE= }}
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'''5'-D(*CP*GP*CP*GP*AP*AP*TP*TP*CP*GP*CP*G)-3'-SYMMETRIC BIS-BENZIMIDAZOLE COMPLEX'''
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===5'-D(*CP*GP*CP*GP*AP*AP*TP*TP*CP*GP*CP*G)-3'-SYMMETRIC BIS-BENZIMIDAZOLE COMPLEX===
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==Overview==
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The synthesis and evaluation of the novel head-to-head bisbenzimidazole compound 2,2-bis[4'-(3' '-dimethylamino-1' '-propyloxy)phenyl]-5,5-bi-1H-benzimidazole is described. An X-ray crystallographic study of a complex with the DNA dodecanucleotide sequence d(CGCGAATTCGCG) shows the compound bound in the A/T minor groove region of a B-DNA duplex and that the head-to-head bisbenzimidazole motif hydrogen-bonds to the edges of all four consecutive A:T base pairs. The compound showed potent growth inhibition with a mean IC(50) across an ovarian carcinoma cell line panel of 0.31 microM, with no significant cross-resistance in two acquired cisplatin-resistant cell lines and a low level of cross-resistance in the P-glycoprotein overexpressing acquired doxorubicin-resistant cell line. Studies with the hollow fiber assay and in vivo tumor xenografts showed some evidence of antitumor activity.
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The line below this paragraph, {{ABSTRACT_PUBMED_11170623}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 11170623 is the PubMed ID number.
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{{ABSTRACT_PUBMED_11170623}}
==About this Structure==
==About this Structure==
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[[Category: Parkinson, G.]]
[[Category: Parkinson, G.]]
[[Category: Minor groove binding]]
[[Category: Minor groove binding]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 16:44:34 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 1 03:55:11 2008''

Revision as of 00:55, 1 July 2008

Image:1ftd.png

Template:STRUCTURE 1ftd

5'-D(*CP*GP*CP*GP*AP*AP*TP*TP*CP*GP*CP*G)-3'-SYMMETRIC BIS-BENZIMIDAZOLE COMPLEX

Template:ABSTRACT PUBMED 11170623

About this Structure

Full crystallographic information is available from OCA.

Reference

A new class of symmetric bisbenzimidazole-based DNA minor groove-binding agents showing antitumor activity., Mann J, Baron A, Opoku-Boahen Y, Johansson E, Parkinson G, Kelland LR, Neidle S, J Med Chem. 2001 Jan 18;44(2):138-44. PMID:11170623

Page seeded by OCA on Tue Jul 1 03:55:11 2008

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