1ftd: Difference between revisions

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[[Image:1ftd.~~gif~~|left|200px]]

[[Image:1ftd.png|left|200px]]

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

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

~~==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.~~

The line below this paragraph, {{ABSTRACT_PUBMED_11170623}}, adds the Publication Abstract to the page

(as it appears on PubMed at http://www.pubmed.gov), where 11170623 is the PubMed ID number.

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==About this Structure==

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[[Category: Parkinson, G.]]

[[Category: Minor groove binding]]

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on ~~Fri May~~ ~~2 16~~:44:34 2008''

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 1 03:55:11 2008''

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-[[Image:1ftd.gif|left|200px]]
+{{Seed}}
+[[Image:1ftd.png|left|200px]]
 <!--
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 {{STRUCTURE_1ftd|  PDB=1ftd  |  SCENE=  }}
-'''5'-D(*CP*GP*CP*GP*AP*AP*TP*TP*CP*GP*CP*G)-3'-SYMMETRIC BIS-BENZIMIDAZOLE COMPLEX'''
+===5'-D(*CP*GP*CP*GP*AP*AP*TP*TP*CP*GP*CP*G)-3'-SYMMETRIC BIS-BENZIMIDAZOLE COMPLEX===
-==Overview==
+<!--
-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.
+The line below this paragraph, {{ABSTRACT_PUBMED_11170623}}, adds the Publication Abstract to the page
+(as it appears on PubMed at http://www.pubmed.gov), where 11170623 is the PubMed ID number.
+-->
+{{ABSTRACT_PUBMED_11170623}}
 ==About this Structure==
@@ Line 28: / Line 32: @@
 [[Category: Parkinson, G.]]
 [[Category: Minor groove binding]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May  2 16:44:34 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul  1 03:55:11 2008''