2cct: Difference between revisions

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[[Image:2cct.~~gif~~|left|200px]]

[[Image:2cct.png|left|200px]]

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~~'''~~HUMAN HSP90 WITH 5-(5-CHLORO-2,4-DIHYDROXY-PHENYL)-4-PIPERAZIN-1-YL-2H-PYRAZOLE-3-CARBOXYLIC ACID ETHYLAMIDE~~'''~~

===HUMAN HSP90 WITH 5-(5-CHLORO-2,4-DIHYDROXY-PHENYL)-4-PIPERAZIN-1-YL-2H-PYRAZOLE-3-CARBOXYLIC ACID ETHYLAMIDE===

~~==Overview==~~

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~~Novel piperazinyl~~, ~~morpholino and piperidyl derivatives of the pyrazole-based Hsp90 inhibitor CCT018159 are described. Structure-activity relationships have been elucidated by X-ray co-crystal analysis of~~ the ~~new compounds bound~~ to the ~~N-terminal domain of human Hsp90~~. ~~Key features of the binding mode are essentially identical to the recently reported potent analogue VER-49009~~. ~~The most potent of the new compounds has a methylsulfonylbenzyl substituent appended to the piperazine nitrogen~~, ~~possesses an IC50 of less than 600 nM binding against~~ the ~~enzyme and demonstrates low micromolar inhibition of tumour cell proliferation~~.

The line below this paragraph, {{ABSTRACT_PUBMED_16480864}}, adds the Publication Abstract to the page

(as it appears on PubMed at http://www.pubmed.gov), where 16480864 is the PubMed ID number.

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==About this Structure==

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[[Category: Phosphorylation]]

[[Category: Pyrazole]]

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on ~~Sat May 3 21~~:49:51 2008''

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 16:54:27 2008''

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-[[Image:2cct.gif|left|200px]]
+{{Seed}}
+[[Image:2cct.png|left|200px]]
 <!--
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 {{STRUCTURE_2cct|  PDB=2cct  |  SCENE=  }}
-'''HUMAN HSP90 WITH 5-(5-CHLORO-2,4-DIHYDROXY-PHENYL)-4-PIPERAZIN-1-YL-2H-PYRAZOLE-3-CARBOXYLIC ACID ETHYLAMIDE'''
+===HUMAN HSP90 WITH 5-(5-CHLORO-2,4-DIHYDROXY-PHENYL)-4-PIPERAZIN-1-YL-2H-PYRAZOLE-3-CARBOXYLIC ACID ETHYLAMIDE===
-==Overview==
+<!--
-Novel piperazinyl, morpholino and piperidyl derivatives of the pyrazole-based Hsp90 inhibitor CCT018159 are described. Structure-activity relationships have been elucidated by X-ray co-crystal analysis of the new compounds bound to the N-terminal domain of human Hsp90. Key features of the binding mode are essentially identical to the recently reported potent analogue VER-49009. The most potent of the new compounds has a methylsulfonylbenzyl substituent appended to the piperazine nitrogen, possesses an IC50 of less than 600 nM binding against the enzyme and demonstrates low micromolar inhibition of tumour cell proliferation.
+The line below this paragraph, {{ABSTRACT_PUBMED_16480864}}, adds the Publication Abstract to the page
+(as it appears on PubMed at http://www.pubmed.gov), where 16480864 is the PubMed ID number.
+-->
+{{ABSTRACT_PUBMED_16480864}}
 ==About this Structure==
@@ Line 44: / Line 48: @@
 [[Category: Phosphorylation]]
 [[Category: Pyrazole]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May  3 21:49:51 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 16:54:27 2008''