1r78: Difference between revisions

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==Overview==

A novel series of oxindole-type inhibitors of CDK2 that have heteroatom, substituted alkynyl moieties at their C-4 position is described. These, novel 4-alkynyl-substituted inhibitors have superior potency relative to, their parent compound in free enzyme and in cell based assays. The crystal, structure of CDK2 in complex with one of these analogues was determined, and gives insight to their increased potency. The biochemical evaluation, of a representative derivative is also described.

A novel series of oxindole-type inhibitors of CDK2 that have heteroatom substituted alkynyl moieties at their C-4 position is described. These novel 4-alkynyl-substituted inhibitors have superior potency relative to their parent compound in free enzyme and in cell based assays. The crystal structure of CDK2 in complex with one of these analogues was determined and gives insight to their increased potency. The biochemical evaluation of a representative derivative is also described.

==About this Structure==

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[[Category: Dunten, P.]]

[[Category: Kammlott, U.]]

[[Category: Luk, K.C.]]

[[Category: Luk, K C.]]

[[Category: Rowan, K.]]

[[Category: Schutt, A.]]

[[Category: Simcox, M.E.]]

[[Category: Simcox, M E.]]

[[Category: Thompson, T.]]

[[Category: FMD]]

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[[Category: serine/threonine protein kinase]]

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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 14:47:52 2008''

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@@ Line 4: / Line 4: @@
 ==Overview==
-A novel series of oxindole-type inhibitors of CDK2 that have heteroatom, substituted alkynyl moieties at their C-4 position is described. These, novel 4-alkynyl-substituted inhibitors have superior potency relative to, their parent compound in free enzyme and in cell based assays. The crystal, structure of CDK2 in complex with one of these analogues was determined, and gives insight to their increased potency. The biochemical evaluation, of a representative derivative is also described.
+A novel series of oxindole-type inhibitors of CDK2 that have heteroatom substituted alkynyl moieties at their C-4 position is described. These novel 4-alkynyl-substituted inhibitors have superior potency relative to their parent compound in free enzyme and in cell based assays. The crystal structure of CDK2 in complex with one of these analogues was determined and gives insight to their increased potency. The biochemical evaluation of a representative derivative is also described.
 ==About this Structure==
@@ Line 18: / Line 18: @@
 [[Category: Dunten, P.]]
 [[Category: Kammlott, U.]]
-[[Category: Luk, K.C.]]
+[[Category: Luk, K C.]]
 [[Category: Rowan, K.]]
 [[Category: Schutt, A.]]
-[[Category: Simcox, M.E.]]
+[[Category: Simcox, M E.]]
 [[Category: Thompson, T.]]
 [[Category: FMD]]
@@ Line 28: / Line 28: @@
 [[Category: serine/threonine protein kinase]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri Feb 15 16:47:21 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 14:47:52 2008''