Phosphatase inhibitors and methods of use thereof
AssigneeUniversity of Pittsburgh
InventorsJohn S. Lazo, Robert L. Rice, April Cunningham, Peter Wipf
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Abstract
The present invention is directed to compounds having the formula: ##STR1## The invention further provides a method of making the compounds. The compounds are useful as inhibitors of protein phosphatases, for example PP1, PP2A, PP3, CDC25A and CDC25B. The invention is further directed to a method of inhibiting a protein phosphatase, a method of inhibiting cell proliferation, and pharmaceutical compositions comprising the subject compounds.
Claims6
A method of making a compound having the formula I ##STR9## comprising in order the steps of:
- (a) coupling a diprotected glutamate to a solid support;
- (b) deprotecting the glutamate amino-terminus;
- (c) adding R'" COX, wherein X is a leaving group;
- (d) deprotecting the glutamate carboxy terminus;
- (e) adding diamine having the formula A--NHCH.sub.2 CH.sub.2 NH(R"), wherein A is a protecting group, and a coupling agent;
- (f) deprotecting the amino-terminus of said diamine;
- (g) adding ##STR10## (h) cleaving the resulting compound from the solid support.
A method of making a compound having the formula I ##STR11## comprising in order the steps of:
- (a) coupling diprotected glutamate to a solid support;
- (b) deprotecting the glutamate amino-terminus;
- (c) distributing the solid support to multiple vessels;
- (d) adding R'" COX, wherein X is a leaving group, to each vessel;
- (e) deprotecting the glutamate carboxyl terminus;
- (f) distributing the solid support to additional multiple vessels;
- (g) adding diamine having the formula A--NHCH.sub.2 CH.sub.2 NH(R"), wherein A is a protecting group, and a coupling agent to each vessel;
- (h) deprotecting the amino terminus of said diamine;
- (i) distributing the solid support to additional multiple vessels;
- (j) adding ##STR12## (k) cleaving the resulting compound from the solid support.
Dependencies are inferred from the claim text.