Human cancer inhibitory pentapeptide methyl esters

• US 5,504,191 A
• Filed: 08/01/1994
• Issued: 04/02/1996
• Est. Priority Date: 08/01/1994
• Status: Expired due to Fees

• Current Assignee: Arizona Board of Regents (University of Arizona)
• Original Assignee: Arizona Board of Regents (University of Arizona)
• Inventors: Williams, Michael D., Pettit, George R., Srirangam, Jayaram K.
• Primary Examiner(s): Schain, Howard E.
• Assistant Examiner(s): HUFF, SHEELA JITENDRA
• Application Number:
  US08/283,682
• Time in Patent Office: 610 Days
• Field of Search: 530/330, 514/17
• US Class Current: 530/330
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: C07K 5/0205 containing the structure -NH-(X)3-C(=0)-, e.g. statine or derivatives thereof

Abstract

Herein disclosed are several pentapeptide methyl ester derivatives of dolatin 10, using both naturally occurring and modified amino acids. The selected modified amino acids are constituents of dolastatin 10 which is a structurally distinct peptide with excellent in vitro and in vivo antineoplastic activity. The structures of these compounds are as shown below: ##STR1##

Claims

1. A composition of matter having the general structure shown below wherein:

##STR4## R is selected from the group consisting of the substituents shown above, R₁ is selected from the group consisting of the substituents shown above, and R.sub. 2 is selected from the group consisting of the substituents shown above.

2. A composition of matter according to claim 1 designated herein as compound "10a".

3. A composition of matter according to claim 1 designated herein as compound "10b".

4. A composition of matter according to claim 1 designated herein as compound "11a."

5. A composition of matter according to claim 1 designated herein as compound "11b."

6. A composition of matter according to claim 1 designated herein as compound "11c."