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US 5,663,149 AGranted
Human cancer inhibitory pentapeptide heterocyclic and halophenyl amides
AssigneeArizona Board of Regents acting on behalf of Arizona State University
InventorsGeorge R. Pettit, Jayaram K. Srirangam, Darko Kantoci
Life of this patent
Estimating the term…
Abstract
The synthesis and elucidation of nineteen heterocyclic or halophenyl amide erivatives of dolastatin 10 are disclosed. These compounds and the methods of producing those compounds offer demonstrated significant in vitro activity against several human cancer cell lines. These compounds and the methods of producing those compounds offer a commercially viable alternative to natural and synthetic dolastatin 10.
Claims23
A composition having the general structure set forth below:
- ##STR11## wherein substituents X and Ar are as set forth below:
- a) X=Met, Ar=4FPh;
- b) X=Met, Ar=2ClPh;
- c) X=Met, Ar=3ClPh;
- e) X=Met, Ar=4ClPh;
- g) X=Met, Ar=2,5diClPh;
- i) X=Met, Ar=4ClPEA;
- m) X=Met, Ar=BnThz;
- n) X=Pro, Ar=BnThz;
- o) X=Met, Ar=2Py;
- p) X=Met, Ar=3Q;
- q) X=Pro, Ar=3Q;
- r) X=Val, Ar=3Q;
- and
- s) X=Ile, Ar=3Q.
12 more elements
A composition having the general structure set forth below:
- ##STR12## wherein substituents X and Ar are as set forth below:
- d) X=Phe, Ar=3ClPh;
- f) X=Phe, Ar=4ClPh;
- h) X=Phe, Ar=2,5diClPh;
- j) X=Phe, Ar=6FBnThz;
- k) X=Phe, Ar=6ClBnThz;
- l) X=pCl-Phe, Ar=6ClBnThz.
4 more elements
Dependencies are inferred from the claim text.