Biologically active peptides and compositions, their use

Details Biologically active peptides and compositions, their use Biologically active peptides and compositions, their use

1998-02-02

2000-11-28

Low, Christopher S. F.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

514 18, 530331, 548496, C07K 5078

Patent

active

061535907

DESCRIPTION:

BRIEF SUMMARY
FIELD OF THE INVENTION

This invention relates to novel biologically active compounds and compositions, their use and derivation.
The invention has involved the extraction of novel biologically active compounds from marine sponges.


SUMMARY OF THE INVENTION

The present invention concerns new biologically active peptides and derivatives of hemiasterlin, criamide and geodiamolide. Another aspect of the invention are methods of therapy, such as anti-tumor chemotherapy, by administering the biologically active peptides or derivatives of hemiasterlin, criamide and geodiamolide.
Except where otherwise stated, throughout this specification, any alkyl moiety suitably has up to 8, especially up to 6, most preferably up to 4, carbon atoms and may be of straight chain or, where possible, of branched chain structure. Generally, methyl is a preferred alkyl group. Halogen atoms may be fluorine, chlorine, bromine or iodine. A preferred acyl group is alkylcarbonyl, especially acetyl.
Except where otherwise stated in this specification, optional substituents of an alkyl group may include halogen atoms, for example fluorine, chlorine, bromine and iodine atoms, and nitro, cyano, alkoxy, hydroxy, amino, alkylamino, sulphinyl, alkylsulphinyl, sulphonyl, alkylsulphonyl, amido, alkylamido, alkoxycarbonyl, haloalkoxycarbonyl and haloalkyl groups. Preferably, optionally substituted alkyl groups are unsubstituted.
Except where otherwise stated, throughout this specification the recitation of a compound denotes all possible isomers possible within the structural formula given for those compounds, in particular geometrical and optical isomers. Unless otherwise stated definitions are to be regarded as covering mixtures of isomers, and individual isomers, including racemic mixtures, where they can be resolved.
Except if otherwise stated, definitions of compounds in this specification are to be regarded as covering all possible salts of the compounds.
Compounds according to the first aspect of the invention have been found to be surprisingly effective in the in vivo treatment of cancer.
In accordance with the first aspect of the present invention there is provided the use of a hemiasterlin compound of general formula ##STR2## wherein: R.sub.1 and R.sub.70 independently represent a hydrogen atom or an optionally substituted alkyl or acyl group; acyl group or is absent when R represents a group --CH.dbd. as hereinafter described; when R.sub.6 represents a methylene group or a group --CH.dbd. as hereinafter described; group; substituted alkyl or acyl group; optionally substituted alkyl or acyl group; and or acyl group and R.sub.72 represents a hydrogen atom or R.sub.71 and R.sub.72 each represent radicals so that a double bond is formed between the carbon atoms to which they are attached; and indole moiety thereby to form a tricyclic moiety; or indole moiety thereby to form an aromatic tricyclic moiety;


BRIEF DESCRIPTION OF THE DRAWINGS

FIG. 1 depicts a comparison of antimitotic activity of Hemiasterlins with that of known antimitotic agents.
FIG. 2 shows the antimitotic activity of chemically modified Hemiasterlins.


DETAILED DESCRIPTION OF THE INVENTION

Preferably, R.sup.1 represents a hydrogen atom or an alkyl group, especially a methyl group. More preferably, R.sub.1 represents a hydrogen atom.
Suitably, R.sub.2 represents a hydrogen atom or an acyl group. An acyl group may be a benzoyl group, but is preferably an alkylcarbonyl group. An especially preferred acyl group is an acetyl group. Preferably, R.sub.2 represents a hydrogen atom.
Preferably, R.sub.70 represents a hydrogen atom or an alkyl group, especially a methyl group.
Where Y and/or R.sub.73 represent optional substituents, said substituents may be independently selected from halogen, especially fluorine, chlorine, bromine and iodine atoms and alkyl, acyl, --OH, --O-alkyl, O-acyl, --NH.sub.2, --NH-- alkyl, --N(alkyl).sub.2, --NH-acyl, --NO.sub.2, --SH, --S-alkyl and --S-acyl, wherein the alkyl and acyl groups of the substituents are optionally substituted.
Preferred op

REFERENCES:
patent: 5661175 (1997-08-01), Kashman
patent: 5736517 (1998-04-01), Bogden

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