Chemistry: natural resins or derivatives; peptides or proteins; – Peptides of 3 to 100 amino acid residues – Cyclic peptides
Patent
1995-06-07
1998-07-14
Ambrose, Michael G.
Chemistry: natural resins or derivatives; peptides or proteins;
Peptides of 3 to 100 amino acid residues
Cyclic peptides
536 64, 548422, 558272, 558275, 560 30, 560 32, 560163, C07K 756, C07H 1524, C07D48714, C07C27128, C07C26904, C07C 6996, C07C 6800
Patent
active
057805857
ABSTRACT:
A prodrug of the formula (I): ##STR1## where R.sup.1 is a group such that the compound R--NH.sub.2 represents actinomycin D, doxorubicin, mitomycin C, or a nitrogen mustard of the formula (IV): ##STR2## a prodrug of the formula (II): ##STR3## where R.sup.1 is a group such that the compound R.sup.2 OH is a phenolic nitrogen mustard; and processes whereby the prodrugs shown above are made in which a prodrug precursor compound is reacted with 4-nitrobenzyl chloroformate under anhydrous conditions.
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Knox, Richard J., "A New Cytotoxic, DNA Interstrand Crosslinking Agent, 5-(Aziridin-1-YL)-4-Hydroxylamino-2-Nitrobenzamide, is Formed From 5-(Azirdin-1-YL)-2,4-Dinitrobenzamide (CB 1954) by a Nitroreductase Enzyme in Walker Carcinoma Cells", Biochemical Pharmacology, vol. 37, No. 24, pp. 4661-4669 (1988).
Anlezark Gillian
Connors Thomas
Friedlos Frank
Jarman Michael
Knox Richard
Ambrose Michael G.
Cancer Research Campaign - Technology Limited
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