Porphyrin derivatives, and their production and use

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

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C07D48722

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active

049963120

ABSTRACT:
A porphyrin compound of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each --CH.dbd.CH.sub.2, --CH.sub.2 CHJ.sub.3, --CH(O-lower alkanoyl)CH.sub.3, --CH(OR)CH.sub.3 or --CH(O-lower alkylene-OR)CH.sub.3 ; R.sub.3 is --H, --COOH, --COO-lower alkyl, --COO-lower alkylene-OR or --COO-lower alkylene-OOC-Z; R.sub.4 is --H, -lower alkyl or -lower alkylene-OR; R is --H, -lower alkyl or a residue of a polyfunctional carboxyl compound excluding a hydrogen atom therefrom; Z is a residue of the compound of the formula (I) excluding R.sub.3 therefrom; A is --CH.sub.2 -- or --CO--; and the dotted line from the gamma-position indicates no bonding or a single direct bond; and the dotted line between the 7- and 8-positions indicates the presence of a single bond or a double bond; and its complexes with a metal(s) in the porphine skeleton and/or at the residue of the polyfunctional carboxyl compound, at least one of R.sub.1, R.sub.2, R.sub.3 and R.sub.4 being a group containing R which represents the residue of the polyfunctional carboxyl compound and R.sub.1 being capable of representing 1-iodoethyl in addition to said meanings when R.sub.3 is --COO-lower alkylene-OOC-Z, which shows a high accumulation in the locus of cancer with quick excretion from normal tissues.

REFERENCES:
patent: 4604241 (1986-08-01), Sakata et al.
patent: 4634557 (1987-01-01), Sato
patent: 4649151 (1987-03-01), Dougherty et al.
patent: 4675338 (1987-06-01), Bommer
patent: 4849207 (1989-07-01), Sakata et al.
Morrison and Boyd Organic Chemistry, 3rd ed. (Boston, Allyn and Bacon, 1973, p. 1042.

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