From the pigments of the actinomycetes to third generation antitumor anthracyclines.

Abstract:

:After the assessment of the antitumor activity of the anthracycline pigments, the S peucetius group of metabolites was discovered and eventually doxorubicin, a major anticancer agent of established clinical usefulness was developed in the early seventies. A second generation of compounds followed, represented mainly by the better tolerated epirubicin and by the highly potent antileukemic drug, idarubicin. This was the result of a wide program of analog development that provided the basis for further investigations concerning both the study of structure-activity relationships and the synthesis of novel promising derivatives including the 8- and 10-fluoro compounds and the disaccharides. A member of the latter group, namely 7-O-(4'-O-alpha-L-daunosaminyl-2'-deoxy- alpha-L-fucosyl)-4-demethoxyadriamycinone, is undergoing clinical trials as a third generation antitumor anthracycline.

journal_name

Biochimie

journal_title

Biochimie

authors

Arcamone FM

doi

10.1016/s0300-9084(98)80003-5

subject

Has Abstract

pub_date

1998-03-01 00:00:00

pages

201-6

issue

3

eissn

0300-9084

issn

1638-6183

pii

S0300-9084(98)80003-5

journal_volume

80

pub_type

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