Linked Life Data

10066891

Source:http://linkedlifedata.com/resource/pubmed/id/10066891

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
3
pubmed:dateCreated
1999-5-7
pubmed:abstractText
One of the most investigated classes of antitumor drugs is represented by anthracyclines. Over thirty years since the original discovery of daunorubicin and doxorubicin thousands of anthracycline analogues have been synthesized and tested to identify compounds superior to the parent drugs in terms of increased therapeutic effectiveness, reduced toxicity or both. Previous structure-activity studies had shown that minor modifications of the anthracycline structure can result not only in active agents, but, more importantly, analogues with reduced cardiotoxicity and activity on multi drug resistance. The fact that 4-demethoxydaunorubicin showed higher potency than daunorubicin and a reduced cardiotoxicity, prompted us to explore novel analogues with altered substitution patterns on the anthraquinone system, particularly ring-B. In this review we will describe total synthesis and antitumor activity of three classes of derivatives: whereby one hydroxyl group in ring-B was either removed or replaced with nitro or amino groups. While these modifications yielded anthracyclines with a promising pharmacological activity, they did not modify activity on multidrug resistant (MDR) tumors. On the other hand, introduction of morpholino group in the sugar part of these new molecules, dramatically increased activity on MDR tumors. We conclude that activity on MDR tumors is not bound to modifications in the aglycone moiety of anthracyclines.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Mar
pubmed:issn
1381-6128
pubmed:author
pubmed:issnType
Print
pubmed:volume
5
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
217-27
pubmed:dateRevised
2006-2-27
pubmed:meshHeading
pubmed:year
1999
pubmed:articleTitle
Ring-B modified anthracyclines.
pubmed:affiliation
Discovery Research Oncology, Pharmacia & Upjohn S.p.A., Viale Pasteur, Nerviano, 10 20014 (MI), Italy.
pubmed:publicationType
Journal Article, Review