Switch to
| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
2
|
| pubmed:dateCreated |
1993-6-10
|
| pubmed:abstractText |
The novel cisplatin analogue D-17872 was studied for its anticancer activity using in vivo and in vitro preclinical models. The compound at the sublethal dose of 215 mg/kg (ca. 50% of the approximate LD50) induced no nephrotoxic effect strong enough to increase the blood urea level in rats. It had good in vivo antitumor efficacy against murine P388 (max. ILS: D-17872 132%, cisplatin 55%) and L1210 leukemia (max. ILS: D-17872 43%, cisplatin 38%), L5222 leukemia of the rat (max. ILS: D-17872 163%, cisplatin 163%) and murine B16 melanoma. Activity against P388 leukemia substantially exceeded that of cisplatin. Moreover, the M5076 reticulum cell sarcoma implanted into the subrenal capsule and the DMBA-induced mammary tumor of the rat were inhibited by D-17872 to a greater extent than by cisplatin (min. T/C: D-17872 -3%, cisplatin 11%). Using clonogenic microassays, D-17872 was active in vitro against a variety of human and rodent tumor cell lines, albeit at higher concentrations than cisplatin (IC50 values: D-17872 2.6-12.7 mumol/l, cisplatin 0.13-0.42 mumol/l). Apart from its cytotoxic action it was able to induce in vitro differentiation of the human HL-60 and K562 and of the murine M1-T22 cell lines, while cisplatin induced differentiation only in the HL-60 cell line. Thus D-17872 exhibited a pharmacological and toxicological profile different from that of the parent compound. The results suggest that induction of differentiation contributes to the antineoplastic efficacy of this novel cisplatin derivative.
|
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical | |
| pubmed:status |
MEDLINE
|
| pubmed:issn |
0344-5704
|
| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:volume |
32
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
123-8
|
| pubmed:dateRevised |
2003-11-14
|
| pubmed:meshHeading |
pubmed-meshheading:8485806-Animals,
pubmed-meshheading:8485806-Antineoplastic Agents,
pubmed-meshheading:8485806-Cell Differentiation,
pubmed-meshheading:8485806-Cell Division,
pubmed-meshheading:8485806-Cisplatin,
pubmed-meshheading:8485806-Erythrocytes,
pubmed-meshheading:8485806-Ethylenediamines,
pubmed-meshheading:8485806-Female,
pubmed-meshheading:8485806-Injections, Intraperitoneal,
pubmed-meshheading:8485806-Male,
pubmed-meshheading:8485806-Mice,
pubmed-meshheading:8485806-Mice, Inbred C57BL,
pubmed-meshheading:8485806-Monocytes,
pubmed-meshheading:8485806-Neoplasms, Experimental,
pubmed-meshheading:8485806-Rats,
pubmed-meshheading:8485806-Rats, Sprague-Dawley,
pubmed-meshheading:8485806-Tumor Cells, Cultured
|
| pubmed:year |
1993
|
| pubmed:articleTitle |
The antitumor activity of the platinum complex D-17872 is associated with tumor cell differentiation.
|
| pubmed:affiliation |
Institut für Pharmazie, Freien Universität Berlin, Germany.
|
| pubmed:publicationType |
Journal Article
|