B Das Sarma | PubMed Health

PubMed1985

Antitumour activity of some platinum compounds.

A group of cis-ethylenediammine platinum (II) complexes were synthesized and their activity against Sarcoma-180 ascites tumour cells in mouse was tested. One of the compounds, Pt(HOCH2CH2NHCH2CH2NH2)Cl2, showed significant antitumour activity having little toxicity to the host. Like the parent compound, cis-DDP, it binds to DNA, but transcription is not the primary process inhibited by these compounds. The drug-DNA complex, though less toxic, was not more effective than the free drug.

Animals↗

PubMed1983

Platinum complexes with anticancer potential and their evaluation by a colorimetric lambda prophage induction assay.

A simple biochemical phage induction assay (BIA) showed significant activity with 90% of the antitumor platinum compounds tested and lack of activity for all Pd(II) compounds and Pt(II) cationic complexes, compounds that are expected to be inactive. Structure-activity relationships for a large number of chemicals can be studied simultaneously by this simple, rapid, inexpensive and quantitative biochemical assay. Fifty-three platinum complexes were tested, including a number of ethylenediamines synthesized for this work. The magnitude of inducing activity varied over a 25-fold range; differences among analogs reflected structural differences in a chemically consistent manner. Seven platinum complexes showed greater activity than that of cis-diamminedichloroplatinum(II) (cisplatin, cis-DDP), while other compounds appeared to be substantially less toxic. The assay was predictive for most compounds with very high or very low activity in vivo against L1210. For compounds with intermediate levels of activity, no correlation between inducing and antitumor activity was observed.

Antineoplastic Agents↗