The synthesis and antitumor activity of metal complexes of amine–carboxyborane adducts

✍ Scribed by M. C. Miller; A. Sood; B. F. Spievogel; I. H. Hall

• Publisher: John Wiley and Sons
• Year: 1998
• Tongue: English
• Weight: 171 KB
• Volume: 12
• Category: Article
• ISSN: 0268-2605
• DOI: 10.1002/(sici)1099-0739(199802)12:2<87::aid-aoc671>3.0.co;2-#

✦ Synopsis

The amine carboxyborane metal complexes, tetrakis --(trimethylamine -boranecarboxylato)acetonitrile dicopper(II) and bis--(morpholine-boranecarboxylato)zinc(II) dihydrate demonstrated cytotoxic activity against human Tmolt 3 , HeLa-S 3 and MB-9812 cell growth. Tetrakis--(trimethylamine-boranecarboxylato)-acetonitrile dicopper(II) and bis --(morpholine -boranecarboxylato)zinc (II) dihydrate inhibited L 1210 DNA, RNA and protein syntheses, with greatest inhibitory effects on DNA synthesis. The reduction in DNA synthesis correlates well with inhibition of de novo purine synthesis and the key enzymes involved in this pathway, i.e. IMP dehydrogenase and PRPP amido transferase. These compounds were also observed to induce DNA strand scission but did not appear to intercalate between base pairs of DNA, alkylate bases or cause cross-linking of the strands of DNA. Tetrakis--(trimethylamine -boranecarboxylato)acetonitrile dicopper(II) also demonstrated the ability to inhibit L 1210 DNA topoisomerase II activity.