Cytotoxic activity of two polyaspartamide- based monoamineplatinum(II) conjugates against the HeLa cancer cell line
✍ Scribed by Gregg Caldwell; Eberhard W. Neuse; Constance E. J. van Rensburg
- Publisher
- John Wiley and Sons
- Year
- 1999
- Tongue
- English
- Weight
- 63 KB
- Volume
- 13
- Category
- Article
- ISSN
- 0268-2605
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✦ Synopsis
In this screening study in vitro, two polymerconjugated, square-planar platinum(II) complexes bound to the carrier via a single primary amine ligand were tested for antineoplastic activity against the HeLa human cervical epithelioid carcinoma cell line. In the first of these conjugates, 1-Pt, the spacer connecting the metal complex with the carrier backbone is a short oligo(ethylene oxide) segment, whereas a long poly(ethylene oxide) chain represents the spacer unit in the second conjugate, 2-Pt. IC 50 data, expressed as conjugate concentration at 50% cell growth inhibition, are 48 mg Pt ml À1 for 1-Pt and 120 mg Pt ml À1 (estimated) for 2-Pt, the long tether in the latter conjugate presumably causing retarded enzymic release and lysosomal membrane crossing of the monomeric complex. The IC 50 value of 1-Pt is close to that (44 mg Pt ml À1 ) of a similar conjugate of an earlier investigation, 3-Pt, in which the metal is chelated by two carrier-attached, cis-oriented amino groups in conformance with the ligand arrangement in cisplatin. It thus appears that, in the carrier-bound state, both monoamine-and cis-diamine-coordinated platinum(II) complexes of suitable structures may well show similar biological performance patterns.