Premium
Cytotoxic activity of two polyaspartamide‐ based monoamineplatinum(II) conjugates against the HeLa cancer cell line
Author(s) -
Caldwell Gregg,
Neuse Eberhard W.,
Rensburg Constance E. J. van
Publication year - 1999
Publication title -
applied organometallic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.53
H-Index - 71
eISSN - 1099-0739
pISSN - 0268-2605
DOI - 10.1002/(sici)1099-0739(199903)13:3<189::aid-aoc835>3.0.co;2-o
Subject(s) - chemistry , conjugate , hela , platinum , ligand (biochemistry) , stereochemistry , conjugated system , cytotoxicity , chelation , metal , ic50 , in vitro , polymer , biochemistry , organic chemistry , mathematical analysis , receptor , mathematics , catalysis
In this screening study in vitro , two polymer‐conjugated, 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 µg Pt ml −1 for 1‐Pt and 120 µg Pt ml −1 (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 µg Pt ml −1 ) 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. Copyright© 1999 John Wiley & Sons, Ltd.