Cell Growth-Inhibiting Properties of Selected Carrier-Bound, Monoamine-Coordinated Platinum(II) Compounds

摘要: In contradistinction to the ligand arrangement in coordination compounds of square-planar cis-diamminedichloroplatinum(II) type as represented by prototype anticancer drug cisplatin, scant attention has been paid cancer research those platinum complexes which only a single amino group (in addition different ligands) is coordinated metal. continuation earlier this laboratory focused on macromolecular containing monoamine-coordinated platinum, we have now synthesized series such polymeric conjugates and assessed their antiproliferative activity cell culture tests conducted against several human lines. Conjugates hydroxylated side groups hydrosolubilizing entities are found exhibit poor, or no, up highest concentration tested (50 μg Pt/mL). contrast, solubilizing units characterized presence potentially cationic tert-amine chain terminals show remarkably high cell-killing activity, with IC50 range 1–6 Pt/mL HeLa cervical epitheloid carcinoma line. Two selected samples A-2780 ovarian line its cisplatin-resistant A-2780-cis counterpart shows lack cross-resistance cisplatin (resistance factor ≤1). These findings augur well for development polymer-conjugated carcinostatic properties.