Antitumor and Cellular Pharmacological Properties of a Novel Platinum(IV) Complex:trans-[PtCl2(OH)2(Dimethylamine) (Isopropylamine)]

摘要: The antitumor and cellular pharmacological properties of the trans-Pt(IV) complex, trans-[PtCl(2)(OH)(2)(dimethylamine)(isopropylamine)] (compound 2) has been evaluated in comparison with its corresponding trans-Pt(II) counterpart, trans-[PtCl(2)(dimethylamine)(isopropylamine)] 1). results reported here indicate that compound 2 markedly circumvents cisplatin resistance 41McisR CH1cisR ovarian tumor cell lines endowed different mechanisms (decreased platinum accumulation enhanced DNA repair/tolerance, respectively). However, 1 is able to circumvent only cells. Interestingly, at equitoxic concentrations, compounds induce a higher amount apoptotic cells than Moreover, number induced by correlates their ability form interstrand cross-links Although showed remarkable cytotoxic activity, was inhibit growth CH1 human carcinoma xenografts mice. Binding studies serum albumin possesses much reactivity against 2. level binding plasma proteins during period 15 min h after administration mice (15 mg/kg, i.p.) 2.5-fold Therefore, lack vivo activity shown might be related extracellular inactivation before reaching site because high rate proteins.