successful complete regression of these large tumors in 63 to 100% of the animals. c1L@@@†• Chart 1. Structural diagrams of the 2 platinum compounds found to be active against Sarcoma 180 and Leukemia L1210 in mice: the octahedral complex, cis-Pt(I\')(NH3)@CL@and the square planar com plex, cis-Pt(II)(NH3)2Cl2. MATERIALS AND METHODS Random-bred Swiss white mice, obtained from Spartan Research...

The binding of the antitumor drug cis-dichlorodiammineplatinum(II) and its inactive trans isomer with the nucleosome core particle has been investigated. Kinetic studies show that platinum binding increases with incubation time, from a few bound platinum atoms per nucleosome core in the first 0.5 hr to 40-50 after 40 hr. There is no crosslinking or dissociation of nucleosome cores upon platinum...

The formation and isolation of the antitumor drug cisplatin analogue cis-[PtCl2(Hmtpo-N3)2].2H2O (1) (where Hmtpo = 4,7-H-5-methyl-7-oxo[1,2,4]triazolo[1,5-a]pyrimidine) by reaction of Hmpto with K2[PtCl4] in HCl (0.5 N) is reported. This complex crystallizes in the monoclinic space group P21/c with unit cell dimensions a = 15.215(2) A, b = 9.629(1) A, c = 13.115(3) A, beta = 97.40(2) degrees, ...

Abstract Two tungstates containing platinum nanoparticles (Pt Npts) were obtained by air-calcining α-Keggin-type diplatinum(II)-coordinated polyoxotungstates, Cs 3 [α-PW 11 O 39 { cis -Pt(NH ) 2 } ]⋅8H ( Cs-P-Pt and 4 [α-SiW ]⋅11H Cs-Si-Pt ), at 700–900 °C for 5 h. The polyoxotungstate was transformed to a mixture of Pt Npts PW 12 40 upon calcination, while the structures W 35 . generated 700 h...

Three new ligands of the general formula [RNHCH(py)(2)] (py = pyridine; R = tosyl, Ts-dpm; R = dansyl, Ds-dpm; R = 7-nitro-1,2,3-benzoxadiazole, NBD-dpm) have been synthesized and characterized. Reactions of these ligands with cis-[Pt(DMSO)(2)Cl(2)] (DMSO = dimethyl sulfoxide) in methanol affords [Pt(Ts-dpm)Cl(2)] (1), [Pt(Ds-dpm)Cl(2)] (2), and [Pt(NBD-dpm)Cl(2)] (3). The crystal structures of...

Unlike cisplatin, which forms bifunctional DNA adducts, monofunctional platinum(II) complexes bind only one strand of DNA and might target cancer without causing auditory side-effects associated with cisplatin treatment. We synthesized the monofunctional triamine-ligated platinum(II) complexes, Pt(diethylenetriamine)Cl, [Pt(dien)Cl]+, and Pt(N,N-diethyldiethylenetriamine)Cl, [Pt(Et2dien)Cl]+, a...

ROSENBERG (1977) put forward a hypothesis concerning the mechanism of anticancer activity of cis-platinum complexes in vivo. According to this hypothesis, the simple cytotoxic effect is accompanied by an enhanced expression of cancer antigens on the surface of malignant cells. Therefore, the observed regression of malignant growth is at least partly due to the immunological response of the orga...

The interactions of four antitumor azolato-bridged dinuclear platinum(II) complexes, [{cis-Pt(NH(3))(2)}(2)(μ-OH)(μ-azolato)](2+), with calf thymus DNA were monitored dose- and time-dependently, by using circular dichroism. Complexes 1-4 reacted with DNA via a two-step interaction that comprised a prompt diffusion-controlled reaction, which induced a B- to C-form transition, and a relatively sl...