• 대한약학회:학술대회논문집
• /
• 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
• /
• pp.358.3-358.3
• /
• 2002

We recently synthesized new platinum(II) complex analogs containing trans-1 and cis-l.2-diaminocyclohexane (DACH) as carrier ligands and L -3-phenyllactic acid(PLA) as a leaving group. Our platinum-based drug discovery program has been aimed at developing drugs capable of diminishing toxicity and improving selective cytotoxicity. (omitted)

• 한국환경보건학회지
• /
• 제20권3호
• /
• pp.31-38
• /
• 1994

Dithiocarbamates containing polar groups which give very water soluble metal complexes were prepared from the reaction of carbon disulfide with diamines. The compounds have been characterized by elemental analysis, molar conductivity, and spectroscopic results. Dithiocarbamate and its complex were soluble in water. N, N-Dimethylammoniumpropylenedithiocarbamate(A) is clearly effective as inhibition of cis-platinum nephrotoxicity in rats. From the result of A rescue after cis-dichlorodiammineplatinum(II) treatment, it is suggested that dithiocarbamate removes platinum(II) coordinated to -SH groups bound to protein of kidney tubule cells by the reaction of platinum(II) with dithiocarbamate injected. A is effective as antidots for acute cadmium poisoning in Bacillus subtills. Growth of Bacillus subtills may be accelerated by A ligand dissociated from cadmium (II)-A complex.

• 분석과학
• /
• 제8권4호
• /
• pp.691-698
• /
• 1995

The complexation of platinum and palladium with synthetic polyelectrolytes was studied. The successive and overall stability constants of Pd(II) with PEI and 2PVP were obtained by potentiometric titration. Because of the slow equilibrium time, the potentiometric titrations were performed using the home-made automatic titrator in order to analyze the complexations according to the modified Bjerrum method. The complex formation constant of Pt(IV) with 2PVP, measured by differential pulse polarography, was calculated from the peak currents that were obtained in non-complexing media and in solution containing 2PVP.

• Environmental Analysis Health and Toxicology
• /
• 제8권3_4호
• /
• pp.23-32
• /
• 1993

This study was designed to elucidate the mechanism of nephrotoxicity caused by antitumor agent tetraphosphine platinum (II) complex (RC-1), which was synthesized as a tetraphosphine Pt (II) derivatives recently. Rats treated with RC-1 (20mg/kg/day) showed the increase of BUN value and malondialdehyde contents in kidney homogenate, compared to the control and which means the lipid peroxidation was a main cause of nephrotoxicity. In order to investigate the cytotoxic mechanism of RC-1, we also tested and revealed the generation of oxygen free radicals derived from neutrophil stimulated by RC-1 and interaction of the oxygen free radicals with the erythrocyte membrane. From the above results, we suggest that nephrotoxicity of general platinum (II) antitumor compounds as well as RC-1 were inhibited by radical scavengers.

• Biomolecules & Therapeutics
• /
• 제11권2호
• /
• pp.91-98
• /
• 2003

A new series of highly water soluble platinum(II) complexes[Pt(II)(DL-2-hydroxy-3-methylbutyrate)(trans-l-1,2-dimninocyc1ohexane)] (PC-1) and [Pt(II)DL-2-hydroxy-3-methylbutyrate](cis-1,2-diaminocyclohexane)](PC-2) were synthesized and characterized by their elemental analysis and by various spectroscopic techniques [infrared(IR), $^{13}C$-nuclear magnetic resonance (NMR)]. In vitro antitumor activity of new Pt(II)complexes was tested against MKN-45, MKN/ADM and MKN/CDDP human gastric adenocarcinoma cell lines using colorimetric MTT[3-(4,5-dimethyl thiazol-2-yl)-2,5-diphenyltetrazoliumbromide] assay for cell survival and proliferation. PC-1 and PC-2 showed active against MKN-45/P, MKN/ADM and MKN/CDDP human gastric cancer cell lines, and the antitumor activity of these compounds were comparable or superior to that of cisplatin. The nephrotoxicities of PC-1 and PC-2 were found quite less then that of cisplatin using MTT and [$^3H$] thymidine uptake tests in rabbit proximal tubule cells, human kidney cortical cells human renal cortical tissues. Based on these results, these novel platinum(II) complex compounds(PC-1 ＆ PC-2) represent a valuable lead in the development of the new anticancer chemotherapeutic agents capable of improving antitumor activity and low nephrotoxicity.

• Bulletin of the Korean Chemical Society
• /
• 제29권8호
• /
• pp.1491-1494
• /
• 2008

A novel platinum aminoalkoxide complex, Pt$(dmamp)_2$ has been prepared by the reaction of cis-$(py)_2PtI_2$ with two equivalents of Na(dmamp) (dmamp = 1-dimethylamino-2-methyl-2-propanolate). Single-crystal X-ray crystallographic analysis shows that the Pt(dmamp)2 complex keeps a square planar geometry with each two nitrogen atoms and two oxygen atoms having trans configuration. Platinum films have been deposited on TaN/ Ta/Si substrates by metal organic chemical vapor deposition (MOCVD) using Pt$(dmamp)_2$. As-deposited platinum thin films did not contain any appreciable amounts of impurities except a little carbon. As the deposition temperature was increased, the films resistivity and deposition rate increased. The electrical resistivity (13.6 $\mu\Omega$cm) of Pt film deposited at 400 ${^{\circ}C}$ is a little higher than the bulk value (10.5 $\mu\Omega$cm) at 293 K. The chemical composition, crystalline structure, and morphology of the deposited films were investigated by X-ray photoelectron spectroscopy, X-ray diffraction, and atomic force microscopy.

• Bulletin of the Korean Chemical Society
• /
• 제22권1호
• /
• pp.15-16
• /
• 2001

• Biomolecules & Therapeutics
• /
• 제5권2호
• /
• pp.125-132
• /
• 1997

Cisplatin, a platinum-complex, is currently one of the most effective compounds used in the treat-ment of solid tumors. However, its use is limited by severe side effects such as renal toxicity. Our platinum-based drug discovery program is aimed at developing drugs capable of diminishing toxicity and improving selective cytotoxicity. We synthesized new Pt (II) complex analogue containing 1,2-diaminocyclohexane (DACH) as carrier ligand and 1,2-bis (diphenylphosphino) ethane (DPPE) as a leaving group. Furthermore, nitrate was added to improve the solubility. A new series of [Pt(cia-DACH)(DPPE)] . $2NO_3$ (PC) was synthes-ized and characterized by their elemental analysis and by various spectroscopic techniques [infrared (IR), $_{13}$carbon nuclear magnetic resonance (NMR)] .PC demonstrated acceptable and significant antitumor activity against SKOV-3 and OVCAR-3 human ovarian carcinoma cell lines as compared with that of cisplatin. The cytotoxicity of PC in normal cells was found quite less than that of cisplatin using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT), ($^3$H)thymidine uptake and glucose consumption tests in rabbit renal proximal tubular cells, human renal cortical cells and tissues. In conclusion, PC is considered to be more selective cytotoxicity toward human ovarian cancer cells than normal human/rabbit kidney cells.

• 한국응용약물학회:학술대회논문집
• /
• 한국응용약물학회 1995년도 춘계학술대회
• /
• pp.124-124
• /
• 1995

Cisplatinum is often effective in cancer treatment, but potent nephrotoxicity limits its clinical use. We have, therefore, developed new anticancer drugs that contain platinum. We have synthesized six new platinum compounds based on Figure 1. Drugs were initially administrated at 5${\times}$10$\^$-4/M with 48 hours exposure in monolayer cultures of primary rabbit proximal tubular cells and human renal cortical cells with the M.T.T. endpoint to measure toxicity. Drug concentrations of 10$\^$-3/M, 10$\^$-4/M, and 10$\^$-5/M with 72 hours exposure were used for human renal cortical tissues in 7 weeks histoculture with toxicity measured by the glucose-consumption endpoint. From these studies, we determined that the new platinum drugs have lower nephrotoxicity than cisplatinum. Drugs D, E, and H. have lower nephrotoxicity than the other new drugs. We are currently measuring the anticancer efficacy of drugs D, E, and H.

• 대한화학회지
• /
• 제28권6호
• /
• pp.399-402
• /
• 1984

l-tartaric acid를 이용하여 두자리 아민리간드인 6,6'-dimethyl-2,2'-dia minobiphenyl (dmdabp)를 분할하여 S광학이성질체인 S-dmdabp를 얻었다. S-dmdabp로 부터 평면사각형 착물[Pt(S-dmdabp)Cl$_2]$를 합성하였으며, 이 착물에서 S-dmdabp 리간드가 ${\delta}$-confomation으로 배위 되어 있음을 확인하였다.