a new class of platinum(II) complexes [Pt(trans-l-dach)(DPPP)] 2NO₃ and [Pt(trans-l-dach)(DPPE)] 2NO₃ exhibiting antitumor activity and nephrotoxicity

Author: Lee, Kyung Tae ; Yoon, Chin Hee ; Rho, Young Soo ; Chang, Sung Goo ; Jung, Jee Chang

Pt-complexes are compounds used in the treatment of solid tumors.However, their use is limited by severe side effects such as renal toxicity.The authors platinum-based drug discovery program is aimed at developing drugs capable of diminishing toxicity and improving antitumor activity.The authors synthesized new Pt (II) complex analogs containing 1,2-diaminocyclohexane (dach) as the carrier ligand and 1,3-bis(diphenylphosphino)propane (DPPP) or 1,2-bis(diphenylphosphino)ethane (DPPE) as a leaving group.Furthermore, nitrate was added to improve the solubilityA new series of (KHPC-001) [Pt(trans-1-dach)(DPPP)] 2NO₃ and (KHPC-002) [Pt(trans-1-dach)(DPPE)] 2NO₃ were synthesized and characterized by their elemental anal. and by various spectroscopic techniques [IR, ¹³carbon NMR].KHPC-001 and KHPC-002 demonstrated acceptable antitumor activity against P-388 and L-1210 lymphocytic leukemia cells and significant activity as compared with that of cisplatin.The toxicity of KHPC-001 and KHPC-002 was found to be less than that of cisplatin using MTT and [³H]thymidine uptake and glucose consumption tests in rabbit proximal tubule cells and human kidney cortical cells.

Yakche Hakhoechi

Synthesis of platinum(II) complexes containing diphosphines and evaluation of antitumor activity

Author: Noh, Young Soo ; Noji, Masahide

New antitumor-active [PtQL](NO₃)₂ (Q = trans-(-)-1,2-cyclohexanediamine; L = DPPE, Ph₂P(CH₂)₃PPh₂ (DPPP) leaving group) were synthesized.The structures of [PtQL](NO₃)₂ were determined by analyzing the IR and ³¹P NMR spectra.Antitumor activities of [PtQL](NO₃)₂ were tested against murine leukemia L₁₂₁₀ according to the protocol of the Natl. Cancer Inst.All [PtQL](NO₃)₂ synthesized were antitumor-active.H₂O-soluble [PtQ(DPPP)](NO₃)₂ exhibited excellent antitumor activity, giving T/C % values of 341 and 356 resp., each with 4 cured mice out of 6 at a dose of 25 mg/kg.

Anticancer Research

New platinum complex compounds with reduced nephrotoxicity discovered in long-term histoculture of human renal cortical tissue

Author: Rho, Young-Soo ; Chang, Sung-Goo ; Jung, Jee-Chang ; Kim, Jin-Il ; Kwon, Dong-Uk ; Hoffman, Robert M.

Cisplatinum is often effective in cancer treatment, but potent nephrotoxicity limits its clin. use.The authors have synthesized six new platinum compounds with the goal of reducing toxicity while maintaining efficacy.The authors initially tested drugs at 5×10^-4M with 48 h exposure in monolayer cultures of primary rabbit proximal tubular cells and human renal cortical cells with the MTT endpoint to measure toxicity.Drug concentration of 10^-3M, 10^-4M and 10^-5M with 72 h exposure were used for human renal cortical tissues in 7 wk sponge-gel-supported histoculture with toxicity measured by the glucose-consumption endpoint.From these studies, the authors determined that the new platinum drugs have lower nephrotoxicity than cisplatinum.

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Indication	Highest Phase	Country/Location	Organization	Date
Neoplasms	Phase 1	-	Kyung Hee University	-

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