Synthesis and antitumor activity of (diamine)platinum(II) complexes of benzylmalonate derivatives.
(Diamine)platinum(II) complexes of benzylmalonate derivatives as a leaving group designed in a wide range of lipophilicity and water-solubility were prepared and their antitumor activities were attempted to correlate to their lipophilicity or solubility. A good relationship was observed between their in vitro toxicity and solubility of the title complexes with the same carrier ligand, DACH (trans-(+/-)-1,2-diaminocyclohexane): The most soluble complexes are most cytotoxic whereas the least soluble complexes are least cytotoxic. However, no relationship could be established between their in vivo activity and their lipophilicity or solubility presumably due to other pharmacokinetic factors involved in vivo. The molecular structure of (IPA)2Pt(DBM).2CH3OH (IPA = isopropylamine; DBM = dibenzylmalonate) was determined by X-ray diffraction: space group P2(1)/n, a = 11.433 (3), b = 14.461 (4), c = 17.478 (4) A, beta = 97.25 (3) degrees, z = 4, R = 0.0437.
Lee
Y A
YA
Inorganic Chemistry Laboratory, Korea Institute of Science and Technology, Seoul, Korea.
Chung
Y K
YK
Sohn
Y S
YS
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D007939:Leukemia L1210 / Q000188:drug therapy; D050356:Lipid Metabolism; D009682:Magnetic Resonance Spectroscopy; D008314:Malonates / Q000737:chemistry*; D051379:Mice; D008958:Models, Molecular; D015394:Molecular Structure; D009944:Organoplatinum Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D017671:Platinum Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D012995:Solubility; D013329:Structure-Activity Relationship; D014961:X-Ray Diffraction
C110113:(dibenzylmalonate)diisopropylamineplatinum(II); D000970:Antineoplastic Agents; D008314:Malonates; D009944:Organoplatinum Compounds; D017671:Platinum Compounds