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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 21, Number 10
BKCSDE 21(10)
October 20, 2000 

Lpophilicity vs. Antitumor Activity of Carboxylatoplatinum(lV) Complexes
Rita Song, Kwan Mook Kim, Youn Soo Sohn
Acylation of an intermediate tetrahydroxoplatinum(IV) complex, [Pt(OH)₄(dach)] (dach = trans-(±)-1,2-di-aminocyclohexane), with one or two kinds of carboxylic anhydrides in stepwise manner afforded various car-boxylatoplatinum(IV) complexes, [Pt(O₂CR)χ(OR’)4-χ(dach)] (R = (CH₂)₃CH₃ or C(CH₃)₃, R’ = H or OCCH₃, and χ = 1-4) with a wide range of lipophilicity. The title complexes were subjected to bioassay using the murine leukemia L1210 cell line, and in particular, their in vivo oral antitumor activity was attempted to correlate with their lipophilicity and water solubility. The most orally active complex exhibited intermediate lipophilicity and water solubility, but it has been found that an exact relationship between the lipophilicity and oral anticancer activity could not be established, since the lipophilicity of the complexes is not the sole parameter to determine the oral activity. One of the important intermediate complexes partially substituted was subjected to X-ray anal-ysis for positit of the substituted group: [Pt(OPiv)₃(OH)(dach)] crystallizes in the tetragonal sys-tem, space group P42₁c with a = 21.161(3) Å, b = 21.161(6) Å, c = 12.816(3) Å, α= β= r =90°, V = 5739(2) ų and Z = 8.
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