TY - JOUR
T1 - Comparative Antitumor Studies on Platinum(II) and Platinum(IV) Complexes Containing 1,2-Diaminocyclohexane
AU - Vollano, Jean F.
AU - Al-baker, Salaam
AU - Dabrowiak, James C.
AU - Schurig, John E.
PY - 1987/4/1
Y1 - 1987/4/1
N2 - The synthesis and characterization of a group of platinum(IV) compounds containing the various isomeric forms of 1,2-diaminocyclohexane (DACH) are described. Antitumor tests with the new complexes, as well as with other platinum(II) compounds containing the DACH ligand, revealed that trans,cis-PtIV(SS-DACH)(OH)2Cl2, 7, is more active than its mirror image, trans,cis-PtIV(RR-DACHH)(OH)2Cl, 6, against L1210 leukemia implanted in mice. However, activity is dependent on the tumor model, and against B16 melanoma implanted in mice, the activities of the two enantiomers are reversed, with 6 being more active than 7. The results of the tests are discussed in light of the mechanism by which Pt(IV) compounds are believed to express their antitumor effects.
AB - The synthesis and characterization of a group of platinum(IV) compounds containing the various isomeric forms of 1,2-diaminocyclohexane (DACH) are described. Antitumor tests with the new complexes, as well as with other platinum(II) compounds containing the DACH ligand, revealed that trans,cis-PtIV(SS-DACH)(OH)2Cl2, 7, is more active than its mirror image, trans,cis-PtIV(RR-DACHH)(OH)2Cl, 6, against L1210 leukemia implanted in mice. However, activity is dependent on the tumor model, and against B16 melanoma implanted in mice, the activities of the two enantiomers are reversed, with 6 being more active than 7. The results of the tests are discussed in light of the mechanism by which Pt(IV) compounds are believed to express their antitumor effects.
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U2 - 10.1021/jm00387a023
DO - 10.1021/jm00387a023
M3 - Article
C2 - 3560163
AN - SCOPUS:0023189985
SN - 0022-2623
VL - 30
SP - 716
EP - 719
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
IS - 4
ER -