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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 20, Number 12
BKCSDE 20(12)
December 20, 1999 

Synthesis, Structure, and Antitumor Activity of Novel Platinum(II) Complexes Involving Asymmetric Chiral Diamines as Carrier Ligands
Eun Ju Lee, Moo-Jin Jun, Youn Soo Sohn
New platinum(II) complexes with asymmetrically substituted chiral diamine ligands A2PtX2, (A2 = NH2CH(CH3)CH2NH(c-C5H9) (apcpa), NH2CH(CH3)CH2NH(c-C6H11) (apcha); X2 = 2Cl, isopropylidenmalonate (IPM), 1,1'-cyclobutandicarboxylate (CBDCA)) have been synthesized and characterized by means of elemental analyses, infrared and NMR spectroscopies, and X-ray crystallography. The crystal structures of (S-apcha)Pt[CBDCA] ·3H2O (orthorhombic, P21212(No. 18), a = 6.926(3), b = 15.243(3), c = 19.319(4)Å, V = 2039.5(10) Å 3 , Z = 4, R = 0.072) and (S-apcha)Pt[IPM] ·2.5 H2O (monoclinic, P2/C(No. 13), a = 9.882(1), b =18.502(1), c = 22.056(1)Å, V = 4032.8(5)Å3 , Z = 8, R=0.093) exhibit that the platinum atoms achieve a typical square planar arrangement with two nitrogen atoms in cis position and with the chiral center retained. The spectroscopic data disclose that these platinum complexes are stable and their molecular structures are retained in aqueous solution. Among these platinum complexes, the asymmetric diamine-Pt(II) complexes with chloride leaving group exhibit high in vivo activity comparable to cisplatin against leukemia L1210 cell line.
1469 - 1474
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