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SYNTHESIS, PHYSICO-CHEMICAL PROPERTIES AND CYTOTOXIC ACTIVITY OF BISCAROXYLATE COMPLEXES OF PLATINUM (II) WITH N-SUBSTITUTED 5-AMINOTETRAZOLES

Abstract

Effective methods for preparation of tetrazole-containing biscaroxylate complexes of platinum (II) were developed and novel oxalate, malonate and succinate platinum (II) complexes with 1-R- and 2-R-5-aminotetrazoles (R = 1-CH3, 2-CH3, 1-C6H5, 2-t-C4H9), analogues of third-generation antitumor platinum drugs were prepared. Studies of the obtained complexes showed their stability in solution, which is sufficient for biological studies. Cell proliferation tests and bioanalytical studies showed that increasing the hydrophobicity of substituents at the tetrazole heteroring leads to an increase in the intracellular concentration of complexes followed by a growth of their cytotoxic activity. Two platinum oxalate complexes with 5-amino-1-phenyl- and 5-amino-2-tert-butyltetrazoles having cis-configuration were chosen as leader compounds featuring the best combination of the antiproliferative activity, lipophilicity, and solubility.

About the Authors

T. V. SEREBRYANSKAYA
Научно-исследовательский институт физико-химических проблем БГУ, Минск
Belarus


Y. V. GRIGORIEV
Научно-исследовательский институт физико-химических проблем БГУ, Минск
Belarus


I. M. GRIGORIEVA
Научно-исследовательский институт физико-химических проблем БГУ, Минск
Belarus


O. A. IVASHKEVICH

Belarus


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ISSN 1561-8323 (Print)
ISSN 2524-2431 (Online)