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- W403589225 abstract "Platinum complexes (cisplatin, carboplatin) [1 – 3] or their combination with other cytostatics are widely used in modern clinical practice to treat malignant tumors. A serious disadvantage of these drugs is the high toxicity and the narrow range of therapeutic doses due to this. This limits their potential for practical application. Another disadvantage of modern antitumor drugs based on divalent platinum is the low selectivity of their action. A review of the literature showed that attempts to modify cisplatin in order to increase its effectiveness, reduce its toxicity, and increase its solubility in water had not been previously attempted [4 – 6]. Therefore, we prepared new Pt(II) complexes with the cis-configuration, which have higher antitumor activity than those with the trans-configuration [7, 8]. For this, we used compound such as ethylenediamine, trimethylenediamine, unsubstituted pyridine, and several others as ligands, which themselves are highly toxic. The metal complexes based on them exhibited high toxicity, which was one of the reasons for their limited practical use. Herein we use biogenic nontoxic compounds as ligands, namely nicotinic and isonicotinic acids, which are widely used to prepare drugs such as nicotinamide (vitamin PP) [9], diethylnicotinamide (cordiamine) [10], isonicotinehydrazide (isoniazide) [11], and others. The structures were modified at the carboxylic groups of the pyridinecarboxylic acids by introducing into them ethanolamine, diethanolamine, trimethylolamine, and several other groups. We surmised that such modification would produce metal complexes with different solubilities in water and membranes. Nitrate and hydroxylamide groups were introduced in order to study the effect of nitric oxide (NO) formed by biotransformation on the antitumor and antimetastatic activity of the Pt(IV) complexes. The biological activity of NO is known to be due to activation of cyclic nucleotides, which determine the functional activity of several organs and tissues and can correct immunity [12 – 14]." @default.
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- W403589225 date "2009-01-01" @default.
- W403589225 modified "2023-09-27" @default.
- W403589225 title "SEARCH FOR NEW DRUGS SYNTHESIS AND ANTIMETASTATIC ACTIVITY OF METAL COMPLEXES BASED ON SUBSTITUTED PYRIDINECARBOXYLIC ACID AMIDES AND PLATINUM TETRACHLORIDE" @default.
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