Complexes of ruthenium(III) with some 2-aminothiazole derivatives/synthesis, properties and pharmacological studies.
Four new complexes of Ru(III) with a general formula [Ru(L)2Cl2]Cl, where L = 2-amino-4-phenylthiazole (CAS 2010-06-2), 2-amino-4-methylthiazole (CAS 1603-91-4), ethyl 2-amino-4-methyl-5-thiazolecarboxylate (CAS 7210-76-6) and ethyl 2-amino-4-phenyl-5-thiazolecarboxylate (CAS 64399-23-1), were prepared. The syntheses were carried out in polar medium and inert atmosphere at a molar ratio Ru:L = 1:2 or 1:3. The compounds obtained were characterised by IR-, 1H-NMR- 13C-NMR-, UV-VIS-, EPR spectroscopy, magnetochemical and conductivity measurements. The ligands behaved as bidental, bounding Ru(III) through the nitrogen atoms from the amino group and the heterocycle. The complex of ethyl 2-amino-4-phenyl-5-thiazolecarboxylate showed significant antileukaemic activity on various human cells (IC50 values ranging from 20 to 92 micromol/l). Toxicological studies on mice indicated that such concentrations could be reached without mortality. This compound exhibited a promising antineoplastic potential and needs further pharmacological and toxicological evaluation.
Faculty of Pharmacy, Medical University, Sofia, Bulgaria.
Antonina
A
Nikolova
Darvin
D
Ivanov
Panayot
P
Bontchev
Rossen
R
Buyukliev
Dimitar
D
Mehandjiev
Georgi
G
Gochev
Spiro
S
Konstantinov
Margarita
M
Karaivanova
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D004578:Electron Spin Resonance Spectroscopy; D006801:Humans; D007202:Indicators and Reagents; D007928:Lethal Dose 50; D008024:Ligands; D009682:Magnetic Resonance Spectroscopy; D012428:Ruthenium / Q000737:chemistry*; D013055:Spectrophotometry, Infrared; D013696:Temperature; D013778:Tetrazolium Salts; D013844:Thiazoles / Q000138:chemical synthesis* / Q000494:pharmacology
D000970:Antineoplastic Agents; D007202:Indicators and Reagents; D008024:Ligands; D013778:Tetrazolium Salts; D013844:Thiazoles; D012428:Ruthenium; C022616:thiazolyl blue