ISSN:
0268-2605
Keywords:
platinum compound antileukaemic
;
cytotoxic
;
DNA
;
thiosemicarbazone
;
Chemistry
;
Industrial Chemistry and Chemical Engineering
Source:
Wiley InterScience Backfile Collection 1832-2000
Topics:
Chemistry and Pharmacology
Notes:
p-Isopropylbenzaldehyde thiosemicarbazone (p-is.TSCN) (1) reacts with [Pt(µ-Cl)(η3-C4H7)]2 to form a dinuclear [Pt(µ-Cl)(p-is.TSCN)]2 complex (2) and a cyclometallated cluster [Pt(p-is.TSCN)]4 (3). Biological testing of these complexes against HL-60 and U-937 human leukemic cells suggest that complexes 2 and 3 may be endowed with important cytotoxic activity properties since they exhibit IC50 values (50% inhibition of cell growth) in the micromolar range, as does the clinically used drug cisplatin (cis-DDP). Analysis of the interaction of compounds 2 and 3 with DNA indicates that the kinetics of DNA platination due to compounds 2 and 3 is faster than that of cisplatin and that after 24 h of incubation most of the platinum centers are bound to DNA. Thus, it is likely that the cytotoxic activity displayed by compounds 2 and 3 may be correlated with their high level of DNA platination. Copyright © 1998 John Wiley & Sons, Ltd.
Additional Material:
1 Ill.
Type of Medium:
Electronic Resource
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