DNA binding and in vitro antileukemic activity of dimeric and tetrameric platinated complexes derived from p-isopropylbenzaldehyde thiosemicarbazone
✍ Scribed by Adoración G. Quiroga; José M. Pérez; Carlos Alonso; Carmen Navarro-Ranninger
- Publisher
- John Wiley and Sons
- Year
- 1998
- Tongue
- English
- Weight
- 90 KB
- Volume
- 12
- Category
- Article
- ISSN
- 0268-2605
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✦ Synopsis
p-Isopropylbenzaldehyde thiosemicarbazone (pis.TSCN) (1) reacts with [Pt(m-Cl)(h 3 -C 4 H 7 )] 2 to form a dinuclear [Pt(m-Cl)(p-is.TSCN)] 2 complex (2) and a cyclometallated cluster [Pt(pis.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 IC 50 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.