CYTOTOXIC DI(8-QUINOLYL) DISULFIDES

Abstract

It has been shown that the nature of  the  substituent and its position in the quinoline ring markedly affects the antitumor activity and  toxicity  of  di(8-quinolyl) disulfides. The greatest cytotoxicity in the series of methyl derivatives was shown by the 7-, 6-, and 3- isomers towards HT-1080  (human fibrosarcoma) and MG-22A (mouse hepatoma) tumor cells while the 2-methyl derivatives generally have no effect on these cells. High cytotoxicity was also shown (LC50 <1  µg/ml) by other 7- substituted compounds (Cl, PhO, PhS) but they also appear to be highly toxic  towards  normal NIH  3Y3  mouse embryonic fibroblasts. A similar trend was observed in the series of 5- substituted compounds (NH2, Cl, OMe, NO2) which were highly active towards tumor cells but were toxic to normal cells. The best selectivity was found for the 6- substituted quinolines, the 6-methoxy derivative at low concentration brought about the death of tumor cells but appeared much less toxic towards normal fibroblasts (LC50 100 µg/ml with a corresponding LD50 of 874 mg/kg ).

How to Cite
Lukevics, E.; Shestakova, I.; Domracheva, I.; Yashchenko, E.;  Zaruma, D.; Ashaks, J.  Chem. Heterocycl. Compd. 2007, 43, 629. [Khim. Geterotsikl. Soedin. 2007, 750.]

For this article in the English edition see DOI 10.1007/s10593-007-0097-7