Abstract
Six mercapto-quinoline derivatives have been tested on « in vitro » cultures of KB cells at concentrations ranging from 0.1 γ/ml to 50 γ/ml. Three of them, i. e. No. 1 (4-mercapto-2-methyl-quinoline), No. 2 (6-methoxy-4-mercapto-2-methyl-quinoline) and No. 4 (8-methoxy-4-mercapto-2-methyl-quinoline) showed interesting anticellular activities consisting in:
1) antimitotic action: compounds No. 1 and No. 2 cause principally a methaphase block with colchicine-like effect; compound No. 4 shows a clear inhibiting action of preprophasic type.
2) aspecific and late cytotoxic action: more or less common to the three derivatives, it causes severe cell damage.
The most active of these three compounds was found to be No. 2. On the other hand three other compounds: 7-methoxy-4. thio-2. methylcholine; acid (6-methoxy-2-methyl-quinoline-4) thioglycolic; 6. ethoxy-4. thio-2. methylcholine, proved inactive.
It is concluded that these mercapto-quinoline compounds, require, to be active, the presence of a free sulfhydryl group in their molecule.
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