Antileukemic activity of 4-pyranone derivatives.
In a search for new compounds possessing antitumor activity, we examined the effects of a group of oxygen containing heterocyclic derivatives on L1210 murine leukemia cell growth. Several 5-hydroxy-2-hydroxymethyl-4-pyranone derivatives were tested in a growth assay employing a human leukemia K562 cells line. IC50 was extrapolated from the growth inhibition curves at compound concentrations ranging from 0.1 to 100 microM. The halogen derivatives of 5-hydroxy-2-hydroxymethyl-4-pyranone inhibited L1210 cell growth in suspension culture after 96 hr incubation in the following order: 5-hydroxy-2-iodomethyl-4-pyranone (IC50 3.15 microM) > 6-bromo-2-bromomethyl-5-hydroxy-4-pyranone (IC50 3.40 microM) > 6-bromo-5-hydroxy-2-hydroxy-methyl-4-pyranone (IC50 3.75 microM) > 2-bromomethyl-5-hydroxy-4-pyranone (IC50 4.30 microM) > 5-benzyloxy-2-chloromethyl-4-pyranone (IC50 5 microM) > 6-bromo-2-chloromethyl-4-pyranone (IC50 13.50 microM) > 6-chloro-2-chloromethyl-5-hydroxy-4-pyranone (IC50 18 microM) > 2-chloromethyl-5-hydroxy-4-pyranone (IC50 20 microM). The compound, 5-hydroxy-2-hydroxymethyl-4-pyranone has no effect on L1210 cell growth. These results suggest that 5-hydroxy-2-hydroxymethyl-4-pyranone derivatives might represent a new class of compounds with antileukemic activity.
Bransová
J
J
Institute of Experimental Endocrinology, Slovak Academy of Sciences, Bratislava.
Brtko
J
J
Uher
M
M
Novotný
L
L
D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D002452:Cell Count / Q000187:drug effects; D002455:Cell Division / Q000187:drug effects; D006571:Heterocyclic Compounds / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D007938:Leukemia / Q000473:pathology*; D007939:Leukemia L1210; D051379:Mice; D015394:Molecular Structure; D011753:Pyrones / Q000737:chemistry / Q000494:pharmacology*; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D006571:Heterocyclic Compounds; D011753:Pyrones