In vitro antiproliferative activity of 2'-(2-hydroxyphenyl)-2'-thiazoline-4'-carboxylic acid and its methyl ester on L1210 and P388 murine neoplasms.
The activity of three iron chelators, methyl [2'-(2-hydroxyphenyl)-2'-thiazoline-4'-carboxylate] (MTL); 2'-(2-hydroxyphenyl)-2'-thiazoline-4'-carboxylic acid (TFAL); and 2-hydroxyphenyl-imido-ethyl-ether (Imidate), regarding antiproliferative, cytocidal, and cell-cycle effects are reported and compared with hydroxyurea (HU). In vitro, against L1210 and P388 murine neoplasms, MTL and TFAL displayed substantially greater antiproliferative activity than HU, although Imidate displayed no appreciable activity. MTL also induced a statistically more complete G1/S cell-boundary block than did HU at equimolar concentrations (100 microM). The IC50 values produced by MTL and TFAL were low enough (less than or equal to 20 microM) to warrant further testing of these chelators as potential antineoplastic agents.
Elliot
G T
GT
Department of Biopharmaceutical Sciences, University of Arkansas for Medical Sciences, Little Rock 72205.
Kelly
K F
KF
Bonna
R L
RL
Wardlaw
T R
TR
Burns
E R
ER
D000818:Animals; D002453:Cell Cycle / Q000187:drug effects; D002455:Cell Division / Q000187:drug effects; D003864:Depression, Chemical; D006918:Hydroxyurea / Q000494:pharmacology; D007094:Imides / Q000494:pharmacology*; D007939:Leukemia L1210 / Q000473:pathology*; D007941:Leukemia P388 / Q000473:pathology*; D007942:Leukemia, Experimental / Q000473:pathology*; D051379:Mice; D013844:Thiazoles / Q000494:pharmacology*; D014407:Tumor Cells, Cultured / Q000187:drug effects
D007094:Imides; D013844:Thiazoles; C055756:methyl-(2'-(2-hydroxyphenyl)-2'-thiazoline-4'-carboxylate); C055757:2-hydroxyphenyl-imido-ethylether; C055755:2'-(2-hydroxyphenyl)-2'-thiazoline-4'-carboxylic acid; D006918:Hydroxyurea