In vitro antiproliferative activity of 2'-(2-hydroxyphenyl)-2'-thiazoline-4'-carboxylic acid and its methyl ester on L1210 and P388 murine neoplasms

• Published in: Cancer chemotherapy and pharmacology Vol. 21; no. 3; pp. 233 - 236
• Main Authors: ELLIOT, G. T, KELLY, K. F, BONNA, R. L, WARDLAW, T. R, BURNS, E. R
• Format: Journal Article
• Language: English
• Published: Berlin Springer 01-05-1988
• Subjects: Animals; Antineoplastic agents; Biological and medical sciences; Cell Cycle - drug effects; Cell Division - drug effects; Depression, Chemical; General aspects; Hydroxyurea - pharmacology; Imides - pharmacology; Leukemia L1210 - pathology; Leukemia P388 - pathology; Leukemia, Experimental - pathology; Medical sciences; Mice; Pharmacology. Drug treatments; Thiazoles - pharmacology; Tumor Cells, Cultured - drug effects; Antineoplastic agent; Cell culture; Flow cytometry; P388»-Leukemia; Chelating agent; L1210-Leukemia; In vitro; Biological activity
• ISSN: 0344-5704; 1432-0843
• DOI: 10.1007/BF00262776

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.