In vitro antitumour activities of a novel 2:3 condensation product of salicylaldoxime with di‐n‐butyltin(IV) oxide

Abstract

AbstractThe antitumor activities of three novel condensation products of salicylaldoxime with di‐n‐butyltin(IV) oxide (compound 1), di‐t‐butyltin oxide (compound 2) and diphenyltin oxide (compound 3) are presented. Against MCF‐7, a human mammary tumor cell line, compounds 1 and 2 are characterized by inhibition doses ID50 in vitro of 67 and 49 ng cm−3 respectively, whereas cis‐platin, an antitumor drug used clinically, has an ID50 of 850 ng cm−3. Against WiDr, a colon carcinoma, they also score better than cis‐platin: 215 and 121 ng cm−3 versus 624 ng cm−3. In contrast, the diphenyltin compound, 3, is inactive against both tumor cell lines.The results of a pre‐screening performed on compound 1 by the National Cancer Institute (NCI) on a panel of 60 human tumor cell lines show that two of the selectivity parameters calculated by the NCI for that compound are statistically significant, namely DG150 (51.9>50) and MGDH (80.1>75). One is almost satisfactory (DH = 72.4 = ca75). The other two, DTGI (40.0<50) and DLC50 (16.7<50) are not. (Abbreviations are explained in the text and in Gielen, M. and Willem, R. Anticancer Res., 1992, in press).