Abdelaziz El Khloufi

(2-Methylthio-3-Pyridinecarboxylato)-diethyltin and -di-n-butyltin compounds: synthesis, spectroscopic characterization and in vitro antitumour activity. X-ray crystal structure of bis[diethyl(2-methylthio-3-Pyridinecarboxylato)tin] oxide and of diethyltin bis(2-methylthio-3-pyridinecarboxylate)

The X-ray crystal structures of [diethyl(2-methylthio-3-pyridinecarboxylato)tin] oxide (1a) and diethyltin bis(2-methylthio-3-pyridinecarboxylate) (1b) were determined. Compound 1a is a centrosymmetric dimer with two distinct types of carboxylate moieties and tin atoms with trigonal bipyramidal geometries. Compound 1b is monomeric with a six-coordinate tin atom and two equivalent carboxylate groups chelating the tin atom. Compounds 2a and 2b, the di-n-butyl analogues of 1a and 1b, have also been synthesized and characterized spectroscopically. The in vitro activity of compounds 2b and 2a against the human tumour cell line WiDr, a colon carcinoma, is better than that of cis-platin and doxorubicin. They are much less active than doxorubicin against MCF-7, a mammary tumour cell line. Compound 1b is inactive.

Diorganotin difluorobenzoates: synthesis, spectroscopic characterization and in vitro antitumour activity. X-Ray structure determination of bis[di-n-butyl(2,6-difluorobenzoato)tin] oxide

The synthesis and spectroscopic characterization of diorganotin(IV) bis(difluorobenzoates) [F2C6H3COO]2SnR2 [type a] and bis[diorgano(difluorobenzoato)tin(IV)] oxides {[(F2C6H3COO)R2Sn]2O}2 [type b] are described. An X-ray structure study has revealed compound 3b, {[(2,6-F2C6H3COO)(n-C4H9)2Sn]2O}2, to be dimeric and built around a planar Sn2O2 ring. The crystals are triclinic P1BAR with the cell dimensions a=11.935(13), b=12.3675(14), c=12.974 angstrom, alpha=92.89(8), beta=84.32(7), gamma=67.49(9)-degrees; Z=1, with the dimer being centro-symmetric. Selected compounds have been tested in vitro against two human tumour cell lines, MCF-7 (a mammary tumour) and WiDr (a colon carcinoma), and exhibit promising cytotoxicities.

Synthesis, characterization and high in vitro antitumour activity of novel triphenyltin carboxylates.

The synthesis and spectral characterization of six novel triphenyltin compounds are described. The in vitro antitumour activity of three of these compounds against two human tumour cell lines, MCF-7, a mammary tumour, and WiDr, a colon carcinoma, was determined. All three compounds are more active than cis-platin, etoposide and doxorubicin against both tumour cell lines. They are as active as mitomycin C against WiDr, but less active against MCF-7.