Danièle De Vos

Synthesis, characteristic spectral studies and in vitro antimicrobial and antitumour activities of organotin(IV) complexes of Schiff bases derived from amino-acids

Equimolar reactions of dibutyltin(IV) oxide with Schiff bases derived from amino-acids led to the formation of a new series of dibutyltin(IV) complexes of general formula, Bu2SnL [L=dianion of tridentate Schiff bases derived from the condensation of 2-hydroxy-1-naphthaldehyde or acetyl acetone with glycine (L-1), L-β-alanine (L-2), DL-valine (L-3), DL-4-aminobutyric acid (L-4), L-methionine (L-5), L-leucine (L-6) and phenylglycine (L-7)]. An attempt has been made to prove the structures of the resulting complexes on the basis of elemental analyses, conductance measurements and electronic, IR, multinuclear magnetic resonance (1H, 13C and 117Sn) and 119Sn Mossbauer spectral studies. The complexes have been tested against various bacteria [Streptococcus faecalis, Klebsiella pneumoniae, Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus penicillin resistance (2500 units)] and fungi (Candida albicans, Cryptococcus neoformans, Sporotrichum schenckii,Trichophyton mentagrophytes and Aspergillus fumigatus). All the complexes showed moderate activity. The cytotoxicity of a few compounds has been screened in vitro against seven human tumour cell lines, viz. MCF-7, EVSA-T, WiDr, IGROV, M19 MEL, A498 and H226. The activities found experimentally were better than those obtained for cisplatin and carboplatin

Synthesis, Characterization and In Vitro Antitumour Activity of Di-n-Butyl, Tri-n-Butyl and Triphenyltin 3,6-Dioxaheptanoates and 3,6,9-Trioxadecanoates.

A series of di- and triorganotin 3,6-dioxaheptanoates and 3,6,9-trioxadecanoates were synthesized and characterized by 1H, 13 and 117Sn NMR, electrospray mass and 119mSn Mössbauer spectroscopy, as well as elemental analysis. Their in vitro antitumour activity against seven tumoural cell lines of human origin, two breast cancers (MCF-7, EVSA-T), a colon carcinoma (WiDr), an ovarian cancer (IGROV), a melanoma (M 19 MEL), a renal cancer (A 498) and a non small cell lung cancer (H 226), is reported. They are characterized by similar inhibition doses ID50 as the analogous di- and triorganotin derivatives of 4-carboxybenzo-15-crown-5 and -18-crown-6 and in some cases by much lower ID50 values than clinically used reference compounds such as doxorubicine and methotrexate.

Organotin(IV) derivatives of 3,4-(methylenedioxy)phenylacetic acid: Synthesis, spectroscopic characterization and in vitro antitumour properties

The triphenyltin and tri-n-butyltin 3,4-(methylenedioxy)phenylacetates as well as the tetra-n-butylbis[3,4-(methylenedioxy)phenylacetato]distannoxane dimer have been synthesized and characterized by H-1, C-13, Sn-117 NMR, Sn-119m Mossbauer and mass spectroscopy. The compounds have been screened against a panel of tumour cell lines of human origin.

Di‐ and tri‐organotin derivatives of 3S,4S‐3‐[(R)‐1‐(tert‐butyl‐dimethylsilyloxy)ethyl]‐4‐[(R)‐1‐carboxyethyl]‐2‐azetidinone: synthesis, characterization and in vitro antitumour activity

Di-n-butyl-, triphenyl and tri-n-butyltin derivatives of 3S,4S-3-[(R)-1-(tert-butyldimethylsilyloxy)ethyl-4-[(R)-1-carboxyethyl]-2-azetidinone were synthesized and characterized. Their antitumour activity was screened against seven tumoural cell lines of human origin. Copyright (C) 1999 John Wiley & Sons, Ltd.

Synthesis, Characterization and Antitumour Activity of Di-n-Butyltin Salicyloxamate

The synthesis and characterization of di-n-butyltin and dimethyltin salicyloxamate, respectively compounds 1 and 2, are reported. Compound 1 is more active than cisplatin, 5-fluorouracil and etoposide against seven tumoural cell lines of human origin, but less active than methotrexate and doxorubucin. Diorganotin derivatives of salicylic acid and its substituted analogs exhibit antitumour activities in vitro against human tumoural cell lines 1,2. The phenolic hydroxy group of salicylic acid is not involved in its reaction with diorganotin oxides3,4. In fact, salicylic acid behaves in this respect as benzoic acid, giving rise to diorganotin disalicylates with free hydroxy groups. This report presents the synthesis and characterization of di-n-butyltin and dimethyltin salicyloxamate, respectively compounds 1 and 2, in order to find out whether the phenolic hydroxy group of salicyloxamic acid is involved when reacting with diorganotin oxides. The antitumour activity of compound 1 was determined for comparison with that of the corresponding di-n-butyltin salicylate5.