444 research outputs found
Tin-based Antitumour Drugs
Journal Articleinfo:eu-repo/semantics/publishe
Tin-Based Antitumour Drugs: New Developments
An overview of the in vitro test results on several human tumour cell lines of several series of
organotin compounds synthesized at the Free University of Brussels VUB. Several compounds
exhibit excellent antitumour activities. in vivo screening also gave very promising results
Synthesis, Characterization and Antitumour Activity of Di-n-Butyltin Salicyloxamate
Journal Articleinfo:eu-repo/semantics/publishe
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
Di-n-Butyl-, Tri-n-Butyl- and Triphenyltin dl-Terebates: Synthesis, Characterization and In Vitro Antitumour Activity
Di-n-butyltin, tri-n-butyltin and triphenyltin terebates were screened against several human tumour cell lines and found comparably or more active than carboplatin, cis-platin, 5-fluorouracil, methotrexate and doxorubicin, some reference compounds used clinically
The Development of Novel Organotin Anti-Tumor Drugs: Structure and Activity
An overview of the development of anti-tumor organotin derivatives in selected classes of
compounds is presented and discussed. High to very high in vitro activity has been found,
sometimes equaling that of doxorubicin. Solubility in water is an important issue, dominating
the in vivo testing of compounds with promising in vitro properties.
The cytotoxicity of the compounds was increased by the presence of a bulky group, an active substituent or one or
more polar substituents. Polar substituents may also improve the water solubility. Although
organotin derivatives constitute a separate class of compounds, the comparison with cisplatin
is inevitable. Among the observed toxicities, neurotoxicity, known from platinum cytostatics,
and gastrointestinal toxicity, typical for many oncology drugs, have been detected. Further
research to develop novel, useful organotin anti-tumor compounds should be carried out
Synthesis, Characterization and Antitumour Activities of Di-n-Butyl- and Dimethyltin D-(+)-Camphorates
Journal Articleinfo:eu-repo/semantics/publishe
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
X-Ray Structure and In Vitro Anti-Tumoural Activity of the Dimeric Bis[(2-Phenyl-1,2-Dicarba-Closo-Dodecaborane-1-Carboxylato)-Di-n-Butyltin] Oxide
X-ray diffraction studies reveal the structure of {[(2-C6H5-1,2-C2B10H10-1-COO)Bu2Sn]2O}2, 1, to conform to the common motif found for {[(R′COO)R2Sn]2O}2 compounds. The dimer features a central Bu2Sn2O2 unit (two-fold symmetry) with the two Bu2Sn groups being linked via bridging oxygen atoms, each of which also carries an exocyclic Bu2Sn moiety. The two pairs of exo- and endo-cyclic tin atoms are each linked via an almost symmetrically bridging carboxylate ligand and the two remaining ligands coordinate an exocyclic tin atom only, in the monodentate mode. The in vitro anti-tumour activity of 1, determined against a variety of cell lines, is compared with those of the corresponding 2-methylcarboranylacetate, derivative 2, and with clinically used compounds
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