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In vitro antiproliferative effects, toxicity profiles in vivo in mice and antitumour activity in tumour-bearing mice of five organotin compounds.

Published on Jan 1, 1995in in Vivo 1.61
Marcel Gielen34
Estimated H-index: 34
,
Rudolph Willem38
Estimated H-index: 38
+ 4 AuthorsGodefridus J. Peters63
Estimated H-index: 63
Abstract
The in vitro antiproliferative effects, the toxicity profiles in vivo in mice and the antitumour activity in tumour-bearing mice were screened for five recently synthesized organotin compounds: triphenyltin 5-sulfosalicylate (1), triphenyltin 5-aminosalicylate (2), triphenyltin 4-fluorobenzoate (3), tri-n-butyltin 2,6-difluorobenzoate (4) and di-n-butyltin bis (2,5-dihydroxybenzoate) (5). The in vitro chemosensitivity tests showed that compound 1 has the lowest antiproliferative effect in C26-10. In WiDr, compounds 1 and 5 were less active than the other compounds tested. The IC50 for cisplatin in C26-10 was in the same range as for 1. For compound 3 a steep dose response curve in C26-10 turned out to be remarkably different from the curves of the other compounds. In vivo, compound 1 was most toxic, mainly through paralysis. At their maximum tolerated dose (MTD) for single administration compounds 1, 2, 3 and 4 are inactive against murine colon carcinoma Colon 26. At a single administration, compound 5 was the most active compound with Test/Control ratio (T/C) below 0.6 and Growth Delay Factor (GDF) above 1.0, their respective cut-off levels for sensitivity.
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Published on Jan 1, 2013in Polyhedron 2.28
Hanna Pruchnik10
Estimated H-index: 10
(Wroclaw University of Environmental and Life Sciences),
Małgorzata Latocha12
Estimated H-index: 12
(Medical University of Silesia)
+ 2 AuthorsFlorian P. Pruchnik18
Estimated H-index: 18
(UWr: University of Wrocław)
Abstract Butyltin complexes with 5-sulfosalicylic acid (H 3 ssal) [Sn(C 4 H 9 ) 3 {O 3 SC 6 H 3 (OH)COOH}] ( 1 ), [Sn 2 (C 4 H 9 ) 6 (OOCC 6 H 3 OHSO 3 )] ( 2 ) and [Sn 3 (C 4 H 9 ) 6 (OOCC 6 H 3 (OH)SO 3 ) 2 O] ( 3 ) have been synthesized and characterized by ESI-MS, IR and 1 H, 13 C and 119 Sn NMR spectra. Their structures and properties in solid state and solutions were proposed on the basis of the spectroscopic data and density functional theory (DFT) calculations at B3LYP/3-21G ∗∗ level. Th...
10 Citations Source Cite
Published on Oct 21, 2009in Materials 2.97
Charles E. Carraher24
Estimated H-index: 24
(FAU: Florida Atlantic University),
Michael R. Roner19
Estimated H-index: 19
Organotin polyethers are easily synthesized employing interfacial polymerization systems involving the reaction of hydroxyl-containing Lewis bases and organotin halides. A wide variety of organotin-containing polymeric products have been synthesized including those derived from natural and synthetic polymers such as lignin, xylan, cellulose, dextran, and poly(vinyl alcohol). Others have been synthesized employing known drug diols such as dicumarol, DES, and dienestrol and a wide variety of synth...
24 Citations Source Cite
Published on Aug 1, 2009in Investigational New Drugs 2.66
Biplob Koch17
Estimated H-index: 17
(NEHU: North Eastern Hill University),
Tushar S. Basu Baul23
Estimated H-index: 23
(NEHU: North Eastern Hill University),
Anupam Chatterjee17
Estimated H-index: 17
(NEHU: North Eastern Hill University)
Purpose: A series of diorganotin(IV) dichloride complexes of N-(2-pyridylmethylene)arylamine (nitrogen-chelating ligands) have been synthesized and characterized. The present study was carried out to investigate the comparative anti-proliferative and anti-tumor effect of Me2SnCl2.L1 (OTC-1), Et2SnCl2.L2 (OTC-2) and nBu2SnCl.L2 (OTC-3) in combination with X-rays (1.5 Gy). Method: The cytotoxicity of these diorganotin(IV) compounds was studied in human peripheral lymphocytes and the antitumor acti...
11 Citations Source Cite
Girish Barot11
Estimated H-index: 11
(FAU: Florida Atlantic University),
Michael R. Roner19
Estimated H-index: 19
(UTA: University of Texas at Arlington)
+ 3 AuthorsCharles E. Carraher24
Estimated H-index: 24
(FAU: Florida Atlantic University)
A variety of dibutyltin polyethers have been synthesized employing the interfacial polymerization technique. The products are polymers with degrees of polymerization ranging from 60 to 390. Infrared spectral and mass spectral results are consistent with the proposed structure. The products show good inhibition of a variety of cancer cells including those associated with bone, breast, prostrate, and lung cancers. Some also show good viral inhibition of the HSV-1 (herpes simplex) and Vaccina (smal...
26 Citations Source Cite
Published on May 1, 2008in Journal of Applied Toxicology 3.06
Biplob Koch17
Estimated H-index: 17
(NEHU: North Eastern Hill University),
Tushar S. Basu Baul23
Estimated H-index: 23
(NEHU: North Eastern Hill University),
Anupam Chatterjee17
Estimated H-index: 17
(NEHU: North Eastern Hill University)
Diorganotin(IV) compounds, R2SnCl2 are often tetrahedral, and structurally resemble the active platinum compounds, i.e. cisplatin, and consequently a large number of such complexes have been tested for antitumor activity. A structural correlation with biological activity for diorganotin(IV) complexes has shown that active species are associated with complexes having Sn–N bonds longer than 2.39 A which in turn determines the formation of a tin–DNA complex. In view of these, a series of diorganoti...
30 Citations Source Cite
Girish Barot11
Estimated H-index: 11
(FAU: Florida Atlantic University),
Kimberly Shahi10
Estimated H-index: 10
(UTA: University of Texas at Arlington)
+ 1 AuthorsCharles E. Carraher24
Estimated H-index: 24
(FAU: Florida Atlantic University)
A series of organotin poly(ethylene glycols) were synthesized including the first water soluble organotin polymers. These products are all polymeric with weight average molecular weights about 105. Infrared spectroscopy shows the presence of moieties from both reactants and the formation of the Sn–O linkage. F MALDI MS shows the presence of up to over a hundred units and by isotopic abundance the presence of one, two, and three tin-containing ion fragments. The polymers inhibit the growth of can...
34 Citations Source Cite
Published on Apr 1, 2005in Applied Organometallic Chemistry 3.26
Marcel Gielen34
Estimated H-index: 34
(Vrije Universiteit Brussel),
Monique Biesemans34
Estimated H-index: 34
(Vrije Universiteit Brussel),
Rudolph Willem38
Estimated H-index: 38
(Vrije Universiteit Brussel)
An overview is given of the research performed by the authors at the Universite Libre de Bruxelles and Vrije Universiteit Brussel, including the kinetics, stereochemistry and mechanism of SE2 reactions at a saturated carbon atom, the synthesis of chiral organotin compounds and their configurational and optical stability, the fluxionality of trigonal bipyramidal metal atoms and the stereochemistry of SN2 reactions at tetrahedrally substituted P, Si, Ge, Sn atoms, the cytotoxicity of many series o...
157 Citations Source Cite
Published on Sep 1, 2002in Applied Organometallic Chemistry 3.26
Marcel Gielen34
Estimated H-index: 34
(Free University of Brussels)
An overview of the development of antitumour organotin derivatives is presented and discussed for selected classes of compounds, such as tetraorganodicarboxylatodistannoxanes and related diorganotin dicarboxylates, and for triorganotin carboxylates. Among the carboxylate groups used are steroidcarboxylates and other biologically relevant carboxylates. High to very high in vitro activities have been found, sometimes equalling that of doxorubicin. Solubility in water is an important issue, dominat...
406 Citations Source Cite
Published on Jul 1, 2002in Anti-Cancer Drugs 1.80
Federica Barbieri32
Estimated H-index: 32
,
Maurizio Viale18
Estimated H-index: 18
+ 5 AuthorsAngela Alama20
Estimated H-index: 20
The toxicity and antitumor activity of the novel organotin compound triethyltin(IV)lupinylsul¢de hydrochloride (IST-FS 29), administered by the oral route, have been evaluated against three transplantable murine tumor models: P388 lymphocytic leukemia, B16F10 melanoma and 3LL Lewis lung carcinoma. Mild and reversible signs of acute toxicity such as behavioral symptoms, weight loss and histological alterations were mainly reported at the highest single dose of 28 mg/kg. Conversely, lower concentr...
31 Citations Source Cite
Published on Apr 1, 2000in Journal of Inorganic Biochemistry 3.22
Marcel Gielen25
Estimated H-index: 25
(Vrije Universiteit Brussel),
Monique Biesemans34
Estimated H-index: 34
(Vrije Universiteit Brussel)
+ 1 AuthorsRudolph Willem38
Estimated H-index: 38
(Vrije Universiteit Brussel)
Abstract An overview of the development of anti-tumor organotin derivatives, sometimes as active in vitro as doxorubicin, is presented and discussed. Solubility in water is an important issue, dominating the in vivo testing of compounds with promising in vitro properties. Several water-soluble organotin compounds gave the best in vitro activities. Novel, useful organotin anti-tumor compounds should be designed toward improved water solubility.
157 Citations Source Cite