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Antitumor activity of a new orally active organotin compound: a preliminary study in murine tumor models

Published on Jul 1, 2002in Anti-Cancer Drugs 1.80
· DOI :10.1097/00001813-200207000-00006
Federica Barbieri32
Estimated H-index: 32
,
Maurizio Viale18
Estimated H-index: 18
+ 5 AuthorsAngela Alama20
Estimated H-index: 20
Cite
Abstract
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 concentrations of compound ranging from 7 to 21 mg/kg did not result in major toxic eiects, even after repeated dosing.The antitumor activity studies showed that fractionation dosing, rather than single bolus administration, over 1 week, might prove more active and better tolerated by allowing the achievement of the highest therapeutic total dose of IST-FS 29 (42 mg/kg). Indeed, repeated administrations of IST-FS 29 resulted in marked signi¢cant improvement of antitumor activity against B16F10 (50% of tumor volume inhibition, p 5 0.0003) and, to a greater extent, 3LL (90% of tumor volume inhibition, p 5 0.0001) tumors. These results indicate that IST-FS 29 might be a suitable candidate as an orally administrable anticancer drug and support its further development in human tumor xenografts. [r 2002 Lippincott Williams & Wilkins.]
  • References (16)
  • Citations (31)
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References16
Newest
Published on Mar 1, 2001in Chemico-Biological Interactions 3.41
Federica Barbieri32
Estimated H-index: 32
,
Fabio Sparatore21
Estimated H-index: 21
+ 3 AuthorsAngela Alama20
Estimated H-index: 20
Abstract Organotin compounds, particularly tri-organotin, have demonstrated cytotoxic properties against a number of tumor cell lines. On this basis, triethyltin(IV)lupinylsulfide hydrochloride (IST-FS 29), a quinolizidine derivative, was synthesized and developed as a potential antitumor agent. This tin-derived compound exhibited potent antiproliferative effects on three different human cancer cell lines: teratocarcinoma of the ovary (PA-1), colon carcinoma (HCT-8) and glioblastoma (A-172). Cyt...
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.
Published on Jan 1, 2000in Anticancer Research 1.94
Federica Barbieri32
Estimated H-index: 32
,
Viale M9
Estimated H-index: 9
+ 5 AuthorsAngela Alama20
Estimated H-index: 20
The cytotoxic effect and antitumor activity induced by the novel organotin compound triethyltin(IV)lupinyisulfide hydrochloride, have been investigated. Different patterns of antiproliferative effects have been observed in a panel of human tumor cell lines in vitro. Toxicity studies in mice reported acute toxicity at the doses of 21 and 17.5 mg/kg which progressively disappeared at lower concentrations. On this basis, the doses of 3.5, 7 and 14 mg/kg were selected to assess the antitumor activit...
Published on Apr 1, 1999in Cancer Treatment Reviews 8.33
Jetske M. Meerum Terwogt9
Estimated H-index: 9
(NKI-AVL: Netherlands Cancer Institute),
Jan H. M. Schellens78
Estimated H-index: 78
(NKI-AVL: Netherlands Cancer Institute)
+ 1 AuthorsJos H. Beijnen104
Estimated H-index: 104
(NKI-AVL: Netherlands Cancer Institute)
Abstract In the past years, alternative administration routes and pharmaceutical formulations of anticancer agents have been investigated in order to improve conventional chemotherapy treatment. The impact of these adjustments on the pharmacokinetics and pharmacodynamics is discussed. A review of the literature shows many examples of alternative administration forms of anticancer agents with improved pharmacokinetics. Local administration routes have been investigated in order to reduce the syst...
Published on Aug 1, 1998in Anti-Cancer Drugs 1.80
Monica Cagnoli8
Estimated H-index: 8
,
Angela Alama20
Estimated H-index: 20
+ 3 AuthorsFabio Sparatore21
Estimated H-index: 21
(UniGe: University of Genoa)
Published on Oct 1, 1996in Toxicology and Applied Pharmacology 3.58
Barbara Viviani3
Estimated H-index: 3
(KI: Karolinska Institutet),
Anna D. Rossi8
Estimated H-index: 8
(KI: Karolinska Institutet)
+ 1 AuthorsPierluigi Nicotera82
Estimated H-index: 82
(KI: Karolinska Institutet)
Abstract We have investigated the effects of triethyltin (TET) on agonist-stimulated Ca 2+ signaling and neurosecretion in PC12 cells. Treatment of PC12 cells with 10 μ M TET elicited a slow increase of the resting cytosolic free Ca 2+ concentration due to Ca 2+ release from intracellular stores. Furthermore, TET modified the Ca 2+ responses elicited by bradykinin (Bk), adenosine triphosphate (ATP), or high K + . TET potentiated the peak Ca 2+ response stimulated by Bk in both the presence and t...
Published on May 1, 1996in Oncology Reports 3.04
Marcel Gielen34
Estimated H-index: 34
(UvA: University of Amsterdam),
Rudolph Willem38
Estimated H-index: 38
(UvA: University of Amsterdam)
+ 4 AuthorsG. Peters1
Estimated H-index: 1
(UvA: University of Amsterdam)
The in vitro antiproliferative effects, the in vivo toxicity profiles in mice and the antitumour activity in tumour bearing mice were screened for four novel di-n-butyltin carboxylates, di-n-butyltin bis(2,4-dihydroxybenzoate) [compound 1 (C1)], di-n-butyltin bis(2,5-dihydroxybenzoate) (C2), di-n-butyltin bis(pentafluorophenylacetate) (C3), and bis[di-n-butyl(pentafluorophenylacetato)tin] oxide (C4). All compounds revealed similar in vitro chemosensitivities in two cell lines, C26-10 and C26-A, ...
Published on Jan 1, 1996in Drugs of The Future 0.10
J. Respondek1
Estimated H-index: 1
,
J. Engel1
Estimated H-index: 1
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
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...
Published on Aug 1, 1993in Farmaco
Novelli F1
Estimated H-index: 1
,
Sparatore F1
Estimated H-index: 1
Cited By31
Newest
Published on May 1, 2019in Journal of Photochemistry and Photobiology B-biology 4.07
Muhammad Sirajuddin13
Estimated H-index: 13
(University of Science and Technology),
Saqib Ali29
Estimated H-index: 29
(QAU: Quaid-i-Azam University)
+ 3 AuthorsAbdul Wadood19
Estimated H-index: 19
(AWKUM: Abdul Wali Khan University Mardan)
Abstract In the search for new therapeutic agents we have synthesized 13 new organotin(IV) carboxylate derivatives of ( E )-4-((4-methoxy-2-nitrophenyl)amino)-4-oxobut-2-enoic acid. The synthesized complexes were characterized by several spectroscopic techniques. A chelating or bridging bidentate nature of the carboxylate ligand was suggested from the solid state FT-IR results. Solution state multinuclear NMR ( 1 H, 13 C and 119 Sn) results reveal that the geometry around the Sn atom in triorgan...
Published on Mar 9, 2019in International Journal of Molecular Sciences 4.18
Hunáková L14
Estimated H-index: 14
,
Eva Horváthová18
Estimated H-index: 18
+ 3 AuthorsJulius Brtko17
Estimated H-index: 17
The cytotoxicity of two recently synthesized triorganotin isothiocyanate derivatives, nuclear retinoid X receptor ligands, was tested and compared in estrogen-receptor-positive MCF 7 and -negative MDA-MB-231 human breast carcinoma cell lines. A 48 h MTT assay indicated that tributyltin isothiocyanate (TBT-ITC) is more cytotoxic than triphenyltin isothiocyanate (TPT-ITC) in MCF 7 cells, and the same trend was observed in the MDA-MB-231 cell line. A comet assay revealed the presence of both crossl...
Published on Jan 17, 2019in Journal of Chemistry 1.73
Nebojša Pantelić4
Estimated H-index: 4
(University of Belgrade),
Bojana B. Zmejkovski7
Estimated H-index: 7
(University of Belgrade)
+ 4 AuthorsGoran N. Kaluđerović8
Estimated H-index: 8
A novel triphenyltin(IV) compound with 1-(4-carboxyphenyl)-3-ethyl-3-methylpyrrolidine-2,5-dione was synthesized and characterized by IR, NMR spectroscopy, mass spectrometry, and elemental analysis. In vitro anticancer activity of ligand precursor and synthesized organotin(IV) compound was determined against tumor cell lines: human adenocarcinoma (HeLa), human myelogenous leukemia (K562), and human breast cancer (MDA-MB-453), using microculture tetrazolium test (MTT) assay. The results indicate ...
Published on Oct 18, 2018in Journal of Coordination Chemistry 1.69
Niaz Muhammad17
Estimated H-index: 17
(AWKUM: Abdul Wali Khan University Mardan),
Naseer Ali Shah15
Estimated H-index: 15
(CUI: COMSATS Institute of Information Technology)
+ 6 AuthorsAuke Meetsma55
Estimated H-index: 55
(UG: University of Groningen)
AbstractFour new diorganotin(IV) carboxylates, [n-Bu2SnL2] (1), [Et2SnL2] (2), [Me2SnL2] (3) and [n-Oct2SnL2] (4), where L = 3-(4-chlorophenyl)-2-methylacrylate, were synthesized and characterized by elemental analysis, FT-IR, multinuclear NMR (1H, 13C, and 119Sn) and X-ray single crystal analysis for 1. A chelating bidentate ligand and six-coordinate tin centers were confirmed in the solid state by IR for all complexes and for 1 by X-ray single crystal analysis. The NMR study has shown a decrea...
Published on May 1, 2018in Inorganic Chemistry Communications 1.79
Jai Devi5
Estimated H-index: 5
(Guru Jambheshwar University of Science and Technology),
Sushila Pachwania1
Estimated H-index: 1
(Guru Jambheshwar University of Science and Technology)
Abstract DNA interaction studies of organotin(IV) complexes have got tremendous attention during the recent years due to their anticancer and antitumor properties. Most of the chemotherapeutic organotins are DNA-targeted as they recognize specific DNA sequences, alter the local DNA structure, inhibit access to the activator or repressor protein and ultimately affect the gene expression process. The binding ability of organotin(IV) compounds with DNA depends on the coordination number and the nat...
Published on Sep 1, 2017in Toxicology Letters 3.50
Hunáková L14
Estimated H-index: 14
(SAV: Slovak Academy of Sciences),
Julius Brtko17
Estimated H-index: 17
(SAV: Slovak Academy of Sciences)
Abstract Among a variety of metal containing organic compounds, tin derivatives are enjoying an increasing interest and appear to be very promising as potential drug candidates. We studied eight organometallic derivatives, nuclear retinoid X receptor (RXR) ligands and two germanium containing derivates that do not serve as RXR ligands. Tributylgermanium chloride (TBGe) and triphenylgermanium chloride (TPGe) did not inhibit growth of human triple negative MDA-MB-231 breast cancer cells. On the ot...
Published on Jan 1, 2017in Journal of Inorganic Biochemistry 3.22
Tushar S. Basu Baul23
Estimated H-index: 23
(NEHU: North Eastern Hill University),
Dhrubajyoti Dutta3
Estimated H-index: 3
(NEHU: North Eastern Hill University)
+ 6 AuthorsSunil K. Manna17
Estimated H-index: 17
(Centre for DNA Fingerprinting and Diagnostics)
Abstract Synthesis and spectroscopic properties of seven new dibutyltin(IV) compounds of 2-{( E )-4-hydroxy-3-[( E )-4-(aryl)iminomethyl]phenyldiazenyl}benzoic acids (L n HH′; n = 2–8) with general formula {[Bu 2 Sn(L n H)] 2 O} 2 ( 1 – 7 ) are reported. The compounds were characterized by elemental analysis and by UV–Visible, fluorescence, IR, 1 H, 13 C and 119 Sn NMR spectroscopies. Solid state structures of dibutyltin(IV) compounds 1 – 3 , 6 and 7 were accomplished from single crystal X-ray c...
Published on Nov 1, 2015in Inorganica Chimica Acta 2.43
Leila Tabrizi11
Estimated H-index: 11
(IUT: Isfahan University of Technology),
Patrick McArdle25
Estimated H-index: 25
(National University of Ireland, Galway)
+ 1 AuthorsHossein Chiniforoshan11
Estimated H-index: 11
(IUT: Isfahan University of Technology)
We are grateful for the financial support from the Department of Chemistry, Isfahan University Of Technology (IUT).
Published on Apr 1, 2015in Toxicology Letters 3.50
Julius Brtko17
Estimated H-index: 17
(SAV: Slovak Academy of Sciences),
Zdenek Dvorak29
Estimated H-index: 29
(Palacký University, Olomouc)
Abstract We review trialkyltin and triaryltin compounds, representing a class of organometallic compounds that function as nuclear retinoid X receptors (RXR) agonists due to their capability to bind to the ligand-binding domain of RXR subtypes and function as transcriptional activators. RXRs act predominantly as heterodimers with other nuclear receptors as permissive heterodimers with peroxisome proliferator-activated receptors, liver X receptors, farnesoid X receptor, pregnane X receptor and co...
Published on Oct 1, 2014in European Journal of Medicinal Chemistry 4.83
Min Hong14
Estimated H-index: 14
(Liaocheng University),
Honglin Geng2
Estimated H-index: 2
(Liaocheng University)
+ 4 AuthorsHandong Yin14
Estimated H-index: 14
(Liaocheng University)
Abstract Five organotin(IV) compounds were synthesized from N′-[(1E)-(2-hydroxy-3-methoxyphenyl)methylidene]pyridine-4-carbohydrazone and the corresponding dialkyltin(IV) or trialkyltin(IV) precursor. Solid state structures were determined by IR, elemental analysis, NMR spectroscopy, and for 1 , 2 , 4 and 5 single crystal X-ray diffraction analysis. Compounds 1 , 2 and 4 are monomers with the tin atoms five-coordinated in distorted trigonal bipyramid, of which the deprotonated Schiff base ligand...