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2-[(Aminopropyl)amino]ethanethiol (WR1065) is anti-neoplastic and anti-mutagenic when given during 60Co gamma-ray irradiation.

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We have studied the effect of 2-[(aminopropyl)amino]ethanethiol (WR1065) on the induction of neoplastic transformation using 10T1/2 cells and on mutation at the hypoxanthine guanine phosphoribosyl transferase (HGPRT) locus using Chinese hamster V79 cells. Here we report the first observations that

Protection against cis-diamminedichloroplatinum cytotoxicity and mutagenicity in V79 cells by 2-[(aminopropyl)amino]ethanethiol.

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The effect(s) of the radioprotector 2-[(aminopropyl)amino]ethanethiol (WR1065) on cis-diamminedichloroplatinum(II) (cis-DDP)-induced cytotoxicity and mutagenesis at the hypoxanthineguanine phosphoribosyl transferase locus in V79 Chinese hamster cells was examined. With a standard exposure time of 30

Protective effects of 2-[(aminopropyl)amino] ethanethiol against bleomycin and nitrogen mustard-induced mutagenicity in V79 cells.

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This study examines the effects of the radioprotector 2-[(aminopropyl)amino] ethanethiol (WR-1065) on bleomycin (BLM) and nitrogen mustard- (HN2) induced cytotoxicity, DNA damage, and mutagenesis at the hypoxanthine-guanine phosphoribosyl transferase (HGPRT) locus in V79 Chinese hamster cells. The

Kinetics of cisplatin binding to cellular DNA and modulations by thiol-blocking agents and thiol drugs.

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DNA platination by cisplatin (CDDP) was investigated in peripheral blood mononuclear cells and ovarian cancer cells using atomic absorption spectroscopy. Plots showing the amount of platinum (Pt) bound to DNA versus the molar concentration of cisplatin in the incubation medium ([CDDP]) were

'3+1' mixed-ligand oxotechnetium(V) complexes with affinity for melanoma: synthesis and evaluation in vitro and in vivo.

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'3+1' Mixed-ligand [(99m)Tc]oxotechnetium complexes with affinity for melanoma were synthesized in a one-pot reaction. Complexation of technetium-99m with a mixture of N-R(3-azapentane-1,5-dithiol) [R = Me, Pr, Bn, Et(2)N(CH(2))(2)] and N-(2-dialkylamino)ethanethiol [alkyl = X = Et, Bu, morpholinyl]

A molecular CT blood pool contrast agent.

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OBJECTIVE A molecular-based computed tomographic (CT) contrast agent with prolonged vascular residence time is needed for vascular and tumor imaging. No particulate agents have reached clinical practice due to nonspecific macrophage activation. The authors' objective was to synthesize a

Analysis of proteins in biological samples by capillary sieving electrophoresis with postcolumn derivatization/laser-induced fluorescence detection.

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Previously, we have demonstrated postcolumn derivatization of proteins separated by capillary sieving electrophoresis (CSE), in which naphthalene-2,3-dicarbaldehyde was employed as a fluorogenic labeling reagent. Standard proteins separated by CSE were reacted with naphthalene-2,3-dicarbaldehyde in

Pharmacokinetic profile of amifostine.

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This article reviews the chemistry, measurement, metabolism, and pharmacokinetics of the cytoprotective agent amifostine. Validated analytic methodology to measure parent drug and pharmacologically active metabolites and pharmacokinetic studies are essential to the efficient performance and analysis

Amifostine: chemotherapeutic and radiotherapeutic protective effects.

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Amifostine (Ethyoltrade mark, Alza Pharmaceuticals) is an inorganic thiophosphate cytoprotective agent known chemically as ethanethiol, 2-[3- aminopropyl)amino]dihydrogen phosphate. It is a prodrug of free thiol (WR-1065) that may act as a scavenger of free radicals generated in tissues exposed to

Time dependence of the selective modulation of cisplatin-induced nephrotoxicity by WR2721 in the mouse.

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2-(3-Aminopropylamino)ethylphosphorothioic acid (WR2721; ethiofos) was shown to selectively protect nontumor tissues from cis-diamminedichloroplatinum(II) (cisplatin)-induced toxicity, when administered 30 min prior to the platinum drug. Selectivity of protection by WR2721 is probably due to the

Synthesis and calculated properties of some 1,4-bis(amino)anthracene-9,10-diones.

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The synthesis of a number of 1,4-bis(amino)anthracene-9,10-diones containing chlorine or sulfur which are related to the anti-cancer drugs Ametantrone and Mitoxantrone are reported. 1,4-Dichloro-2,3-dihydro-5,8-dihydroxyanthracene-9,10-dione reacts readily with a series of alkylamines to yield the

Preclinical evaluation of WR-151327: an orally active chemotherapy protector.

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Clinical trials are in progress to evaluate radio- and chemoprotection by the aminothiol 2-[(3-aminopropyl)amino]ethanethiol-dihydrogen phosphate ester (WR-2721; amifostine). Phase II and III clinical studies have demonstrated that i.v. administered WR-2721 protects against the toxicities of

Synthesis of α-Aminophosphonic Acid Derivatives Through the Addition of O- and S-Nucleophiles to 2 H-Azirines and Their Antiproliferative Effect on A549 Human Lung Adenocarcinoma Cells

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This work reports a straightforward regioselective synthetic methodology to prepare α-aminophosphine oxides and phosphonates through the addition of oxygen and sulfur nucleophiles to the C-N double bond of 2H-azirine derivatives. Determined by the nature of the nucleophile, different

Photogeneration and reactivity of naphthoquinone methides as purine selective DNA alkylating agents.

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A one-step protecting-group-free synthesis of both 6-hydroxy-naphthalene-2-carbaldehyde and the bifunctional binaphthalenyl derivative afforded 6-hydroxymethylnaphthalen-2-ol, 6-methylaminomethyl-naphthalen-2-ol, [(2-hydroxy-3-naphthyl)methyl]trimethyl ammonium iodide, and a small library of

The potential of amifostine: from cytoprotectant to therapeutic agent.

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OBJECTIVE Amifostine is an inorganic thiophosphate cytoprotective agent known chemically as ethanethiol, 2-[(3-aminopropyl)amino]dihydrogen phosphate. It is a pro-drug of free thiol that may act as a scavenger of free radicals generated in tissues exposed to cytotoxic drugs, and binds to

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