Literature DB >> 7108898

(2-Chloroethyl)nitrosourea congeners of amino acid amides.

T Suami, T Kato, H Takino, T Hisamatsu.   

Abstract

Fourteen (2-chloroethyl)nitrosourea congeners of L-amino acid amides have been synthesized as potential antineoplastic agents. Almost all the congeners tested were found to be highly active against experimental leukemia L1210 in mice. The chemical decomposition rates of the congeners were measured in a buffered solution (pH 7.4) at 37 degrees C. Acute toxicities of some of the congeners were determined for mice. The congener of sarcosinamide shows the longest half-life (T0.5 = 329.7 min) and the lowest toxicity, LD50 = 392.0 mg/kg (ip) and 426.6 mg/kg (iv), in this series.

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Year:  1982        PMID: 7108898     DOI: 10.1021/jm00349a012

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  11 in total

1.  Enhanced antitumor activity of sarCNU in comparison to BCNU in an extraneuronal monoamine transporter positive human glioma xenograft model.

Authors:  Z P Chen; G Wang; Q Huang; Z F Sun; L Y Zhou; A D Wang; L C Panasci
Journal:  J Neurooncol       Date:  1999-08       Impact factor: 4.130

2.  Relationship between drug delivery and the intra-arterial infusion rate of SarCNU in C6 rat brain tumor model.

Authors:  N Takeda; M Diksic
Journal:  J Neurooncol       Date:  1999-02       Impact factor: 4.130

3.  The cytotoxicity of a 2-chloroethylnitrosourea analog of sarcosinamide in the SK-MG-1 human glioma cell line as a possible indicator for transport.

Authors:  V Skalski; W Feindel; L C Panasci
Journal:  J Neurooncol       Date:  1989-07       Impact factor: 4.130

4.  Utilization of the HTSCA and CFU-C assay to identify two new 2-chloroethylnitrosourea congeners of amino acid amides with increased in vitro activity against human glioma compared with BCNU.

Authors:  L C Panasci; M Dufour; L Chevalier; G Isabel; P Lazarus; A McQuillan; E Arbit; S Brem; W Feindel
Journal:  Cancer Chemother Pharmacol       Date:  1985       Impact factor: 3.333

5.  Pharmacokinetics of 11C-labelled BCNU and SarCNU in gliomas studied by PET.

Authors:  S Mitsuki; M Diksic; T Conway; Y L Yamamoto; J G Villemure; W Feindel
Journal:  J Neurooncol       Date:  1991-02       Impact factor: 4.130

6.  Lack of evidence for a high-affinity sarcosinamide carrier or a catecholamine carrier in Calu-1 lung-cancer cells, HT-29 colon-cancer cells, and DHF fibroblasts.

Authors:  A Malapetsa; J L Bramson; A J Noë; L C Panasci
Journal:  Cancer Chemother Pharmacol       Date:  1992       Impact factor: 3.333

7.  Antitumor action of N-(2-chloroethyl)-N-nitrosocarbamoyl derivatives of biologically active polypeptide hormone fragments.

Authors:  A Jeney; L Kopper; P Nagy; K Lapis; H Süli-Vargha; K Medzihradszky
Journal:  Cancer Chemother Pharmacol       Date:  1986       Impact factor: 3.333

8.  New derivatives of CNC-amino acids and -oligopeptides: experimental antitumor activity.

Authors:  W J Zeller
Journal:  J Cancer Res Clin Oncol       Date:  1986       Impact factor: 4.553

9.  The cytotoxicity of sarcosinamide chloroethylnitrosourea (SarCNU) and BCNU in primary gliomas and glioma cell lines: analysis of data in reference to theoretical peak plasma concentrations in man.

Authors:  V Skalski; J Rivas; L Panasci; A McQuillan; W Feindel
Journal:  Cancer Chemother Pharmacol       Date:  1988       Impact factor: 3.333

10.  Antineoplastic activity of esters and amides of N-[N'-(2-chloroethyl)-N'-nitrosocarbamoyl]-aminoacids.

Authors:  W J Zeller; K Ehresmann; G Eisenbrand
Journal:  J Cancer Res Clin Oncol       Date:  1984       Impact factor: 4.553

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