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吡嗪重氮氢氧化物钠盐(NSC-361456)的合成、化学稳定性及临床前抗肿瘤活性

Synthesis, chemical stability and pre-clinical anti-tumor activity of pyrazine diazohydroxide, sodium salt (NSC-361456).

作者信息

Baker D C, Hand E S, Plowman J, Rampal J B, Safavy A, Haugwitz R D, Narayanan V L

机构信息

Department of Chemistry, University of Alabama, Tuscaloosa 35487-9671.

出版信息

Anticancer Drug Des. 1987 Dec;2(3):297-309.

PMID:3449093
Abstract

The synthesis, chemical stability and anti-tumor activity of pyrazine diazohydroxide, sodium salt, a compound that has been selected for development to clinical trials, are described. The compound shows a half-life of about 100 minutes at pH 7.4 and is active against a number of experimental tumors.

摘要

本文描述了吡嗪重氮氢氧化物钠盐的合成、化学稳定性和抗肿瘤活性,该化合物已被选定用于开展临床试验。该化合物在pH 7.4时的半衰期约为100分钟,对多种实验性肿瘤具有活性。

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Anticancer Drug Des. 1987 Dec;2(3):297-309.
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引用本文的文献

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A phase II trial of pyrazine diazohydroxide in patients with disseminated malignant melanoma and no prior chemotherapy--Southwest Oncology Group study.吡嗪重氮氢氧化物用于播散性恶性黑色素瘤且未接受过化疗患者的II期试验——西南肿瘤协作组研究
Invest New Drugs. 2002 Feb;20(1):105-11. doi: 10.1023/a:1014484821460.
2
Pyrazine diazohydroxide (NSC-361456). Phase I clinical and pharmacokinetic studies.
Invest New Drugs. 1994;12(3):207-16. doi: 10.1007/BF00873961.
3
Schedule dependence, activity against natural metastases, and cross-resistance of pyrazine diazohydroxide (sodium salt, NSC 361456) in preclinical models in vivo.吡嗪重氮氢氧化物(钠盐,NSC 361456)在体内临床前模型中的时间依赖性、对自然转移灶的活性及交叉耐药性。
Cancer Chemother Pharmacol. 1990;25(6):425-9. doi: 10.1007/BF00686053.
4
Comparative toxicity of fostriecin, hepsulfam and pyrazine diazohydroxide to human and murine hematopoietic progenitor cells in vitro.
Invest New Drugs. 1991 May;9(2):149-57. doi: 10.1007/BF00175082.