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5-氨基-1,2-二氢-3-[(N-甲基苯胺基)甲基]-吡啶并[3,4-b]吡嗪-7-基氨基甲酸乙酯(NSC 181928)对有丝分裂的抑制作用及对实验性肿瘤的抗癌活性

Inhibition of mitosis and anticancer activity against experimental neoplasms by ethyl 5-amino-1,2-dihydro-3-[(N-methylanilino)methyl]-pyrido[3,4-b]pyrazin-7-ylcarbamate (NSC 181928).

作者信息

Wheeler G P, Bowdon B J, Werline J A, Adamson D J, Temple C G

出版信息

Cancer Res. 1982 Mar;42(3):791-8.

PMID:7059977
Abstract

Ethyl 5-amino-1,2-dihydro-3-[N-methylanilino)methyl]pyrido[3,4-b]pyrazin-7-ylcarbamate (NSC 181928) is reported to be active against several experimental neoplasms. The experimental data obtained in the present study indicate that it causes the accumulation of cells at mitosis with both cultured cells and ascites cancer cells in vivo. This effect was observed with L1210, P388, colon cancer 26, colon cancer 38, and H.Ep. 2 cells in culture and with L1210 cells and P388 cells in mice. The agent was also active in vitro and in vivo against a line of leukemia P388 cells that are resistant to vincristine.

摘要

据报道,5-氨基-1,2-二氢-3-[[N-甲基苯胺基]甲基]吡啶并[3,4-b]吡嗪-7-基氨基甲酸乙酯(NSC 181928)对多种实验性肿瘤具有活性。本研究获得的实验数据表明,它能使培养细胞和体内腹水癌细胞在有丝分裂时积累细胞。在培养的L1210、P388、结肠癌26、结肠癌38和H.Ep.2细胞以及小鼠体内的L1210细胞和P388细胞中均观察到了这种效应。该药物在体外和体内对一株对长春新碱耐药的白血病P388细胞也具有活性。

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