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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)¹

Departments of Biochemistry [G. P. W., B. J. B., J. A. W., D. J. A.] and Organic Chemistry [C. G. T.], Southern Research Institute, Birmingham, Alabama 35255

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.

¹ This work was supported by Grant 1-RO1-CA25311-01A1 from the National Cancer Institute, NIH.

² To whom requests for reprints should be addressed.

Received 7/27/81. Accepted 11/18/81.

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