Synthesis and Antitumor Activity of O- and N-Propylamino-Derivatives of Betulin.

O- and N-propylamino-derivatives of betulin and betulonic acid oxime and methyl ester were synthesized. Their antitumor activity against a panel of 60 human cancer cell lines was studied. Two betulin derivatives, 3β-hydroxy- 4 and 3β-O-(3-propylamino)-28-O-(3,6-diaminohexyl)lupa-20(29)-ene 5, exhibited antitumor activity against most of 60 cancer cell lines of nine different human tumor types. They were more active than doxorubicin against HCT-15 colon cancer and NCI/ADR-RES ovary cancer cells. [ABSTRACT FROM AUTHOR]