发明名称 |
Synthesis, structure, and antitumor activity of 5,6-dihydro-5-azacytidine |
摘要 |
The compound 5,6-dihydro-5-azacytidine, 5AC[H], and non-toxic acid addition salts such as the hydrochloride, together with its preparation from 5-azacytidine (5-AC) by reduction of the 5,6-double bond of 5-AC with an alkali metal borohydride such as sodium borohydride. Additionally, 5,6-dihydro-5-azacytidine, 5AC[H], has antitumor activity for murine leukemia systems L1210 and P388 as an injectable. In comparison with the parent compound, 5-AC, the antitumor activity is comparable and 5AC[H] exhibits a more favorable therapeutic index. It also has better solution stability over a broad pH range. A structure for the HCl salt is given below. <IMAGE>
|
申请公布号 |
US4058602(A) |
申请公布日期 |
1977.11.15 |
申请号 |
US19760712854 |
申请日期 |
1976.08.09 |
申请人 |
THE UNITED STATES OF AMERICA AS REPRESENTED BY THE DEPARTMENT OF HEALTH, EDUCATION AND WELFARE |
发明人 |
BEISLER, JOHN A.;ABBASI, MOHAMED M.;DRISCOLL, JOHN S. |
分类号 |
C07H19/12;(IPC1-7):A61K31/34;A61K31/53 |
主分类号 |
C07H19/12 |
代理机构 |
|
代理人 |
|
主权项 |
|
地址 |
|