Synthesis, structure, and antitumor activity of 5,6-dihydro-5-az

Drug – bio-affecting and body treating compositions – Conjugate or complex of monoclonal or polyclonal antibody,... – Conjugated via claimed linking group – bond – chelating agent,...

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536 23, A61K 3134, A61K 3153, C07H 1912

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active

040586022

ABSTRACT:
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. ##STR1##

REFERENCES:
patent: 3171833 (1965-03-01), Sorm et al.
patent: 3221010 (1965-11-01), Duschinsky
patent: 3462416 (1969-08-01), Hanze et al.

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