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The carbocyclic analog of cytidine, synthesis and antineoplastic activity
Author(s) -
Shealy Y. Fulmer,
O'Dell C. Allen
Publication year - 1976
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.5570130645
Subject(s) - cytidine , chemistry , derivative (finance) , uridine , stereochemistry , leukemia , biochemistry , rna , enzyme , genetics , biology , financial economics , economics , gene
The carbocyclic analog (VI) of cytidine was prepared from the carbocyclic analog (I) of uridine. The intermediate stages were a tetrabenzoyl derivative of I, the tribenzoyl derivative of the uridine analog, and the tribenzoyl 4‐chloropyrimidinone obtained from the latter derivative. The cytidine analog (VI) is active against KB cells in culture and against L1210 leukemia in mice. In the initial tests against L1210 leukemia, the highest dose (200 mg./kg./day, q.d. 1‐9), of three active doses, increased lifespan by 82% and showed no evidence of toxicity.