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Synthesis of variants of 5‐benzylacyclouridine and 5‐benzyloxybenzylacyclouridine
Author(s) -
Chu ShihHsi,
Chen ZhiHao,
Weng ZumYao,
Rowe Elizabeth C.,
Chu Edward,
Chu MingYu Wang
Publication year - 1986
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.5570230609
Subject(s) - chemistry , potentiator , uracil , methylene , uridine , stereochemistry , combinatorial chemistry , biochemistry , medicinal chemistry , rna , pharmacology , dna , medicine , gene
A number of variations and derivatives of BAU (5‐benzylacyclouridine) and BBAU (5‐benzyloxybenzylacy‐clouridine), potent inhibitors of uridine phosphorylase were synthesized for evaluation as potential cancer chemotherapeutic agents. (“Acyclo” = 2′‐hydroxymethoxymethyl‐). These included a modification of the methylene group at N‐1, esters of the terminal hydroxyl of the acyclo group, and extension of the benzyl chain at position 5 of the uracil base. BBBAU was a very good potentiator of FUdR in cell culture.