Antimetabolites

To enhance the efficacy of 1-b-d-arabinofuranosylcytosine (ara-C) in simple dosage schedules, researchers synthesized two ara-C conjugates with PG via an amide bond: one where ara-C is directly coupled with the N-4 of ara-C to the carboxyl groups of PG and one where ara-C is linked with PG via the aminoalkylphosphoryl side chain introduced at the C-50 of ara-C.34 Both conjugates exhibited markedly decreased cytotoxicity in L1210 murine leukemia cells when compared with free ara-C. However, the anti-tumor activity of both conjugates was greater than or equal to that of free ara-C in mice bearing L1210 tumors after a single intraperitoneal injection of the conjugate. The authors suggested that both slow cleavage of free ara-C from the conjugates and protection of ara-C from deactivation by cytidine deaminase contributed to the enhanced anti-tumor activity of PG-ara-C conjugates in vivo.

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