Selective bone targeting 5-fluorouracil prodrugs: Synthesis and preliminary biological evaluation
作者： Liang Ouyang , Dongsheng He , Jing Zhang , Gu He , Bo Jiang
DOI: 10.1016/J.BMC.2011.05.004
关键词:
摘要: Bone tumor is a notoriously difficult disease to manage, requiring frequent and heavy doses of systemically administered chemotherapy. Targeting anticancer drug the bone after systemic administration may provide both greater efficacy treatment less administration. In this paper, series targeting Asp oligopeptides 5-fluorouracil conjugates have been synthesized in convergent approach well characterized by NMR MS techniques. Their hydroxyapatite (HAP) affinity, release cytotoxicity characteristics were evaluated vitro conditions. All prodrugs water soluble exhibited high affinity HAP .The efficient active moiety occurring cleavage different linkage physiological conditions significantly reduced number viable human cancer cells. From vivo distribution, we get these compounds with bone-selectivity long halflife. These results provided an effective entry development new chemotherapeutic drugs.
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