作为潜在抗肿瘤/抗病毒药物的卤代3-脱氮腺苷和3-脱氮鸟苷类似物的合成。
Synthesis of halogen-substituted 3-deazaadenosine and 3-deazaguanosine analogues as potential antitumor/antiviral agents.
作者信息
Liu M C, Luo M Z, Mozdziesz D E, Lin T S, Dutschman G E, Gullen E A, Cheng Y C, Sartorelli A C
机构信息
Department of Pharmacology and Developmental Therapeutics Progam, Cancer Center, Yale University School of Medicine, New Haven, Connecticut 06520-8066, USA.
出版信息
Nucleosides Nucleotides Nucleic Acids. 2001 Dec;20(12):1975-2000. doi: 10.1081/NCN-100108327.
Various 2-halogen-substituted analogues (38, 39, 43 and 44), 3-halogen-substituted analogues (51 and 52), and 2',3'-dihalogen-substituted analogues (57-60) of 3-deazaadenosine and 3-halogen-substituted analogues (61 and 62) of 3-deazaguanosine have been synthesized as potential anticancer and/or antiviral agents. Among these compounds, 3-deaza-3-bromoguanosine (62) showed significant cytotoxicity against L1210, P388, CCRF-CEM and B16F10 cell lines in vitro, producing IC50 values of 3, 7, 9 and 7 microM, respectively. Several 3-deazaadenosine analogues (38, 51, 57 and 59) showed moderate to weak activity against hepatitis B virus.
已合成了3-脱氮腺苷的各种2-卤素取代类似物（38、39、43和44）、3-卤素取代类似物（51和52）、2',3'-二卤素取代类似物（57 - 60）以及3-脱氮鸟苷的3-卤素取代类似物（61和62），作为潜在的抗癌和/或抗病毒药物。在这些化合物中，3-脱氮-3-溴鸟苷（62）在体外对L1210、P388、CCRF - CEM和B16F10细胞系显示出显著的细胞毒性，IC50值分别为3、7、9和7微摩尔。几种3-脱氮腺苷类似物（38、51、57和59）对乙型肝炎病毒显示出中度至弱的活性。
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