PURINE AND 8-SUBSTITUTED PURINE ARABINOFURANOSYL AND RIBOFURANOSYL NUCLEOSIDE DERIVATIVES AS POTENTIAL INDUCERS OF THE DIFFERENTIATION OF THE FRIEND-ERYTHROLEUKEMIA
PURINE AND 8-SUBSTITUTED PURINE ARABINOFURANOSYL AND RIBOFURANOSYL NUCLEOSIDE DERIVATIVES AS POTENTIAL INDUCERS OF THE DIFFERENTIATION OF THE FRIEND-ERYTHROLEUKEMIA
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DOI：
10.1021/jm00148a018
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发表时间：
1985-01-01
影响因子：
7.3
通讯作者：
SARTORELLI, AC
中科院分区：
文献类型：
--
作者：
LIN, TS;CHENG, JC;SARTORELLI, AC
几种抗代谢物已被证明具有在体外启动多种白血病细胞系分化的能力。为了探索这种活性的结构要求，合成了一系列嘌呤和8-取代的嘌呤阿拉伯呋喃糖基和呋喃核糖基核苷衍生物，并测试其作为Friend小鼠红白血病细胞分化的诱导剂。9-（β- D-阿拉伯呋喃糖基）次黄嘌呤和6-（羟基氨基）-9-（β- D-阿拉伯呋喃糖基）嘌呤是有效的诱导剂，如果成熟，产生82%和74%联苯胺阳性细胞，合成血红蛋白的细胞数量的措施。6-巯基-9-（β- D-呋喃核糖基）嘌呤和6-（甲巯基）-9-（β- D呋喃核糖基）嘌呤和它们相应的β- D-阿拉伯呋喃糖基衍生物也是成熟的有效引发剂，导致约50%的细胞群体呈现分化的表型。
Several antimetabolites have been demonstrated to have the capacity to initiate differentiation in vitro of a variety of leukemic cell lines. To explore the structural requirements for this activity, a series of purine and 8-substituted purine arabinofuranosyl and ribofuranosyl nucleoside derivatives were synthesized and tested as inducers of the differentiation of Friend murine erythroleukemia cells. 9-(.beta.-D-Arabinofuranosyl)hypoxanthine and 6-(hydroxyamino)-9-(.beta.-D-arabinofuranosyl)purine were effective inducers if maturation, producing 82% and 74% benzidine-positive cells, a measure of the number of cells synthesizing hemoglobin. 6-Mercapto-9-(.beta.-D-ribofuranosyl)purine and 6-(methylmercapto)-9-(.beta.-D ribofuranosyl)purine and their corresponding .beta.-D-arabinofuranosyl derivatives were also effective initiators of maturation, causing approximately 50% of the cell population to assume a differentiated phenotype.