Biochemical and antitumor activity of tiazofurin and its selenium analog (2-beta-D-ribofuranosyl-4-selenazolecarboxamide).
Biochemical and antitumor activity of tiazofurin and its selenium analog (2-beta-D-ribofuranosyl-4-selenazolecarboxamide).
复制标题
噻唑呋林及其硒类似物（2-β-D-呋喃核糖基-4-硒唑甲酰胺）的生化和抗肿瘤活性。
DOI：
10.1016/0006-2952(85)90617-3
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发表时间：
1985
影响因子：
5.8
通讯作者：
R. Jackson
中科院分区：
文献类型：
--
作者：
T. Boritzki;D. Berry;J. Besserer;P. D. Cook;D. W. Fry;W. Leopold;R. Jackson
2-β-D-呋喃核糖基-4-硒唑甲酰胺（Selenazofurin，CI-935）是噻唑弗林（CI-909）的硒类似物，对小鼠或人肿瘤细胞的体外细胞毒作用是噻唑弗林的3 ~ 10倍，对小鼠P388白血病的体内活性也高于噻唑弗林，其体外细胞毒作用可被鸟苷或鸟嘌呤逆转，但不能被其他嘌呤核苷或碱基逆转。三个人肿瘤细胞系选择硒唑弗林或硫唑弗林耐药之间的交叉耐药硒唑弗林和硫唑弗林。用噻唑弗林、硒唑弗林或麦考酚酸处理可减少鸟苷酸池，并导致IMP在WIL 2人淋巴瘤细胞中蓄积。鸟苷酸池的减少伴随着RNA和DNA合成的抑制。硫唑弗林和硒唑弗林的NAD类似物是L1210 IMP脱氢酶（IMP：NAD氧化还原酶，EC 1.2.1.14）的抑制剂，两者对NAD均表现出非竞争性抑制，Ki值分别为5.7 × 10− 8 M和3.3 × 10− 8 M。
2-β-D-Ribofuranosyl-4-selenazolecarboxamide (selenazofurin, CI-935), the selenium analog of tiazofurin (CI-909), was 3- to 10-fold more cytotoxic to murine or human tumor cellsin vitrothan tiazofurin and was also more active against P388 mouse leukemiain vivo.In vitrocytotoxicity could be reversed by guanosine or guanine but not by other purine nucleosides or bases. Three human tumor cell lines selected for selenazofurin or tiazofurin resistance showed crossresistance between selenazofurin and tiazofurin. Treatment with tiazofurin, selenazofurin, or mycophenolic acid decreased guanylate pools and caused an accumulation of IMP in WIL2 human lymphoma cells. The decrease in guanylate pools was accompanied by inhibition of RNA and DNA synthesis. The NAD analogs of tiazofurin and selenazofurin were inhibitors of L1210 IMP dehydrogenase (IMP:NAD oxidoreductase, EC 1.2.1.14), and both showed uncompetitive inhibition with respect to NAD havingKiivalues of 5.7 × 10−8M and 3.3 × 10−8M respectively.
鸟嘌呤和腺嘌呤核苷酸的消耗对小鼠 T 淋巴瘤细胞系中嘌呤饥饿毒性的贡献。
影响因子：
11.2
作者：
Cohen,MB;Sadee,W
通讯作者：
Sadee,W
噻唑呋林和硒唑类似物的体外比较研究。
DOI：
10.1016/s0006-291x(83)80179-x
发表时间：
1983
影响因子：
3.1
作者：
Streeter,DG;Robins,RK
通讯作者：
Robins,RK