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3-硝基-1,2,4-三唑类乏氧细胞放射增敏剂的构效关系
引用本文:仉文升,沈恂,李五岭,吴艳芬,蔡松君,李心愿,汤丽霞,王丽佳,李仁利. 3-硝基-1,2,4-三唑类乏氧细胞放射增敏剂的构效关系[J]. 药学学报, 1994, 0(10)
作者姓名:仉文升  沈恂  李五岭  吴艳芬  蔡松君  李心愿  汤丽霞  王丽佳  李仁利
作者单位:北京医科大学药学院,中国科学院生物物理研究所
摘    要:为了寻找毒性低、增敏作用强的乏氧细胞放射增敏剂,设计并合成了一系列5-溴-,5-甲基-,和5-未取代的3-硝基-1,2,4-三唑-1-乙酰胺类化合物,用HeLaS3细胞进行了体外试验。结果表明5-溴取代衍生物的增敏作用强于相应的5-甲基-或5-未取代的硝基三唑衍生物,但是它们的毒性亦增大。修饰1位乙酰胺侧链也可以改变化合物的增敏作用和亲脂性。在所测定的化合物中TA-101[2-(3-硝基-1-三唑基)乙酰胺]由于有高的增敏作用和低亲脂性,可能是一个有希望的放射增敏剂。

关 键 词:乏氧细胞放射增敏剂;放射增敏剂;构效关系;3-硝基-1,2,4-三唑类化合物

STRUCTURE-ACTIVITY RELATIONSHIPS FOR 3-NITRO-1,2,4- TRIAZOLES AS HYPOXIC TUMOR CELL RADIOSENSTIZER
WS Zhang,X Shen,WL Li,YF Wu,SJ Cai,XY Li,LX Tang,LJ Wang and RL Li. STRUCTURE-ACTIVITY RELATIONSHIPS FOR 3-NITRO-1,2,4- TRIAZOLES AS HYPOXIC TUMOR CELL RADIOSENSTIZER[J]. Acta pharmaceutica Sinica, 1994, 0(10)
Authors:WS Zhang  X Shen  WL Li  YF Wu  SJ Cai  XY Li  LX Tang  LJ Wang  RL Li
Abstract:In order to search for effective radiosensitizer of hypoxic cell with low toxicity,a series of 5-bromo-,5-methy1-,and 5-unsubstituted-3-nitro-1,2,4-triazole-1- acetamides were synthesized and tested in vitro with HeLa S3 cells.The radiosensitlzing activity of 5-bromo-derivatives are more potent than those of corresponding 5-methyl-or 5- unsubstituted-1,2,4-triazole derivatives,but the chronic aerobic cytotoxicities are increased.Modification of the N1-acetamide side chain can also change the radiosensitizing activity and the lipophilicity.Among all the tested nitrotriazole derivatives,TA-101[2-(3- nitro-1-triazolyl)acetamide],may be a potential radiosensitizer because of its higher sensitizing activity and much lower lipophilicity.
Keywords:Hypoxic cell radiosensitizer  Radiosensitizer  Structure-activity relationships  3-Nitro-1  2  4-triazoles
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