一些带有预期具有抗肿瘤活性的磺酰胺部分的新型吡唑和嘧啶衍生物的合成以及γ辐射协同效应的研究

Synthesis of some new pyrazole and pyrimidine derivatives carrying a sulfonamide moiety of expected antitumor activity and study of the synergistic effect of gamma-irradiation.

作者信息

Ghorab Mostafa M, Ragab Fatma A, Heiba Helmy I, Youssef Hanan A, Galal Marwa

机构信息

Department of Drug Radiation Research, National Center for Radiation Research and Technology, Atomic Energy Authority, Nasr City, Cairo, Egypt.

出版信息

Arzneimittelforschung. 2010;60(1):48-55. doi: 10.1055/s-0031-1296248.

DOI:10.1055/s-0031-1296248

PMID:20184227

Abstract

Several novel pyrazole (11-18) and pyrimidine (19-23) derivatives were synthesized starting from different sulfonamides and different active methylenes. The synthesized compounds were characterized by elemental analysis, IR, 1H-NMR and mass spectral data. The obtained compounds were screened as antitumor agents against human tumor cell line. Some of the tested compounds were equipotent while the others were more potent than doxorubicin (CAS 25316-40-9). The synergistic effect with gamma-radiation was also studied.

摘要

从不同的磺酰胺和不同的活性亚甲基出发，合成了几种新型吡唑衍生物（11 - 18）和嘧啶衍生物（19 - 23）。通过元素分析、红外光谱、¹H - 核磁共振和质谱数据对合成的化合物进行了表征。所得到的化合物被作为抗人肿瘤细胞系的抗肿瘤剂进行筛选。一些受试化合物具有同等效力，而其他一些化合物比阿霉素（CAS 25316 - 40 - 9）更有效。还研究了与γ射线的协同效应。