咪唑并[1,2-a]吡嗪衍生物抗癌活性构效关系研究。
Structure activity relationship studies of imidazo[1,2-a]pyrazine derivatives against cancer cell lines.
机构信息
Organic Chemistry Division-II, Indian Institute of Chemical Technology, Tarnaka-uppal road, Tarnaka, Hyderabad 500607, India.
出版信息
Eur J Med Chem. 2010 Nov;45(11):5208-16. doi: 10.1016/j.ejmech.2010.08.035. Epub 2010 Aug 18.
PMID:20832916
Abstract
Designed novel imidazo[1,2-a]pyrazine based inhibitors, synthesized by condensing α-aminopyrazines with α-halocarbonyl compounds followed by electrophilic substitutions. Cytotoxic effects on four cancer cell lines evaluated. Based on preliminary data, imidazo[1,2-a]pyrazine template redesigned to improve activity.
摘要
设计新型咪唑并[1,2-a]吡嗪类抑制剂，通过将α-氨基吡嗪与α-卤代羰基化合物缩合，再进行亲电取代反应合成。评估了对四种癌细胞系的细胞毒性作用。根据初步数据，重新设计咪唑并[1,2-a]吡嗪模板以提高活性。
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