咪唑并[4,5-b]吡啶衍生的嘌呤生物电子等排体的设计、合成及构效关系（SAR）研究及其作为细胞毒性剂的潜力。
Design, synthesis and structure--activity relationship (SAR) studies of imidazo[4,5-b]pyridine derived purine isosteres and their potential as cytotoxic agents.
作者信息
Sajith Ayyiliath M, Abdul Khader K K, Joshi Nithin, Reddy Manchala Nageswar, Syed Ali Padusha M, Nagaswarupa H P, Nibin Joy M, Bodke Yadav D, Karuvalam Ranjith P, Banerjee Rinti, Muralidharan A, Rajendra P
机构信息
Department of Chemistry, Nehru Arts and Science College, Kannur University, Kannur, India; Post Graduate and Research Department of Chemistry, Kasargod Govt. College, Kannur University, Kasaragod, India.
Post Graduate and Research Department of Chemistry, Jamal Mohamed College, Bharathidasan University, Tiruchirapalli, India.
出版信息
Eur J Med Chem. 2015 Jan 7;89:21-31. doi: 10.1016/j.ejmech.2014.10.037. Epub 2014 Oct 14.
Drug resistance to chemotherapeutic agents paved the way to develop novel synthetic molecules which are active on MDR cancer cell lines. Regio-isomeric imidazo[4,5-b]pyridine analogues were synthesized and evaluated for their cytotoxic activity against a range of cancer cell lines. The structure-activity relationship (SAR) studies of the imidazopyridine analogues are also described. Analogue 6b displayed strong cytotoxicity and good microsomal stability.
对化疗药物的耐药性为开发对多药耐药癌细胞系有活性的新型合成分子铺平了道路。合成了区域异构体咪唑并[4,5-b]吡啶类似物，并评估了它们对一系列癌细胞系的细胞毒性活性。还描述了咪唑并吡啶类似物的构效关系（SAR）研究。类似物6b表现出很强的细胞毒性和良好的微粒体稳定性。
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