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合成新型吡咯并[2,3-d]嘧啶衍生物及其对人结肠癌细胞系活性的评价。

Synthesis of new pyrrolo[2,3-d]pyrimidine derivatives and evaluation of their activities against human colon cancer cell lines.

机构信息

University College of Pharmaceutical Sciences, Kakatiya University Warangal 506 009, Andhra Pradesh, India.

出版信息

Eur J Med Chem. 2010 Apr;45(4):1453-8. doi: 10.1016/j.ejmech.2009.12.050. Epub 2010 Jan 22.

DOI:10.1016/j.ejmech.2009.12.050
PMID:20163895
Abstract

New pyrrolo[2,3-d]Pyrimidines with heteroaryl substitution at 5th position through sulfur linker were synthesized incorporating putative pharmacophoric moieties like benzimidazole and benzothiazole as heteroaryl groups. Cytotoxic effect of all the compounds was carried out on HCT116 colon cancer cell lines. Compounds 6c and 6h with nitrobenzimidazole and pyrimidyl heterocycles attached at 5th position via sulfur were the most potent of all with IC50 values approximately 17.6 muM. Among the four compounds tested for apoptosis induction activity, 6c induced apoptosis in a dose dependent manner.

摘要

通过硫连接键在 5 位取代杂芳基的新型吡咯并[2,3-d]嘧啶类化合物，其中杂芳基为苯并咪唑和苯并噻唑等假定药效团。所有化合物的细胞毒性作用均在 HCT116 结肠癌细胞系上进行。带有硝基苯并咪唑和嘧啶杂环的化合物 6c 和 6h 通过硫连接键连接到 5 位，是所有化合物中最有效的，IC50 值约为 17.6 μM。在测试的四种诱导细胞凋亡活性的化合物中，6c 呈剂量依赖性诱导细胞凋亡。

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