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合成含磺酰胺基的新型吡咯和吡咯并[2,3-d]嘧啶衍生物,评估其作为抗癌和放射增敏剂的活性。

Synthesis of novel pyrrole and pyrrolo[2,3-d]pyrimidine derivatives bearing sulfonamide moiety for evaluation as anticancer and radiosensitizing agents.

机构信息

Medicinal, Aromatic and Poisonous Plants Research Center (MAPPRC), College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.

出版信息

Bioorg Med Chem Lett. 2010 Nov 1;20(21):6316-20. doi: 10.1016/j.bmcl.2010.08.005. Epub 2010 Aug 7.

DOI:10.1016/j.bmcl.2010.08.005
PMID:20850308
Abstract

Pyrroles and pyrrolo[2,3-d]pyrimidines were reported to act as potent anticancer agents, in this work, a series of novel 2-substituted-3-cyano-4-phenyl-pyrrole 5, 6, 11-18, and 5-phenyl-pyrrolo[2,3-d]pyrimidine derivatives 7-10, 19-24 bearing either sulfathiazole or sulfapyridine were synthesized. The structures of these compounds were confirmed by elemental analysis, IR, (1)H NMR and mass spectral data. All the newly synthesized compounds were evaluated for their in vitro cytotoxicity against liver and breast cancer cell line (HEPG2 and MCF7). Most of the screened compounds showed interesting cytotoxic activities compared with the used reference drug (doxorubicin). The radiosensitizing ability of some of the synthesized compounds was studied and the results showed an increase in the cell killing effect of γ-radiation after combination with the tested compounds.

摘要

吡咯和吡咯并[2,3-d]嘧啶被报道具有很强的抗癌作用,在这项工作中,合成了一系列新型 2-取代-3-氰基-4-苯基-吡咯 5、6、11-18 和 5-苯基-吡咯并[2,3-d]嘧啶衍生物 7-10、19-24,它们分别带有磺胺噻唑或磺胺吡啶。这些化合物的结构通过元素分析、IR、(1)H NMR 和质谱数据得到证实。所有新合成的化合物都进行了体外细胞毒性测试,针对肝癌和乳腺癌细胞系(HEPG2 和 MCF7)。与使用的参考药物(阿霉素)相比,大多数筛选出的化合物表现出有趣的细胞毒性活性。一些合成化合物的放射增敏能力也进行了研究,结果表明,与测试化合物联合使用后,γ 射线的细胞杀伤效应增加。

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