The utilization of 2-aminoprop-1-ene-1,1,3-tricarbonitrile as a precursor to quinoline, furan and thiophene derivatives with antitumor activities

Heterocyclic communications

article

Rafat M. Mohareb¹  Daisy H. Fleita³  Ola K. Sakka³ 

[1] Department of Chemistry, Faculty of Science, Cairo University;Department of Organic Chemistry, Faculty of Pharmacy, October University for Modern Sciences and Arts;Department of Chemistry, American University in Cairo

关键词: antitumor activity;    furan;    pyrazole;    quinoline;    thiophene;   

DOI  :  10.1515/hc.2011.017

学科分类：内科医学

来源: De Gruyter

【 摘 要 】

The condensation reaction of 2-aminoprop-1-ene-1,1,3-tricarbonitrile ( 1 ) with 2-acetyl-furan ( 2 ) afforded 2-amino-4-(furan-2-yl)penta-1,3-diene-1,1,3-tricarbonitrile ( 3 ). The latter compound underwent a series of heterocyclization reactions to give quinoline, furan, pyrazole and thiophene derivatives. The antitumor evaluation of the newly synthesized products against three cancer cell lines, namely breast adenocarcinoma (MCF-7), non-small cell lung cancer (NCI-H460) and CNS cancer (SF-268) were recorded. Three of the synthesized compounds, namely 4 , 5d and 12 showed high inhibitory effects.

【 授权许可】

CC BY|CC BY-NC-ND