Synthesis and biological evaluation of anthra[1,9-cd]pyrazol-6(2H)-one scaffold derivatives as potential anticancer agents

Tsung Chih Chen, Jih Hwa Guh, Hui Wen Hsu, Chun Liang Chen, Chia Chung Lee, Chia Lun Wu, Yu Ru Lee, Jing Jer Lin, Dah Shyong Yu, Hsu Shan Huang

研究成果: 雜誌貢獻文章同行評審

5 引文 斯高帕斯(Scopus)

摘要

Several anthrapyrazolone derivatives derived from 7-chloroanthra[1,9-cd]pyrazol-6(2H)-one and 7-chloro-2-(2-hydroxyethyl)anthra[1,9-cd] pyrazol-6(2H)-one have been prepared by the addition or substitution nucleophilic reactions and further transformed into extended tetracyclic systems and fused to different nitrogenheterocyclic rings into the pharmacophore structure moiety. The compounds synthesized were evaluated for their cytotoxic activity and telomerase activity in prostate cancer cell line by SRB assay and in human non-small cell lung carcinoma cell line by TRAP assay, respectively. Compounds 1-6, 13, 14, 16, 17, 19, 21, 23, 28 and 31 were selected by the NCI and only 1, 4, and 16 represent the GI50, TGI and LC50, respectively. Among them, 1 and 16 exhibited distinctive selectivity of GI50 of 10.498μM and 4.542μM over 60 cell lines which is better than the average GI50 (20.3μM) for SP600125 (NSC75890). Overall, the test compounds exhibited different telomerase and cytotoxic activities and only few compounds displayed antitumor activity in the low range.
原文英語
期刊Arabian Journal of Chemistry
12
發行號8
DOIs
出版狀態已發佈 - 12月 2019

ASJC Scopus subject areas

  • 化學工程 (全部)
  • 化學 (全部)

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