https://scholars.lib.ntu.edu.tw/handle/123456789/454756
標題: | Synthesis and biological evaluation of anthra[1,9-cd]pyrazol-6(2H)-one scaffold derivatives as potential anticancer agents | 作者: | Chen T.-C. JIH-HWA GUH Hsu H.-W. Chen C.-L. Lee C.-C. Wu C.-L. Lee Y.-R. JING-JER LIN Yu D.-S. Huang H.-S. |
公開日期: | 2019 | 出版社: | Elsevier B.V. | 卷: | 12 | 期: | 8 | 起(迄)頁: | 2864-2881 | 來源出版物: | Arabian Journal of Chemistry | 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 10.498 μM and 4.542 μM over 60 cell lines which is better than the average GI50 (20.3 μM) for SP600125 (NSC75890). Overall, the test compounds exhibited different telomerase and cytotoxic activities and only few compounds displayed antitumor activity in the low range. ? 2015 The Authors |
URI: | https://www.scopus.com/inward/record.uri?eid=2-s2.0-85077098574&doi=10.1016%2fj.arabjc.2015.06.017&partnerID=40&md5=2150d7809022e3b966fa662c982cf5b1 https://scholars.lib.ntu.edu.tw/handle/123456789/454756 |
ISSN: | 1878-5352 | DOI: | 10.1016/j.arabjc.2015.06.017 | SDG/關鍵字: | Cell culture; Cytotoxicity; Diseases; Anthrapyrazolone; Anti-tumor activities; Antiproliferation; Biological evaluation; Non-small cell lung carcinomata; Nucleophilic reaction; Potential anticancer agents; Prostate cancer cells; Cells |
顯示於: | 生物化學暨分子生物學科研究所 |
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