Synthesis and biological evaluation of novel phenanthridinyl piperazine triazoles via click chemistry as anti-proliferative agents

• 出版年: Medicinal Chemistry Research
• 第一著者: Nagesh H.N.; Suresh N.; Prakash G.V.S.B.; Gupta S.; Rao J.V.; Sekhar K.V.G.C.
• フォーマット: 論文
• 言語: English
• 出版事項: Birkhauser Boston 2015
• オンライン･アクセス: https://www.scopus.com/inward/record.uri?eid=2-s2.0-84926482705&doi=10.1007%2fs00044-014-1142-6&partnerID=40&md5=d57036eae9a7303722f809c4acfe5526
• ISSN: 10542523
• DOI: 10.1007/s00044-014-1142-6

The preliminary results describe synthesis of a series of novel 6-(4-((substituted-1H-1,2,3-triazol-4-yl)methyl)piperazin-1-yl)phenanthridine analogs using hybrid approach employing copper(I)-catalyzed azide-alkyne cycloaddition and their evaluation as antiproliferative agents against four cancer cell lines by MTT assay. Among the synthesized compounds, 7g and 7h showed good activity against all the test cell lines. In particular, 7g (IC50 = 9.73 ± 4.09 μM) exhibited excellent activity against THP1 cancer cell line, and 7h (IC50 = 7.22 ± 0.32 μM) emerged as more active compound than the standard drug etoposide against HL60 cancer cell line. © 2014 Springer Science+Business Media New York.