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

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 ce...

وصف كامل

التفاصيل البيبلوغرافية
الحاوية / القاعدة:Medicinal Chemistry Research
المؤلف الرئيسي: Nagesh H.N.; Suresh N.; Prakash G.V.S.B.; Gupta S.; Rao J.V.; Sekhar K.V.G.C.
التنسيق: مقال
اللغة:English
منشور في: Birkhauser Boston 2015
الوصول للمادة أونلاين:https://www.scopus.com/inward/record.uri?eid=2-s2.0-84926482705&doi=10.1007%2fs00044-014-1142-6&partnerID=40&md5=d57036eae9a7303722f809c4acfe5526
الوصف
الملخص: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.
تدمد:10542523
DOI:10.1007/s00044-014-1142-6