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

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...

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Published in:Medicinal Chemistry Research
Main Author: Nagesh H.N.; Suresh N.; Prakash G.V.S.B.; Gupta S.; Rao J.V.; Sekhar K.V.G.C.
Format: Article
Language:English
Published: Birkhauser Boston 2015
Online Access:https://www.scopus.com/inward/record.uri?eid=2-s2.0-84926482705&doi=10.1007%2fs00044-014-1142-6&partnerID=40&md5=d57036eae9a7303722f809c4acfe5526
id 2-s2.0-84926482705
spelling 2-s2.0-84926482705
Nagesh H.N.; Suresh N.; Prakash G.V.S.B.; Gupta S.; Rao J.V.; Sekhar K.V.G.C.
Synthesis and biological evaluation of novel phenanthridinyl piperazine triazoles via click chemistry as anti-proliferative agents
2015
Medicinal Chemistry Research
24
2
10.1007/s00044-014-1142-6
https://www.scopus.com/inward/record.uri?eid=2-s2.0-84926482705&doi=10.1007%2fs00044-014-1142-6&partnerID=40&md5=d57036eae9a7303722f809c4acfe5526
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.
Birkhauser Boston
10542523
English
Article
author Nagesh H.N.; Suresh N.; Prakash G.V.S.B.; Gupta S.; Rao J.V.; Sekhar K.V.G.C.
spellingShingle Nagesh H.N.; Suresh N.; Prakash G.V.S.B.; Gupta S.; Rao J.V.; Sekhar K.V.G.C.
Synthesis and biological evaluation of novel phenanthridinyl piperazine triazoles via click chemistry as anti-proliferative agents
author_facet Nagesh H.N.; Suresh N.; Prakash G.V.S.B.; Gupta S.; Rao J.V.; Sekhar K.V.G.C.
author_sort Nagesh H.N.; Suresh N.; Prakash G.V.S.B.; Gupta S.; Rao J.V.; Sekhar K.V.G.C.
title Synthesis and biological evaluation of novel phenanthridinyl piperazine triazoles via click chemistry as anti-proliferative agents
title_short Synthesis and biological evaluation of novel phenanthridinyl piperazine triazoles via click chemistry as anti-proliferative agents
title_full Synthesis and biological evaluation of novel phenanthridinyl piperazine triazoles via click chemistry as anti-proliferative agents
title_fullStr Synthesis and biological evaluation of novel phenanthridinyl piperazine triazoles via click chemistry as anti-proliferative agents
title_full_unstemmed Synthesis and biological evaluation of novel phenanthridinyl piperazine triazoles via click chemistry as anti-proliferative agents
title_sort Synthesis and biological evaluation of novel phenanthridinyl piperazine triazoles via click chemistry as anti-proliferative agents
publishDate 2015
container_title Medicinal Chemistry Research
container_volume 24
container_issue 2
doi_str_mv 10.1007/s00044-014-1142-6
url https://www.scopus.com/inward/record.uri?eid=2-s2.0-84926482705&doi=10.1007%2fs00044-014-1142-6&partnerID=40&md5=d57036eae9a7303722f809c4acfe5526
description 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.
publisher Birkhauser Boston
issn 10542523
language English
format Article
accesstype
record_format scopus
collection Scopus
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