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Novel pyrazole and indazole derivatives: Synthesis and evaluation of their anti-proliferative and anti-angiogenic activities

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dc.contributor.author Tzanetou, E en
dc.contributor.author Liekens, S en
dc.contributor.author Kasiotis, KM en
dc.contributor.author Fokialakis, N en
dc.contributor.author Haroutounian, SA en
dc.date.accessioned 2014-06-06T06:51:57Z
dc.date.available 2014-06-06T06:51:57Z
dc.date.issued 2012 en
dc.identifier.issn 03656233 en
dc.identifier.uri http://dx.doi.org/10.1002/ardp.201200057 en
dc.identifier.uri http://62.217.125.90/xmlui/handle/123456789/5780
dc.subject Angiogenesis inhibition en
dc.subject Antiproliferative activity en
dc.subject Indazoles en
dc.subject Pyrazoles en
dc.subject Tube formation en
dc.subject.other 3 (4 fluorophenyl) 1 (4 hydroxyphenyl) 4,5 dihydro 1h benzo[g]indazole 7 ol en
dc.subject.other 3 (4 fluorophenyl) 7 methoxy 1 (4 methoxyphenyl) 4,5 dihydro 1h benzo[g]indazole en
dc.subject.other 3 (4 fluorophenyl) 7 methoxy 4,5 dihydro 1h benzo[g]indazole en
dc.subject.other 3 (4 fluorophenyl) 7 methoxy 4,5 dihydro 1h benzo[g]indazole 7 ol en
dc.subject.other 4 [4 methyl 3 (4 nitrophenyl) 1h pyrazol 5 yl]phenol en
dc.subject.other 4 [5 (4 methoxyphenyl) 4 methyl 1h pyrazole 3 yl]aniline en
dc.subject.other 5 (4 methoxyphenyl) 3 (4 nitrophenyl) 1h pyrazole en
dc.subject.other 5 (4 methoxyphenyl) 4 methyl 3 (4 nitrophenyl) 1h pyrazole en
dc.subject.other 5 [4 (2 bromoethoxy)phenyl] 3 (4 nitrophenyl) 1h pyrazole en
dc.subject.other angiogenesis inhibitor en
dc.subject.other antineoplastic agent en
dc.subject.other indazole derivative en
dc.subject.other pyrazole derivative en
dc.subject.other unclassified drug en
dc.subject.other animal cell en
dc.subject.other antiangiogenic activity en
dc.subject.other antiproliferative activity en
dc.subject.other article en
dc.subject.other cell line en
dc.subject.other cell strain MCF 7 en
dc.subject.other controlled study en
dc.subject.other cytostasis en
dc.subject.other drug potency en
dc.subject.other drug screening en
dc.subject.other drug synthesis en
dc.subject.other female en
dc.subject.other human en
dc.subject.other human cell en
dc.subject.other IC 50 en
dc.subject.other nonhuman en
dc.subject.other priority journal en
dc.subject.other Acetophenones en
dc.subject.other Angiogenesis Inhibitors en
dc.subject.other Animals en
dc.subject.other Breast Neoplasms en
dc.subject.other Cell Line, Tumor en
dc.subject.other Cell Proliferation en
dc.subject.other Endothelial Cells en
dc.subject.other Female en
dc.subject.other HeLa Cells en
dc.subject.other Humans en
dc.subject.other Indazoles en
dc.subject.other Inhibitory Concentration 50 en
dc.subject.other Mice en
dc.subject.other Pyrazoles en
dc.subject.other Tetralones en
dc.title Novel pyrazole and indazole derivatives: Synthesis and evaluation of their anti-proliferative and anti-angiogenic activities en
heal.type journalArticle en
heal.identifier.primary 10.1002/ardp.201200057 en
heal.publicationDate 2012 en
heal.abstract The synthesis of several new pyrazole and indazole derivatives from acetophenone and tetralone substrates is reported. The bioactivities of the new compounds were evaluated through in vitro assays for endothelial cell proliferation and tube formation. Results herein indicate that the easily prepared compounds containing the indazole structural framework exhibit potent cytostatic properties against all cell lines tested, with compounds 13 and 14 being the most active displaying IC50 values of 1.5 ± 0.4 μM and 5.6 ± 2.5 μM, respectively, against MCF-7 cells. In addition, the indazole derivative 16 was assessed as a competent inhibitor of endothelial tube formation at 30 μM. Copyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim. en
heal.journalName Archiv der Pharmazie en
dc.identifier.issue 10 en
dc.identifier.volume 345 en
dc.identifier.doi 10.1002/ardp.201200057 en
dc.identifier.spage 804 en
dc.identifier.epage 811 en


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