Literature DB >> 16263294

Synthesis and biological activity of N,N-dialkylaminoalkyl-substituted bisindolyl and diphenyl pyrazolone derivatives.

Miguel F Braña1, Ana Gradillas, Angel G Ovalles, Berta López, Nuria Acero, Francisco Llinares, Dolores Muñoz Mingarro.   

Abstract

New compounds, structurally related to the potent protein kinase C inhibitor staurosporine, with a bisindolylpyrazolone framework and substituted on the pyrazolone nitrogens with N,N-dialkylaminoalkyl side chain, were synthesized and evaluated for growth-inhibitory properties in several human cell lines. Many showed inhibition of TNF-alpha production in response to the tumor promotor TPA on HL-60 cells. The apoptotic activity on HeLa cells has been examined for several of these compounds.

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Year:  2005        PMID： 16263294     DOI： 10.1016/j.bmc.2005.09.059

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  8 in total

1.  Structure-guided design of a highly selective glycogen synthase kinase-3β inhibitor: a superior neuroprotective pyrazolone showing antimania effects.

Authors:  Wenwen Chen; Irina N Gaisina; Hendra Gunosewoyo; Sam A Malekiani; Taleen Hanania; Alan P Kozikowski
Journal:  ChemMedChem       Date:  2011-07-12       Impact factor: 3.466

2.  Enantioselective synthesis of beta-(3-hydroxypyrazol-1-yl) ketones using an organocatalyzed Michael addition reaction.

Authors:  Sanjib Gogoi; Cong-Gui Zhao; Derong Ding
Journal:  Org Lett       Date:  2009-06-04       Impact factor: 6.005

3.  An easy direct arylation of 5-pyrazolones.

Authors:  Hao Gong; Yiwen Yang; Zechao Wang; Chunxiang Kuang
Journal:  Beilstein J Org Chem       Date:  2013-10-08       Impact factor: 2.883

4.  Antibacterial, antifungal and in vitro antileukaemia activity of metal complexes with thiosemicarbazones.

Authors:  Elena Pahontu; Felicia Julea; Tudor Rosu; Victor Purcarea; Yurie Chumakov; Petru Petrenco; Aurelian Gulea
Journal:  J Cell Mol Med       Date:  2015-02-24       Impact factor: 5.310

5.  Synthesis, Characterization, and Biological Activity of N (')-[(Z)-(3-Methyl-5-oxo-1-phenyl-1,5-dihydro-4H-pyrazol-4-ylidene)(phenyl)methyl]benzohydrazide and Its Co(II), Ni(II), and Cu(II) Complexes.

Authors:  Jonnie N Asegbeloyin; Oguejiofo T Ujam; Emmanuel C Okafor; Ilknur Babahan; Esin Poyrazoglu Coban; Ali Ozmen; Halil Biyik
Journal:  Bioinorg Chem Appl       Date:  2014-09-15       Impact factor: 7.778

6.  Synthesis and anti-bacterial activities of some novel Schiff bases derived from aminophenazone.

Authors:  Abdullah M Asiri; Salman A Khan
Journal:  Molecules       Date:  2010-10-08       Impact factor: 4.411

Review 7.  Pyrazolone structural motif in medicinal chemistry: Retrospect and prospect.

Authors:  Zefeng Zhao; Xufen Dai; Chenyang Li; Xiao Wang; Jiale Tian; Ying Feng; Jing Xie; Cong Ma; Zhuang Nie; Peinan Fan; Mingcheng Qian; Xirui He; Shaoping Wu; Yongmin Zhang; Xiaohui Zheng
Journal:  Eur J Med Chem       Date:  2019-11-16       Impact factor: 6.514

8.  Microwave assisted synthesis of novel pyrazolone derivatives attached to a pyrimidine moiety and evaluation of their anti-inflammatory, analgesic and antipyretic activities.

Authors:  Rishikesh V Antre; A Cendilkumar; Divakar Goli; Ganesh S Andhale; Rajesh J Oswal
Journal:  Saudi Pharm J       Date:  2011-06-25       Impact factor: 4.330
  8 in total

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