Literature DB >> 16539377

Synthesis and biological activity of 7-phenyl-6,9-dihydro-3H-pyrrolo[3,2-f]quinolin-9-ones: a new class of antimitotic agents devoid of aromatase activity.

Venusia Gasparotto1, Ignazio Castagliuolo, Gianfranco Chiarelotto, Vincenzo Pezzi, Daniela Montanaro, Paola Brun, Giorgio Palù, Giampietro Viola, Maria Grazia Ferlin.   

Abstract

The newly synthesized 7-phenyl-3H-pyrrolo[3,2-f]quinolinones 16-26 and previously 27 and 28 were assayed for their in vitro antiproliferative activity on tumor cell lines, and the lead compound 16 in vivo on a singenic hepatocellular carcinoma in Balb/c mice. Results from FACS, immunofluorescence microscopy analysis, tubulin polymerization assay, and tritiated water release assay for the CYP19 activity confirmed the new compounds as potential anticancer agents acting by tubulin depolymerization, but devoid of aromatase activity unlike their geometric [2,3-h] isomers.

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Year:  2006        PMID： 16539377     DOI： 10.1021/jm0510676

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  10 in total

1.  Synthesis and in vitro evaluation of 3h-pyrrolo[3,2-f]-quinolin-9-one derivatives that show potent and selective anti-leukemic activity.

Authors:  Maria Grazia Ferlin; Roberta Bortolozzi; Paola Brun; Ignazio Castagliuolo; Ernest Hamel; Giuseppe Basso; Giampietro Viola
Journal:  ChemMedChem       Date:  2010-08-02       Impact factor: 3.466

2.  Synthesis, antimitotic and antivascular activity of 1-(3',4',5'-trimethoxybenzoyl)-3-arylamino-5-amino-1,2,4-triazoles.

Authors:  Romeo Romagnoli; Pier Giovanni Baraldi; Maria Kimatrai Salvador; Filippo Prencipe; Valerio Bertolasi; Michela Cancellieri; Andrea Brancale; Ernest Hamel; Ignazio Castagliuolo; Francesca Consolaro; Elena Porcù; Giuseppe Basso; Giampietro Viola
Journal:  J Med Chem       Date:  2014-07-28       Impact factor: 7.446

3.  Design, synthesis, in vitro, and in vivo anticancer and antiangiogenic activity of novel 3-arylaminobenzofuran derivatives targeting the colchicine site on tubulin.

Authors:  Romeo Romagnoli; Pier Giovanni Baraldi; Maria Kimatrai Salvador; Filippo Prencipe; Carlota Lopez-Cara; Santiago Schiaffino Ortega; Andrea Brancale; Ernest Hamel; Ignazio Castagliuolo; Stefania Mitola; Roberto Ronca; Roberta Bortolozzi; Elena Porcù; Giuseppe Basso; Giampietro Viola
Journal:  J Med Chem       Date:  2015-03-26       Impact factor: 7.446

4.  Synthesis and biological evaluation of 2-(alkoxycarbonyl)-3-anilinobenzo[b]thiophenes and thieno[2,3-b]pyridines as new potent anticancer agents.

Authors:  Romeo Romagnoli; Pier Giovanni Baraldi; Maria Kimatrai Salvador; Delia Preti; Mojgan Aghazadeh Tabrizi; Marcella Bassetto; Andrea Brancale; Ernest Hamel; Ignazio Castagliuolo; Roberta Bortolozzi; Giuseppe Basso; Giampietro Viola
Journal:  J Med Chem       Date:  2013-03-18       Impact factor: 7.446

5.  Synthesis, structure-activity relationships and biological evaluation of 7-phenyl-pyrroloquinolinone 3-amide derivatives as potent antimitotic agents.

Authors:  Davide Carta; Roberta Bortolozzi; Mattia Sturlese; Veronica Salmaso; Ernest Hamel; Giuseppe Basso; Laura Calderan; Luigi Quintieri; Stefano Moro; Giampietro Viola; Maria Grazia Ferlin
Journal:  Eur J Med Chem       Date:  2016-10-21       Impact factor: 6.514

6.  Novel 3-Substituted 7-Phenylpyrrolo[3,2-f]quinolin-9(6H)-ones as Single Entities with Multitarget Antiproliferative Activity.

Authors:  Davide Carta; Roberta Bortolozzi; Ernest Hamel; Giuseppe Basso; Stefano Moro; Giampietro Viola; Maria Grazia Ferlin
Journal:  J Med Chem       Date:  2015-10-07       Impact factor: 7.446

7.  Targeting tubulin polymerization by novel 7-aryl-pyrroloquinolinones: Synthesis, biological activity and SARs.

Authors:  Roberta Bortolozzi; Elena Mattiuzzo; Matteo Dal Pra; Mattia Sturlese; Stefano Moro; Ernest Hamel; Davide Carta; Giampietro Viola; Maria Grazia Ferlin
Journal:  Eur J Med Chem       Date:  2017-11-20       Impact factor: 6.514

8.  Ethyl 5-cyano-8-nitro-2,3,4,4a,5,6-hexahydro-1H-pyrido[1,2-a]quinoline-5-carboxylate.

Authors:  Yapi Marcellin Yapo; Kouakou Michel Konan; Ané Adjou; Adéyolé Timotou; Jules A Tenon
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2010-06-23

9.  Ethyl 4-cyano-7-nitro-1,2,3,3a,4,5-hexa-hydro-pyrrolo-[1,2-a]quinoline-4-carboxyl-ate.

Authors:  Yvon Bibila Mayaya Bisseyou; Adéyolé Timotou; Ajouby Adjou; Rita Kakou-Yao; Jules Tenon Abodou
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2012-01-31

10.  Multifunctional, CD44v6-Targeted ORMOSIL Nanoparticles Enhance Drugs Toxicity in Cancer Cells.

Authors:  Lucía Morillas-Becerril; Elektra Peta; Luca Gabrielli; Venera Russo; Elisa Lubian; Luca Nodari; Maria Grazia Ferlin; Paolo Scrimin; Giorgio Palù; Luisa Barzon; Ignazio Castagliuolo; Fabrizio Mancin; Marta Trevisan
Journal:  Nanomaterials (Basel)       Date:  2020-02-10       Impact factor: 5.076
  10 in total

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