Literature DB >> 17915851

3-substituted 7-phenyl-pyrroloquinolinones show potent cytotoxic activity in human cancer cell lines.

Venusia Gasparotto1, Ignazio Castagliuolo, Maria Grazia Ferlin.   

Abstract

A novel series of 3-alkyl-substituted 7-phenyl-3H-pyrrolo[3,2-f]quinolin-9-ones (7-PPyQs) was synthesized with the aim to optimize the cytotoxic activity of recently identified PPyQs, promising inhibitors of tubulin polymerization. All compounds inhibited the growth of 11 human tumor cell lines at submicromolar concentrations as well as two human resistant cancer sublines, A549-T12 and A549-T24. FACS analysis indicated that all compounds caused significant arrest of the A549 cell cycle in G2/M phase at 0.1 and 1 muM and a good correlation between the cytotoxicity IC50 and their ability to block the cell cycle was observed.

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Year:  2007        PMID： 17915851     DOI： 10.1021/jm070534b

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


  13 in total

1.  MG-2477, a new tubulin inhibitor, induces autophagy through inhibition of the Akt/mTOR pathway and delayed apoptosis in A549 cells.

Authors:  Giampietro Viola; Roberta Bortolozzi; Ernest Hamel; Stefano Moro; Paola Brun; Ignazio Castagliuolo; Maria Grazia Ferlin; Giuseppe Basso
Journal:  Biochem Pharmacol       Date:  2011-09-22       Impact factor: 5.858

2.  The chemistry and pharmacology of privileged pyrroloquinazolines.

Authors:  Bo Chao; Bingbing X Li; Xiangshu Xiao
Journal:  Medchemcomm       Date:  2015-04-01       Impact factor: 3.597

3.  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

Review 4.  Targeted regulation of PI3K/Akt/mTOR/NF-κB signaling by indole compounds and their derivatives: mechanistic details and biological implications for cancer therapy.

Authors:  Aamir Ahmad; Bernhard Biersack; Yiwei Li; Dejuan Kong; Bin Bao; Rainer Schobert; Subhash B Padhye; Fazlul H Sarkar
Journal:  Anticancer Agents Med Chem       Date:  2013-09       Impact factor: 2.505

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.  3-Benzyl-7-methyl-9-phenyl-2-tosyl-2,3,3a,4,9,9a-hexa-hydro-1H-pyrrolo[3,4-b]quinoline.

Authors:  K Chinnakali; D Sudha; M Jayagobi; R Raghunathan; Hoong-Kun Fun
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2009-10-31

9.  The tubulin inhibitor MG-2477 induces autophagy-regulated cell death, ROS accumulation and activation of FOXO3 in neuroblastoma.

Authors:  Judith Hagenbuchner; Lorena Lungkofler; Ursula Kiechl-Kohlendorfer; Giampietro Viola; Maria Grazia Ferlin; Michael J Ausserlechner; Petra Obexer
Journal:  Oncotarget       Date:  2017-05-09

10.  Synthesis, Characterization and Anti-Cancer Activity of Hydrazide Derivatives Incorporating a Quinoline Moiety.

Authors:  Murat Bingul; Owen Tan; Christopher R Gardner; Selina K Sutton; Greg M Arndt; Glenn M Marshall; Belamy B Cheung; Naresh Kumar; David StC Black
Journal:  Molecules       Date:  2016-07-14       Impact factor: 4.411
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