Literature DB >> 11814858

Synthesis and biological activities of fluorinated chalcone derivatives.

Chika Nakamura1, Nobuhide Kawasaki, Hideki Miyataka, Ezhuthachan Jayachandran, In Ho Kim, Kenneth L Kirk, Takeo Taguchi, Yoshio Takeuchi, Hitoshi Hori, Toshio Satoh.   

Abstract

We have designed and synthesized new 5-lipoxygenase inhibitors, fluorinated 3,4-dihydroxychalcones, and evaluated their biological activities with respect to antiperoxidation activity and in vitro antitumor activities. All fluorinated chalcones tested showed 5-lipoxygenase inhibition on rat basophilic leukemia-1 (RBL-1) cells and inhibitory action on Fe(3+)-ADP induced NADPH-dependent lipid peroxidation in rat liver microsomes. The potencies were comparable or better to that of the lead 3,4-dihydroxychalcone. 6-Fluoro-3,4-dihydroxy-2',4'-dimethoxy chalcone (7) was the most effective compound in the in vitro assay using a human cancer cell line panel (HCC panel) consisting of 39 systems.

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Year:  2002        PMID： 11814858     DOI： 10.1016/s0968-0896(01)00319-4

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


  9 in total

1.  Conformation analysis of a novel fluorinated chalcone.

Authors:  Paulo S Carvalho; Jean M F Custodio; Wesley F Vaz; Cassio C Cirilo; Amanda F Cidade; Gilberto L B Aquino; Dulcinea M B Campos; Pedro Cravo; Clarimar J Coelho; Solemar S Oliveira; Ademir J Camargo; Hamilton B Napolitano
Journal:  J Mol Model       Date:  2017-03-01       Impact factor: 1.810

2.  A monoclinic polymorph of 1-(4-chloro-phen-yl)-3-(4-methoxy-phen-yl)prop-2-en-1-one.

Authors:  Jerry P Jasinski; Ray J Butcher; B Narayana; S Samshuddin; H S Yathirajan
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2010-01-09

3.  A second polymorph of (2E)-1-(4-fluoro-phen-yl)-3-(3,4,5-trimethoxy-phen-yl)prop-2-en-1-one.

Authors:  Jerry P Jasinski; Ray J Butcher; K Veena; B Narayana; H S Yathirajan
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2009-07-25

4.  (E)-4-aryl-4-oxo-2-butenoic acid amides, chalcone-aroylacrylic acid chimeras: design, antiproliferative activity and inhibition of tubulin polymerization.

Authors:  Maja D Vitorović-Todorović; Aleksandra Erić-Nikolić; Branka Kolundžija; Ernest Hamel; Slavica Ristić; Ivan O Juranić; Branko J Drakulić
Journal:  Eur J Med Chem       Date:  2013-01-11       Impact factor: 6.514

5.  Trans-4-lodo,4'-boranyl-chalcone induces antitumor activity against malignant glioma cell lines in vitro and in vivo.

Authors:  Takashi Sasayama; Kazuhiro Tanaka; Katsu Mizukawa; Atsufumi Kawamura; Takeshi Kondoh; Kohkichi Hosoda; Eiji Kohmura
Journal:  J Neurooncol       Date:  2007-05-26       Impact factor: 4.130

6.  (2E)-3-[4-(Dimethyl-amino)-phen-yl]-1-(4-fluoro-phen-yl)prop-2-en-1-one.

Authors:  Jerry P Jasinski; Ray J Butcher; B P Siddaraju; B Narayana; H S Yathirajan
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-01-08

Review 7.  Emerging role of Garcinol, the antioxidant chalcone from Garcinia indica Choisy and its synthetic analogs.

Authors:  Subhash Padhye; Aamir Ahmad; Nikhil Oswal; Fazlul H Sarkar
Journal:  J Hematol Oncol       Date:  2009-09-02       Impact factor: 17.388

8.  Synthesis, biological evaluation and in silico molecular docking of novel 1-hydroxy-naphthyl substituted heterocycles.

Authors:  El-Sayed I El-Desoky; Eman M Keshk; Aya A El-Sawi; Mohamed A Abozeid; Laila A Abouzeid; Abdel-Rahman H Abdel-Rahman
Journal:  Saudi Pharm J       Date:  2018-03-27       Impact factor: 4.330

9.  Practical Synthesis of Chalcone Derivatives and Their Biological Activities.

Authors:  Jae-Chul Jung; Yongnam Lee; Dongguk Min; Mankil Jung; Seikwan Oh
Journal:  Molecules       Date:  2017-11-01       Impact factor: 4.411
  9 in total

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