Literature DB >> 27217001

Synthesis and anti-proliferative activity of fluoro-substituted chalcones.

Serdar Burmaoglu1, Oztekin Algul2, Derya Aktas Anıl3, Arzu Gobek3, Gulay Gulbol Duran4, Ronak Haj Ersan5, Nizami Duran6.   

Abstract

A series of novel fluoro-substituted chalcone derivatives have been synthesized. All synthesized compounds were characterized by (1)H nuclear magnetic resonance (NMR), (13)C NMR, and elemental analysis. Their anti-proliferative activities were evaluated against five cancer cells lines, namely, A549, A498, HeLa, A375, and HepG2 using the MTT method. Most of the compounds showed moderate to high activity with IC50 values in the range of 0.029-0.729μM. Of all the synthesized compounds, 10 and 19 exhibited the most potent anti-proliferative activities against cancer cells, and 10 was identified as the most promising compound.
Copyright © 2016 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Anti-proliferative activity; Chalcone; Claisen–Schmidt condensation; Organofluorine; Synthesis

Mesh:

Substances:

Year:  2016        PMID: 27217001     DOI: 10.1016/j.bmcl.2016.04.096

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  9 in total

1.  Novel synthetic chalcones induce apoptosis in the A549 non-small cell lung cancer cells harboring a KRAS mutation.

Authors:  Yiqiang Wang; Andreas Hedblom; Steffi K Koerner; Mailin Li; Finith E Jernigan; Barbara Wegiel; Lijun Sun
Journal:  Bioorg Med Chem Lett       Date:  2016-10-24       Impact factor: 2.823

Review 2.  Chalcone Derivatives: Promising Starting Points for Drug Design.

Authors:  Marcelo N Gomes; Eugene N Muratov; Maristela Pereira; Josana C Peixoto; Lucimar P Rosseto; Pedro V L Cravo; Carolina H Andrade; Bruno J Neves
Journal:  Molecules       Date:  2017-07-25       Impact factor: 4.411

3.  Tertiary amine derivatives of chlorochalcone as acetylcholinesterase (AChE) and buthylcholinesterase (BuChE) inhibitors: the influence of chlorine, alkyl amine side chain and α,β-unsaturated ketone group.

Authors:  Xiao-Hui Gao; Chao Zhou; Hao-Ran Liu; Lin-Bo Liu; Jing-Jing Tang; Xin-Hua Xia
Journal:  J Enzyme Inhib Med Chem       Date:  2016-11-01       Impact factor: 5.051

4.  Design of potent fluoro-substituted chalcones as antimicrobial agents.

Authors:  Serdar Burmaoglu; Oztekin Algul; Arzu Gobek; Derya Aktas Anil; Mahmut Ulger; Busra Gul Erturk; Engin Kaplan; Aylin Dogen; Gönül Aslan
Journal:  J Enzyme Inhib Med Chem       Date:  2017-12       Impact factor: 5.051

5.  Design, Synthesis, and Antibacterial and Antifungal Activities of Novel Trifluoromethyl and Trifluoromethoxy Substituted Chalcone Derivatives.

Authors:  Surendra Babu Lagu; Rajendra Prasad Yejella; Richie R Bhandare; Afzal B Shaik
Journal:  Pharmaceuticals (Basel)       Date:  2020-11-09

6.  Synthesis and in vitro anti-proliferative evaluation of naphthalimide-chalcone/pyrazoline conjugates as potential SERMs with computational validation.

Authors:  Sourav Taru Saha; Mandeep Kaur; Ebenezer Oluwakemi; Paul Awolade; Parvesh Singh; Vipan Kumar
Journal:  RSC Adv       Date:  2020-04-21       Impact factor: 4.036

7.  The synthesis of novel thioderivative chalcones and their influence on NF-κB, STAT3 and NRF2 signaling pathways in colorectal cancer cells.

Authors:  Katarzyna Papierska; Violetta Krajka-Kuźniak; Robert Kleszcz; Tomasz Stefański; Rafał Kurczab; Maciej Kubicki
Journal:  Sci Rep       Date:  2022-09-01       Impact factor: 4.996

8.  Antifungal Activity of Chemical Constituents from Piper pesaresanum C. DC. and Derivatives against Phytopathogen Fungi of Cocoa.

Authors:  Luis C Chitiva-Chitiva; Cristóbal Ladino-Vargas; Luis E Cuca-Suárez; Juliet A Prieto-Rodríguez; Oscar J Patiño-Ladino
Journal:  Molecules       Date:  2021-05-28       Impact factor: 4.411

9.  Synthesis and Evaluation of Antiplasmodial Activity of 2,2,2-Trifluoroethoxychalcones and 2-Fluoroethoxy Chalcones against Plasmodium falciparum in Culture.

Authors:  Kavita Devi; Vinoth Rajendran; T M Rangarajan; Rishi Pal Singh; Prahlad C Ghosh; Manjula Singh
Journal:  Molecules       Date:  2018-05-14       Impact factor: 4.411

  9 in total

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