Literature DB >> 16913727

Synthesis and cytotoxic evaluation of combretafurans, potential scaffolds for dual-action antitumoral agents.

Tracey Pirali1, Sara Busacca, Lorena Beltrami, Daniela Imovilli, Francesca Pagliai, Gianluca Miglio, Alberto Massarotti, Luisella Verotta, Gian Cesare Tron, Giovanni Sorba, Armando A Genazzani.   

Abstract

We have synthesized rigid analogues of combretastatin bearing a furan ring in place of the olefinic bridge. These compounds are cytotoxic at nanomolar concentrations in neuroblastoma cells, display a similar structure-activity relationship compared to combretastatin A4, and inhibit tubulin polymerization. We also show that the furan ring can be further functionalized. Thus, it is possible that combretafurans could act as scaffolds for the development of dual-action antitumoral agents.

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Year:  2006        PMID： 16913727     DOI： 10.1021/jm060621o

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


  8 in total

1.  Structural simplification of bioactive natural products with multicomponent synthesis: dihydropyridopyrazole analogues of podophyllotoxin.

Authors:  Igor V Magedov; Madhuri Manpadi; Elena Rozhkova; Nikolai M Przheval'skii; Snezna Rogelj; Scott T Shors; Wim F A Steelant; Severine Van slambrouck; Alexander Kornienko
Journal:  Bioorg Med Chem Lett       Date:  2006-12-06       Impact factor: 2.823

2.  Combretastatin A-4 derivatives: synthesis and evaluation of 2,4,5-triaryl-1H-imidazoles as potential agents against H1299 (non-small cell lung cancer cell).

Authors:  Chih-Hua Tseng; Chi-Yi Li; Chien-Chih Chiu; Huei-Ting Hu; Chein-Hwa Han; Yeh-Long Chen; Cherng-Chyi Tzeng
Journal:  Mol Divers       Date:  2012-09-26       Impact factor: 2.943

3.  Development of selective estrogen receptor modulator (SERM)-like activity through an indirect mechanism of estrogen receptor antagonism: defining the binding mode of 7-oxabicyclo[2.2.1]hept-5-ene scaffold core ligands.

Authors:  Yangfan Zheng; Manghong Zhu; Sathish Srinivasan; Jerome C Nwachukwu; Valerie Cavett; Jian Min; Kathryn E Carlson; Pengcheng Wang; Chune Dong; John A Katzenellenbogen; Kendall W Nettles; Hai-Bing Zhou
Journal:  ChemMedChem       Date:  2012-04-19       Impact factor: 3.466

4.  Design, synthesis, and biological evaluation of (E)-N-aryl-2-arylethenesulfonamide analogues as potent and orally bioavailable microtubule-targeted anticancer agents.

Authors:  M V Ramana Reddy; Muralidhar R Mallireddigari; Venkat R Pallela; Stephen C Cosenza; Vinay K Billa; Balaiah Akula; D R C Venkata Subbaiah; E Vijaya Bharathi; Amol Padgaonkar; Hua Lv; James M Gallo; E Premkumar Reddy
Journal:  J Med Chem       Date:  2013-06-25       Impact factor: 7.446

5.  (Z)-1-aryl-3-arylamino-2-propen-1-ones, highly active stimulators of tubulin polymerization: synthesis, structure-activity relationship (SAR), tubulin polymerization, and cell growth inhibition studies.

Authors:  M V Ramana Reddy; Balaiah Akula; Stephen C Cosenza; Clement M Lee; Muralidhar R Mallireddigari; Venkat R Pallela; D R C Venkata Subbaiah; Andrew Udofa; E Premkumar Reddy
Journal:  J Med Chem       Date:  2012-05-25       Impact factor: 7.446

6.  Design and synthesis of new trimethoxylphenyl-linked combretastatin analogues loaded on diamond nanoparticles as a panel for ameliorated solubility and antiproliferative activity.

Authors:  Islam Zaki; Amal M Y Moustafa; Botros Y Beshay; Reham E Masoud; Mohammed A I Elbastawesy; Mohammed A S Abourehab; Mohamed Y Zakaria
Journal:  J Enzyme Inhib Med Chem       Date:  2022-12       Impact factor: 5.756

Review 7.  Tubulin-interactive stilbene derivatives as anticancer agents.

Authors:  Renata Mikstacka; Tomasz Stefański; Jakub Różański
Journal:  Cell Mol Biol Lett       Date:  2013-07-01       Impact factor: 5.787

8.  Exploring Diverse-Ring Analogues on Combretastatin A4 (CA-4) Olefin as Microtubule-Targeting Agents.

Authors:  Ming-Yu Song; Qiu-Rui He; Yi-Lin Wang; Hao-Ran Wang; Tian-Cheng Jiang; Jiang-Jiang Tang; Jin-Ming Gao
Journal:  Int J Mol Sci       Date:  2020-03-06       Impact factor: 5.923
  8 in total

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