Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4

Diana Lamaa; Hsin Ping Lin; Lena Zig; Cyril Bauvais; Guillaume Bollot; Jérôme Bignon; Helene Levaique; Olivier Pamlard; Joelle Dubois; Mehdi Ouaissi; Martin Souce; Athena Kasselouri; François Saller; Delphine Borgel; Chantal Jayat-Vignoles; Hazar Al-Mouhammad; Jean Feuillard; Karim Benihoud; Mouad Alami; Abdallah Hamze

doi:10.1021/acs.jmedchem.8b00050

Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4

Diana Lamaa, Hsin Ping Lin, Lena Zig, Cyril Bauvais, Guillaume Bollot, Jérôme Bignon, Helene Levaique, Olivier Pamlard, Joelle Dubois, Mehdi Ouaissi, Martin Souce, Athena Kasselouri, François Saller, Delphine Borgel, Chantal Jayat-Vignoles, Hazar Al-Mouhammad, Jean Feuillard, Karim Benihoud, Mouad Alami, Abdallah Hamze

Résultats de recherche: Contribution à un journal › Article › Revue par des pairs

68 Citations (Scopus)

Résumé

Designing multitarget drugs have raised considerable interest due to their advantages in the treatment of complex diseases such as cancer. Their design constitutes a challenge in antitumor drug discovery. The present study reports a dual inhibition of tubulin polymerization and HDAC activity. On the basis of 1,1-diarylethylenes (isoCA-4) and belinostat, a series of hybrid molecules was successfully designed and synthesized. In particular compounds, 5f and 5h were proven to be potent inhibitors of both tubulin polymerization and HDAC8 leading to excellent antiproliferative activity.

langue originale	Anglais
Pages (de - à)	6574-6591
Nombre de pages	18
journal	Journal of Medicinal Chemistry
Volume	61
Numéro de publication	15
Les DOIs	https://doi.org/10.1021/acs.jmedchem.8b00050
état	Publié - 9 août 2018

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10.1021/acs.jmedchem.8b00050

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Lamaa, D., Lin, H. P., Zig, L., Bauvais, C., Bollot, G., Bignon, J., Levaique, H., Pamlard, O., Dubois, J., Ouaissi, M., Souce, M., Kasselouri, A., Saller, F., Borgel, D., Jayat-Vignoles, C., Al-Mouhammad, H., Feuillard, J., Benihoud, K., Alami, M., & Hamze, A. (2018). Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4. Journal of Medicinal Chemistry, 61(15), 6574-6591. https://doi.org/10.1021/acs.jmedchem.8b00050

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title = "Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4",

abstract = "Designing multitarget drugs have raised considerable interest due to their advantages in the treatment of complex diseases such as cancer. Their design constitutes a challenge in antitumor drug discovery. The present study reports a dual inhibition of tubulin polymerization and HDAC activity. On the basis of 1,1-diarylethylenes (isoCA-4) and belinostat, a series of hybrid molecules was successfully designed and synthesized. In particular compounds, 5f and 5h were proven to be potent inhibitors of both tubulin polymerization and HDAC8 leading to excellent antiproliferative activity.",

author = "Diana Lamaa and Lin, {Hsin Ping} and Lena Zig and Cyril Bauvais and Guillaume Bollot and J{\'e}r{\^o}me Bignon and Helene Levaique and Olivier Pamlard and Joelle Dubois and Mehdi Ouaissi and Martin Souce and Athena Kasselouri and Fran{\c c}ois Saller and Delphine Borgel and Chantal Jayat-Vignoles and Hazar Al-Mouhammad and Jean Feuillard and Karim Benihoud and Mouad Alami and Abdallah Hamze",

note = "Publisher Copyright: {\textcopyright} 2018 American Chemical Society.",

year = "2018",

month = aug,

day = "9",

doi = "10.1021/acs.jmedchem.8b00050",

language = "English",

volume = "61",

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journal = "Journal of Medicinal Chemistry",

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Lamaa, D, Lin, HP, Zig, L, Bauvais, C, Bollot, G, Bignon, J, Levaique, H, Pamlard, O, Dubois, J, Ouaissi, M, Souce, M, Kasselouri, A, Saller, F, Borgel, D, Jayat-Vignoles, C, Al-Mouhammad, H, Feuillard, J, Benihoud, K, Alami, M & Hamze, A 2018, 'Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4', Journal of Medicinal Chemistry, VOL. 61, Numéro 15, p. 6574-6591. https://doi.org/10.1021/acs.jmedchem.8b00050

TY - JOUR

T1 - Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4

AU - Lamaa, Diana

AU - Lin, Hsin Ping

AU - Zig, Lena

AU - Bauvais, Cyril

AU - Bollot, Guillaume

AU - Bignon, Jérôme

AU - Levaique, Helene

AU - Pamlard, Olivier

AU - Dubois, Joelle

AU - Ouaissi, Mehdi

AU - Souce, Martin

AU - Kasselouri, Athena

AU - Saller, François

AU - Borgel, Delphine

AU - Jayat-Vignoles, Chantal

AU - Al-Mouhammad, Hazar

AU - Feuillard, Jean

AU - Benihoud, Karim

AU - Alami, Mouad

AU - Hamze, Abdallah

PY - 2018/8/9

Y1 - 2018/8/9

N2 - Designing multitarget drugs have raised considerable interest due to their advantages in the treatment of complex diseases such as cancer. Their design constitutes a challenge in antitumor drug discovery. The present study reports a dual inhibition of tubulin polymerization and HDAC activity. On the basis of 1,1-diarylethylenes (isoCA-4) and belinostat, a series of hybrid molecules was successfully designed and synthesized. In particular compounds, 5f and 5h were proven to be potent inhibitors of both tubulin polymerization and HDAC8 leading to excellent antiproliferative activity.

AB - Designing multitarget drugs have raised considerable interest due to their advantages in the treatment of complex diseases such as cancer. Their design constitutes a challenge in antitumor drug discovery. The present study reports a dual inhibition of tubulin polymerization and HDAC activity. On the basis of 1,1-diarylethylenes (isoCA-4) and belinostat, a series of hybrid molecules was successfully designed and synthesized. In particular compounds, 5f and 5h were proven to be potent inhibitors of both tubulin polymerization and HDAC8 leading to excellent antiproliferative activity.

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