TY  - JOUR
AU  - Bouchet, Samuel
AU  - Linot, Camille
AU  - Ružić, Dušan
AU  - Agbaba, Danica
AU  - Fouchaq, Benoit
AU  - Roche, Joelle
AU  - Nikolić, Katarina
AU  - Blanquart, Christophe
AU  - Bertrand, Philippe
PY  - 2019
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/3354
AB  - Dissymmetric cross metathesis of alkenes as a convergent and general synthetic strategy allowed for the preparation of a new small series of human histone deacetylases (HDAC) inhibitors. Alkenes bearing Bocprotected hydroxamic acid and benzamide and trityl-protected thiols were used to provide the zinc binding groups and were reacted with alkenes bearing aromatic cap groups. One compound was identified as a selective HDAC6 inhibitor lead. Additional biological evaluation in cancer cell lines demonstrated its ability to stimulate the expression of the epithelial marker E-cadherin and tumor suppressor genes like SEMA3F and p21, suggesting a potential use of this compound for lung cancer treatment. Molecular docking on all 11 HDAC isoforms was used to rationalize the observed biological results.
PB  - Amer Chemical Soc, Washington
T2  - ACS Medicinal Chemistry Letters
T1  - Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling
VL  - 10
IS  - 6
SP  - 863
EP  - 868
DO  - 10.1021/acsmedchemlett.8b00440
ER  - 

@article{
author = "Bouchet, Samuel and Linot, Camille and Ružić, Dušan and Agbaba, Danica and Fouchaq, Benoit and Roche, Joelle and Nikolić, Katarina and Blanquart, Christophe and Bertrand, Philippe",
year = "2019",
abstract = "Dissymmetric cross metathesis of alkenes as a convergent and general synthetic strategy allowed for the preparation of a new small series of human histone deacetylases (HDAC) inhibitors. Alkenes bearing Bocprotected hydroxamic acid and benzamide and trityl-protected thiols were used to provide the zinc binding groups and were reacted with alkenes bearing aromatic cap groups. One compound was identified as a selective HDAC6 inhibitor lead. Additional biological evaluation in cancer cell lines demonstrated its ability to stimulate the expression of the epithelial marker E-cadherin and tumor suppressor genes like SEMA3F and p21, suggesting a potential use of this compound for lung cancer treatment. Molecular docking on all 11 HDAC isoforms was used to rationalize the observed biological results.",
publisher = "Amer Chemical Soc, Washington",
journal = "ACS Medicinal Chemistry Letters",
title = "Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling",
volume = "10",
number = "6",
pages = "863-868",
doi = "10.1021/acsmedchemlett.8b00440"
}

Bouchet, S., Linot, C., Ružić, D., Agbaba, D., Fouchaq, B., Roche, J., Nikolić, K., Blanquart, C.,& Bertrand, P.. (2019). Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling. in ACS Medicinal Chemistry Letters
Amer Chemical Soc, Washington., 10(6), 863-868.
https://doi.org/10.1021/acsmedchemlett.8b00440

Bouchet S, Linot C, Ružić D, Agbaba D, Fouchaq B, Roche J, Nikolić K, Blanquart C, Bertrand P. Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling. in ACS Medicinal Chemistry Letters. 2019;10(6):863-868.
doi:10.1021/acsmedchemlett.8b00440 .

Bouchet, Samuel, Linot, Camille, Ružić, Dušan, Agbaba, Danica, Fouchaq, Benoit, Roche, Joelle, Nikolić, Katarina, Blanquart, Christophe, Bertrand, Philippe, "Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling" in ACS Medicinal Chemistry Letters, 10, no. 6 (2019):863-868,
https://doi.org/10.1021/acsmedchemlett.8b00440 . .

TY  - CONF
AU  - Bouchet, Samuel
AU  - Linot, Camille
AU  - Ružić, Dušan
AU  - Agbaba, Danica
AU  - Fouchaq, Benoit
AU  - Roche, Joëlle
AU  - Nikolić, Katarina
AU  - Cuendet, Muriel
AU  - Ovádi, Judit
AU  - Blanquart, Christophe
AU  - Bertrand, Philippe
PY  - 2017
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/4926
PB  - European Cooperation in Science and Technology (COST)
C3  - EpiChemBio (CM1406) and MuTaLig (CA15135) COST actions joint meeting 2017 Porto (PT), Sept 22-24 2017
T1  - Cross metathesis for the synthesis of HDAC inhibitors. Potential in multitarget drug design
SP  - 19
EP  - 19
UR  - https://hdl.handle.net/21.15107/rcub_farfar_4926
ER  - 

@conference{
author = "Bouchet, Samuel and Linot, Camille and Ružić, Dušan and Agbaba, Danica and Fouchaq, Benoit and Roche, Joëlle and Nikolić, Katarina and Cuendet, Muriel and Ovádi, Judit and Blanquart, Christophe and Bertrand, Philippe",
year = "2017",
publisher = "European Cooperation in Science and Technology (COST)",
journal = "EpiChemBio (CM1406) and MuTaLig (CA15135) COST actions joint meeting 2017 Porto (PT), Sept 22-24 2017",
title = "Cross metathesis for the synthesis of HDAC inhibitors. Potential in multitarget drug design",
pages = "19-19",
url = "https://hdl.handle.net/21.15107/rcub_farfar_4926"
}

Bouchet, S., Linot, C., Ružić, D., Agbaba, D., Fouchaq, B., Roche, J., Nikolić, K., Cuendet, M., Ovádi, J., Blanquart, C.,& Bertrand, P.. (2017). Cross metathesis for the synthesis of HDAC inhibitors. Potential in multitarget drug design. in EpiChemBio (CM1406) and MuTaLig (CA15135) COST actions joint meeting 2017 Porto (PT), Sept 22-24 2017
European Cooperation in Science and Technology (COST)., 19-19.
https://hdl.handle.net/21.15107/rcub_farfar_4926

Bouchet S, Linot C, Ružić D, Agbaba D, Fouchaq B, Roche J, Nikolić K, Cuendet M, Ovádi J, Blanquart C, Bertrand P. Cross metathesis for the synthesis of HDAC inhibitors. Potential in multitarget drug design. in EpiChemBio (CM1406) and MuTaLig (CA15135) COST actions joint meeting 2017 Porto (PT), Sept 22-24 2017. 2017;:19-19.
https://hdl.handle.net/21.15107/rcub_farfar_4926 .

Bouchet, Samuel, Linot, Camille, Ružić, Dušan, Agbaba, Danica, Fouchaq, Benoit, Roche, Joëlle, Nikolić, Katarina, Cuendet, Muriel, Ovádi, Judit, Blanquart, Christophe, Bertrand, Philippe, "Cross metathesis for the synthesis of HDAC inhibitors. Potential in multitarget drug design" in EpiChemBio (CM1406) and MuTaLig (CA15135) COST actions joint meeting 2017 Porto (PT), Sept 22-24 2017 (2017):19-19,
https://hdl.handle.net/21.15107/rcub_farfar_4926 .