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 . .