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Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling

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2019
Authors
Bouchet, Samuel
Linot, Camille
Ružić, Dušan
Agbaba, Danica
Fouchaq, Benoit
Roche, Joelle
Nikolić, Katarina
Blanquart, Christophe
Bertrand, Philippe
Article (Published version)
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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.
Keywords:
Cross metathesis / histone deacetylases / lung cancer / epigenetics / molecular modeling
Source:
ACS Medicinal Chemistry Letters, 2019, 10, 6, 863-868
Publisher:
  • Amer Chemical Soc, Washington
Projects:
  • Synthesis, Quantitative Structure and Activity Relationship, Physico-Chemical Characterisation and Analysis of Pharmacologically Active Substances (RS-172033)

DOI: 10.1021/acsmedchemlett.8b00440

ISSN: 1948-5875

PubMed: 31223439

WoS: 000471834600006

Scopus: 2-s2.0-85066886661
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URI
http://farfar.pharmacy.bg.ac.rs/handle/123456789/3354
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  • Radovi istraživača / Researchers’ publications
Institution
Pharmacy

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