scholarly journals Design and Synthesis of Small Molecules Based on a Substructural Analysis of the Histone Deacetylase Inhibitors TSA and SAHA

2011 ◽  
Vol 8 (3) ◽  
pp. 1394-1400
Author(s):  
Lynda Ekou ◽  
Tchirioua Ekou ◽  
Javier Garcia ◽  
Isabelle Opalinski ◽  
Jean Pierre Gesson
Keyword(s):  
Small Molecules ◽  
Histone Deacetylase ◽  
Histone Deacetylases ◽  
Hydroxamic Acid ◽  
Histone Deacetylase Inhibitors ◽  
Suberoylanilide Hydroxamic Acid ◽  
Considerable Potential ◽  
Design And Synthesis

Inhibitors of histone deacetylases (HDACs) are patent inducers of differentiation and bear considerable potential as drugs for chemoprevention and treatment of cancer. In this paper, we have investigated three synthetic, inhibitors A1a,b, A2a. Analogue hybrid trichostatine A (TSA), suberoylanilide hydroxamic acid SAHA, in order to seek new histone deacetylases (HDACs) inhibitors.

Potential Role of Histone Deacetylase Inhibitors in Mesothelioma: Clinical Experience with Suberoylanilide Hydroxamic Acid

2006 ◽  
Vol 7 (4) ◽  
pp. 257-261 ◽  
Author(s):  
Lee M. Krug ◽  
Tracy Curley ◽  
Lawrence Schwartz ◽  
Stacie Richardson ◽  
Paul Marks ◽  
...  
Keyword(s):  
Histone Deacetylase ◽  
Clinical Experience ◽  
Hydroxamic Acid ◽  
Histone Deacetylase Inhibitors ◽  
Potential Role ◽  
Suberoylanilide Hydroxamic Acid

scholarly journals Histone Deacetylase Inhibitors: Synthesis of Tetrapeptide Analogue SAHA/TPX

2011 ◽  
Vol 8 (s1) ◽  
pp. S79-S84
Author(s):  
Lynda Ekou ◽  
Tchirioua Ekou ◽  
Isabelle Opalinski ◽  
Jean Pierre Gesson
Keyword(s):  
Clinical Trial ◽  
Cancer Therapy ◽  
Phase I ◽  
Histone Deacetylase ◽  
Hydroxamic Acid ◽  
Histone Deacetylase Inhibitors ◽  
Hdac Inhibitors ◽  
Growth Arrest ◽  
Suberoylanilide Hydroxamic Acid ◽  
Specific Inhibitors

The inhibition of HDAC (histone deacetylase) activity by specific inhibitors induces growth arrest, differentiation and apoptosis of transformed or several cancer cells. Some of these inhibitors are in clinical trial at phase I or phase II. The discovery and development of specific HDAC inhibitors are helpful for cancer therapy. In this paper we describe the synthesis of simple inhibitorBhybrid analogue suberoylanilide hydroxamic acid (SAHA), trapoxinB(TPX B) in as little as five steps. This compound is interesting lead for the design of potent inhibitors of histone deacetylase.

SCRIPTAID AND SUBEROYLANILIDE HYDROXAMIC ACID ARE HISTONE DEACETYLASE INHIBITORS WITH POTENT ANTI–TOXOPLASMA GONDII ACTIVITY IN VITRO

2007 ◽  
Vol 93 (3) ◽  
pp. 694-700 ◽  
Author(s):  
Jeannine S. Strobl ◽  
Meredith Cassell ◽  
Sheila M. Mitchell ◽  
Christopher M. Reilly ◽  
David S. Lindsay
Keyword(s):  
Toxoplasma Gondii ◽  
Histone Deacetylase ◽  
Hydroxamic Acid ◽  
Histone Deacetylase Inhibitors ◽  
Suberoylanilide Hydroxamic Acid
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