Synthesis, Biological Evaluation, and Computer-Aided Drug Designing of New Derivatives of Hyperactive Suberoylanilide Hydroxamic Acid Histone Deacetylase Inhibitors

2015 ◽  
Vol 86 (4) ◽  
pp. 795-804 ◽  
Author(s):  
Song Zhang ◽  
Weibin Huang ◽  
Xiaonan Li ◽  
Zhicheng Yang ◽  
Binghong Feng
Keyword(s):  
Histone Deacetylase ◽  
Hydroxamic Acid ◽  
Histone Deacetylase Inhibitors ◽  
Biological Evaluation ◽  
Suberoylanilide Hydroxamic Acid ◽  
Computer Aided ◽  
Drug Designing ◽  
Derivatives Of

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.

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.

Sign in / Sign up

Export Citation Format

Share Document