Molecules 2007, 12(5), 1125-1135; doi:10.3390/12051125
Article

Synthesis of Sulfonamides and Evaluation of Their Histone Deacetylase (HDAC) Activity

Seikwan Oh 1 , Hyung–In Moon 2 email, Il–Hong Son 2 email and Jae–Chul Jung 1,* email
1 Department of Neuroscience and Medical Research Institute, College of Medicine, Ewha Womans University, Seoul 158–710, South Korea 2 Department of Neuroscience and Inam Neuro Science Research Center, Wonkwang University Sanbon Medical Center, Sanbondong, Gunpocity, Kyunggido, 435-040, South Korea
* Author to whom correspondence should be addressed.
Received: 17 April 2007; in revised form: 18 May 2007 / Accepted: 18 May 2007 / Published: 24 May 2007
PDF Full-text Download PDF Full-Text [83 KB, uploaded 2 October 2008 11:53 CEST]
Abstract: A simple synthesis of sulfonamides 4–22 as novel histone deacetylase (HDAC) inhibitors is described. The key synthetic strategies involve N–sulfonylation of L–proline benzyl ester hydrochloride (2) and coupling reaction of N–sulfonyl chloride 3 with amines in high yields. It was found that several compounds showed good cellular potency with the most potent compound 20 exhibiting an IC50 = 2.8 μM in vitro.
Keywords: HDAC; N–Sulfonylation; Coupling reaction; Anticancer

Correction

Article Statistics

Click here to load and display the download statistics.

Cite This Article

MDPI and ACS Style

Oh, S.; Moon, H.; Son, I.; Jung, J. Synthesis of Sulfonamides and Evaluation of Their Histone Deacetylase (HDAC) Activity. Molecules 2007, 12, 1125-1135.

AMA Style

Oh S, Moon H, Son I, Jung J. Synthesis of Sulfonamides and Evaluation of Their Histone Deacetylase (HDAC) Activity. Molecules. 2007; 12(5):1125-1135.

Chicago/Turabian Style

Oh, Seikwan; Moon, Hyung–In; Son, Il–Hong; Jung, Jae–Chul. 2007. "Synthesis of Sulfonamides and Evaluation of Their Histone Deacetylase (HDAC) Activity." Molecules 12, no. 5: 1125-1135.

Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert