Design, synthesis and preliminary bioactivity studies of 1, 3, 4-thiadiazole hydroxamic acid derivatives as novel histone deacetylase inhibitors

P Guan, F Sun, X Hou, F Wang, F Yi, W Xu…

Index: Guan, Peng; Sun, Feng'E; Hou, Xuben; Wang, Feng; Yi, Fan; Xu, Wenfang; Fang, Hao Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 12 p. 3865 - 3872

Full Text: HTML

Citation Number: 30

Abstract

Histone deacetylase (HDAC) inhibitors have emerged as a new class of anticancer agents, targeting the biological processes including cell cycle, apoptosis and differentiation. In the present study, a series of 1, 3, 4-thiadiazole based hydroxamic acids were developed as potent HDAC inhibitors. Some of them showed good inhibitory activity in HDAC enzyme assay and potent growth inhibition in some tumor cell lines. Among them, compound 6i ( ...

Related Articles:

A New Method for Constructing Quaternary Carbon Centres: Tandem Rhodium??Catalysed 1, 4??Addition/Intramolecular Cyclisation

[Le Notre, Jerome; Van Mele, David; Frost, Christopher G. Advanced Synthesis and Catalysis, 2007 , vol. 349, # 3 p. 432 - 440]

Synthesis of 10, 11-dihydroleukotriene B4 metabolites via a nickel-catalyzed coupling reaction of cis-bromides and trans-alkenyl borates

[Nakayama, Yuji; Kumar, G. Biju; Kobayashi, Yuichi Journal of Organic Chemistry, 2000 , vol. 65, # 3 p. 707 - 715]

Effects of counter cations in selective monohydrolyses of symmetric diesters

[Bulletin of the Chemical Society of Japan, , vol. 78, # 3 p. 498 - 500]

Enantiotopically selective oxidation of. alpha.,. omega.-diols with enzyme systems of microorganisms

[Ohta, Hiromichi; Tetsukawa, Hatsuki; Noto, Naoko Journal of Organic Chemistry, 1982 , vol. 47, # 12 p. 2400 - 2404]

Selective monomethyl esterification of dicarboxylic acids by use of monocarboxylate chemisorption on alumina

[Journal of the American Chemical Society, , vol. 107, # 5 p. 1365 - 1369]

More Articles...