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Molecules 2011, 16(6), 4681-4694; doi:10.3390/molecules16064681

Synthetic Routes and Biological Evaluation of Largazole and Its Analogues as Potent Histone Deacetylase Inhibitors

1,2,3, 1, 1,* and 2,3,*
1
School of Pharmacy, China Pharmaceutical University, Nanjing, Jiangsu 210009, China
2
Shanghai Institute of Technology, Shanghai 210032, China
3
Laboratory of Peptide Chemistry, Guangzhou Institute of Biomedicine and Health, CAS, Guangzhou, Guangdong 510530, China
*
Authors to whom correspondence should be addressed.
Received: 25 April 2011 / Revised: 13 May 2011 / Accepted: 18 May 2011 / Published: 7 June 2011
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Abstract

Natural products with interesting biological properties and structural diversity have often served as valuable lead drug candidates for the treatment of various human diseases. Largazole, isolated from the marine cyanobacterium Symploca sp. has exhibited potent inhibitory activity against many cancer cell lines. Besides, it shows remarkable selectivity between transformed and nontransformed cells, which is the main disadvantage of other antitumor natural products such as paclitaxel and actinomycin D. Due to its potential as a potent and selective anticancer drug candidate, a great deal of attention has been focused on largazole and its analogues. It is the aim of this review to highlight synthetic aspects of largazole and its analogues as well as their preliminary structure–activity relationship studies.
Keywords: largazole; histone deacetylase inhibitor; natural products; total synthesis; biological evaluation largazole; histone deacetylase inhibitor; natural products; total synthesis; biological evaluation
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Li, S.; Yao, H.; Xu, J.; Jiang, S. Synthetic Routes and Biological Evaluation of Largazole and Its Analogues as Potent Histone Deacetylase Inhibitors. Molecules 2011, 16, 4681-4694.

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