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Synthetic Routes and Biological Evaluation of Largazole and Its Analogues as Potent Histone Deacetylase Inhibitors
School of Pharmacy, China Pharmaceutical University, Nanjing, Jiangsu 210009, China
Shanghai Institute of Technology, Shanghai 210032, China
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; in revised form: 13 May 2011 / Accepted: 18 May 2011 / Published: 7 June 2011
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
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Cite This Article
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.
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(6):4681-4694.
Li, Shang; Yao, Hequan; Xu, Jinyi; Jiang, Sheng. 2011. "Synthetic Routes and Biological Evaluation of Largazole and Its Analogues as Potent Histone Deacetylase Inhibitors." Molecules 16, no. 6: 4681-4694.