synthetic routes and biological evaluation of largazole and its analogues as potent histone deacetylase inhibitors合成路线和生物评价largazole及其类似物作为有效的组蛋白脱乙酰酶抑制剂.pdf

Molecules 2011, 16, 4681-4694; doi:10.3390/molecules OPEN ACCESS molecules ISSN 1420-3049 /journal/molecules Review Synthetic Routes and Biological Evaluation of Largazole and Its Analogues as Potent Histone Deacetylase Inhibitors Shang Li 1,2,3, Hequan Yao 1, Jinyi Xu 1,* and Sheng Jiang 2,3,* 1 School of Pharmacy, China Pharmaceutical University, Nanjing, Jiangsu 210009, China; Tel.: +86 25 Fax: +86 25 2 Shanghai Institute of Technology, Shanghai 210032, China 3 Laboratory of Peptide Chemistry, Guangzhou Institute of Biomedicine and Health, CAS, Guangzhou, Guangdong 510530, China; Tel.: +86 Fax: +86 20 * Authors to whom correspondence should be addressed; E-Mails: jinyixu@ (J.X.); jiang_sheng@ (S.J.). 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 o