Publications (2)8.25 Total impact
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Article: Synthetic routes and biological evaluation of largazole and its analogues as potent histone deacetylase inhibitors.
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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.Molecules 01/2011; 16(6):4681-94. · 2.39 Impact Factor -
Article: Total synthesis and biological evaluation of largazole and derivatives with promising selectivity for cancers cells.
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ABSTRACT: The efficient total synthesis of the natural substance largazole is described. Using this strategy, a small library of largazole analogs was developed. Structure-activity relationship studies suggested that the geometry of the alkene in the side chain is critical. While the largazole's analogues with trans-alkene are potent for the antiproliferative effect, those with cis-alkene are completely inactive. Most importantly, replacement of valine with tyrosine in largazole increased selectivity toward human cancer cells over human normal cells more than 100-fold.Organic Letters 02/2010; 12(6):1368-71. · 5.86 Impact Factor
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- Molecules (1)
- Organic Letters (1)
Institutions
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2011
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China Pharmaceutical University
- School of Pharmacy
Nanjing, Jiangxi Sheng, China
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