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

Molecules

Shang Li¹  Hequan Yao¹  Jinyi Xu¹ 

[1] ¹School of Pharmacy, China Pharmaceutical University, Nanjing, Jiangsu 210009, China ²Shanghai Institute of Technology, Shanghai 210032, China ³Laboratory of Peptide Chemistry, Guangzhou Institute of Biomedicine and Health, CAS, Guangzhou, Guangdong 510530, China

关键词: largazole;    histone deacetylase inhibitor;    natural products;    total synthesis;    biological evaluation;   

DOI  :  10.3390/molecules16064681

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.