Natural product-based design, synthesis and biological evaluation of anthra[2,1-d]thiazole-6,11-dione derivatives from rhein as novel antitumour agents

  • Eur J Med Chem. 2014 Sep 12:84:505-15. doi: 10.1016/j.ejmech.2014.07.047.
Yu-Kun Liang  1 ,  Zhi-Zhou Yue  2 ,  Jia-Xin Li  3 ,  Cun Tan  3 ,  Ze-Hong Miao  4 ,  Wen-Fu Tan  5 ,  Chun-Hao Yang  6
Affiliations
  • 1. Department of Pharmaceutical Engineering, School of Chemical Engineering, Wuhan University of Technology, 205 Luo Shi Road, Wuhan, Hubei 430070, PR China; State Key Laboratory of Drug Research, Shanghai Institute of MateriaMedica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai 201203, PR China.
  • 2. Department of Pharmaceutical Engineering, School of Chemical Engineering, Wuhan University of Technology, 205 Luo Shi Road, Wuhan, Hubei 430070, PR China.
  • 3. State Key Laboratory of Drug Research, Shanghai Institute of MateriaMedica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai 201203, PR China.
  • 4. State Key Laboratory of Drug Research, Shanghai Institute of MateriaMedica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai 201203, PR China. Electronic address: [email protected].
  • 5. School of Pharmacy, Fudan University, 826 Zhang Heng Road, Shanghai 201203, PR China.
  • 6. State Key Laboratory of Drug Research, Shanghai Institute of MateriaMedica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai 201203, PR China. Electronic address: [email protected].
PMID: 25050882 DOI: 10.1016/j.ejmech.2014.07.047
Abstract

Two series of novel 2-substituted 5,7-dihydroxyanthra[2,1-d]thiazole-6,11-dione derivatives from natural rhein were designed, synthesized and evaluated for their antitumour activities against human Cancer cell lines A549 and HeLa in vitro.

Keywords
Anthra[2,1-d]thiazole-6,11-dione; Antitumour; Rhein analogues; SRB assay.