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.

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