Biological evaluation of new antitumor taxoids: alteration of substitution at the C-7 and C-10 of docetaxel

Bioorg Med Chem Lett. 2014 Feb 1;24(3):855-9. doi: 10.1016/j.bmcl.2013.12.083.

Caihong Li ¹, Yatao Qiu ², Xing Li ¹, Nianjin Liu ¹, Zhiyi Yao ³

Affiliations

1 College of Chemical and Environmental Engineering, Shanghai Institute of Technology, Shanghai 210032, China.
2 Laboratory of Regenerative Biology, Guangzhou Institute of Biomedicine and Health, Chinese Academy of Sciences, Guangzhou 510530, China.
3 College of Chemical and Environmental Engineering, Shanghai Institute of Technology, Shanghai 210032, China. Electronic address: yao99cn@sit.edu.cn.

PMID: 24405702 DOI: 10.1016/j.bmcl.2013.12.083

Abstract

A series of new docetaxol analogues have been designed and synthesized. And their cytotoxicities against Cancer cells have been evaluated by MTT method. Most of these compounds showed selective inhibitions on human Cancer cell lines. Among them, compound 8 exhibited higher inhibitory activity than Paclitaxel (Taxol) against several Cancer cell lines. This work indicated that appropriate modification at C-7 and C-10 of docetaxel might be a promising approach for this unique class of Anticancer compounds.

Keywords

Analogues; Antitumor; Biological assays; Cabazitaxel; Paclitaxel.

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