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

Caihong Li; Yatao Qiu; Xing Li; Nianjin Liu; Zhiyi Yao

doi:10.1016/j.bmcl.2013.12.083

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. Epub 2013 Dec 27.

Authors

Caihong Li¹, Yatao Qiu², Xing Li¹, Nianjin Liu¹, Zhiyi Yao³

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Antineoplastic Agents / chemical synthesis
Antineoplastic Agents / chemistry*
Antineoplastic Agents / pharmacology*
Biological Assay
Cell Line, Tumor
Cell Proliferation / drug effects
Docetaxel
Humans
Molecular Conformation
Molecular Structure
Paclitaxel / chemical synthesis
Paclitaxel / chemistry
Paclitaxel / pharmacology
Taxoids / chemistry*
Taxoids / pharmacology*

Substances

Antineoplastic Agents
Taxoids
Docetaxel
Paclitaxel