Isolation, identification, semi-synthesis of aziditaxel derivatives and their biological evaluation

Shu-En Zhang; Jia-Yi Tao; Ying Zhao; Shao-Rong Wang; Di Zhou; Wei-Shuo Fang

doi:10.1080/10286020.2012.672322

Isolation, identification, semi-synthesis of aziditaxel derivatives and their biological evaluation

J Asian Nat Prod Res. 2012;14(5):463-75. doi: 10.1080/10286020.2012.672322.

Authors

Shu-En Zhang¹, Jia-Yi Tao, Ying Zhao, Shao-Rong Wang, Di Zhou, Wei-Shuo Fang

Affiliation

¹ State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, China.

PMID: 22530674
DOI: 10.1080/10286020.2012.672322

Abstract

Two new taxoids (5 and 6) were obtained by isolating impurities in aziditaxel, and their structures were characterized based on data analysis of (1)H NMR, (13)C NMR, HPLC-MS, and through comparison with literature. In order to test their cytotoxicities against human nonsmall lung cancer cell lines (A549), sufficient amounts of compounds 5 and 6 were obtained by semi-synthesis and both of them showed equipotent cytotoxiesty compared with taxol, docetaxel, and aziditaxel.

MeSH terms

Antineoplastic Agents, Phytogenic / chemical synthesis
Antineoplastic Agents, Phytogenic / chemistry
Antineoplastic Agents, Phytogenic / isolation & purification*
Antineoplastic Agents, Phytogenic / pharmacology*
Carcinoma, Non-Small-Cell Lung
Docetaxel
Drug Screening Assays, Antitumor
Humans
Lung Neoplasms
Molecular Structure
Nuclear Magnetic Resonance, Biomolecular
Paclitaxel / pharmacology
Taxoids / chemical synthesis
Taxoids / chemistry
Taxoids / isolation & purification*
Taxoids / pharmacology*

Substances

Antineoplastic Agents, Phytogenic
Taxoids
Docetaxel
Paclitaxel