Synthesis and biological evaluation of new taxoids derived from 2-deacetoxytaxinine J

Maurizio Botta; Silvia Armaroli; Daniele Castagnolo; Gabriele Fontana; Paula Pera; Ezio Bombardelli

doi:10.1016/j.bmcl.2006.12.101

Synthesis and biological evaluation of new taxoids derived from 2-deacetoxytaxinine J

Bioorg Med Chem Lett. 2007 Mar 15;17(6):1579-83. doi: 10.1016/j.bmcl.2006.12.101. Epub 2007 Jan 8.

Authors

Maurizio Botta¹, Silvia Armaroli, Daniele Castagnolo, Gabriele Fontana, Paula Pera, Ezio Bombardelli

Affiliation

¹ Dipartimento Farmaco Chimico Tecnologico, Università degli Studi di Siena, via A. Moro, 53100 Siena, Italy. [email protected]

PMID: 17254787
DOI: 10.1016/j.bmcl.2006.12.101

Abstract

A small library of 2-deacetoxytaxinine J (DAT-J) 1 derivatives was synthesised and tested in vitro for their reversal activity in human mammary carcinoma MDR cell line MCF7-R. One of the new taxoids showed to be active at 0.1 microM when tested in combination with paclitaxel.

Publication types

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

MeSH terms

Antineoplastic Agents, Phytogenic / chemical synthesis*
Antineoplastic Agents, Phytogenic / pharmacology*
Breast Neoplasms / drug therapy
Breast Neoplasms / pathology
Cell Line, Tumor
Drug Resistance, Neoplasm
Female
Genes, MDR / genetics
Humans
Indicators and Reagents
Taxoids / chemical synthesis*
Taxoids / pharmacology*

Substances

2-deacetoxytaxinine J
Antineoplastic Agents, Phytogenic
Indicators and Reagents
Taxoids