Synthesis and biological evaluation of novel 3'-N-tert-butylsulfonyl analogues of docetaxel

Bowen Ke; Yong Qin; Fengyan Zhao; Yi Qu

doi:10.1016/j.bmcl.2008.07.101

Synthesis and biological evaluation of novel 3'-N-tert-butylsulfonyl analogues of docetaxel

Bioorg Med Chem Lett. 2008 Sep 1;18(17):4783-5. doi: 10.1016/j.bmcl.2008.07.101. Epub 2008 Jul 29.

Authors

Bowen Ke¹, Yong Qin, Fengyan Zhao, Yi Qu

Affiliation

¹ Department of Chemistry of Medicinal Natural Products, Key Laboratory of Drug Targeting and Drug Delivery System of Ministry of Education, West China School of Pharmacy, Sichuan University, Chengdu 610041, PR China.

PMID: 18701281
DOI: 10.1016/j.bmcl.2008.07.101

Abstract

Novel 3'-N-tert-butylsulfonyl analogues 10a-c of docetaxel were synthesized and their biological evaluation in cytotoxicity in vitro against several human tumor cell lines were presented. The biologically tested results showed that N-oxide pyridyl substituted10b-c had potent cytotoxicities against human tumor cell lines Eca-109, SKOV3, SMMC-7721, HCT-8, PC3, MCF-7, HeLa and KB.

Publication types

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

MeSH terms

Antineoplastic Agents / chemical synthesis*
Antineoplastic Agents / pharmacology*
Antineoplastic Agents, Phytogenic / pharmacology
Docetaxel
Drug Screening Assays, Antitumor*
HeLa Cells
Humans
KB Cells
Paclitaxel / chemistry
Paclitaxel / pharmacology
Sulfonic Acids / chemical synthesis*
Sulfonic Acids / pharmacology
Taxoids / chemical synthesis*
Taxoids / pharmacology*

Substances

Antineoplastic Agents
Antineoplastic Agents, Phytogenic
Sulfonic Acids
Taxoids
Docetaxel
Paclitaxel