Synthesis and in vitro antitumor activity of 4(3H)-quinazolinone derivatives with dithiocarbamate side chains

Sheng-Li Cao; Yu-Ping Feng; Yu-Yang Jiang; Shi-Ying Liu; Guo-Yu Ding; Run-Tao Li

doi:10.1016/j.bmcl.2005.01.083

Synthesis and in vitro antitumor activity of 4(3H)-quinazolinone derivatives with dithiocarbamate side chains

Bioorg Med Chem Lett. 2005 Apr 1;15(7):1915-7. doi: 10.1016/j.bmcl.2005.01.083.

Authors

Sheng-Li Cao¹, Yu-Ping Feng, Yu-Yang Jiang, Shi-Ying Liu, Guo-Yu Ding, Run-Tao Li

Affiliation

¹ Department of Chemistry, Capital Normal University, Beijing 100037, China. caoshengli@tsinghua.org.cn

PMID: 15780632
DOI: 10.1016/j.bmcl.2005.01.083

Abstract

A series of 4(3H)-quinazolinone derivatives with dithiocarbamate side chains were synthesized and tested for their in vitro antitumor activity against human myelogenous leukemia K562 cells. Among them, (3,4-dihydro-2-methyl-4-oxoquinazolin-6-yl)methyl 4-(4-fluorophenyl)piperazine-1-carbodithioate 8q exhibited significant inhibitory activity against K562 cells with IC(50) value of 0.5 microM.

Publication types

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

MeSH terms

Animals
Antineoplastic Agents / chemical synthesis*
Antineoplastic Agents / pharmacology
Humans
Inhibitory Concentration 50
K562 Cells
Quinazolines / chemical synthesis*
Quinazolines / pharmacology
Quinazolinones
Structure-Activity Relationship
Thiocarbamates / chemical synthesis*
Thiocarbamates / pharmacology
Tumor Cells, Cultured

Substances

Antineoplastic Agents
Quinazolines
Quinazolinones
Thiocarbamates
4-hydroxyquinazoline