[Synthesis and in vitro antitumor activity of 4(3H)-quinazolinone derivatives bearing dithiocarbamate chains].
A series of 4(3H)-quinazolinone derivatives bearing dithiocarbamate side chains have been synthesized through the reaction of 6-bromomethyl-2-methyl-4(3H)-quinazolinone with CS2 and various amines in the presence of anhydrous K3PO4, and their structures were confirmed with ESI-MS, H NMR, elemental analysis or HRMS. The target compounds 8a -8q were tested for their in vitro antitumor activity against human myelogenous leukaemia K562 and human Hela cell lines by means of colorimetric MTT assay. Among the tested compounds, 8q exhibited in vitro inhibitory activity against K562 and Hela cells with IC50 values of 0.5 and 12.0 micromol x L(-01), respectively. Therefore, compound 8q is worthy to be a lead compound for the design and synthesis of new antitumor agents.
Cao
Sheng-li
SL
Department of Chemistry, Capital Normal University, Beijing 100037, China. sl_cao@sohu.com
Jiang
Yu-yang
YY
Feng
Yu-ping
YP
Liu
Shi-ying
SY
Gao
Hong-he
HH
Zhang
Mei
M
Wan
Rong
R
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D005028:Ethylenebis(dithiocarbamates) / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006367:HeLa Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D020014:K562 Cells; D015394:Molecular Structure; D052999:Quinazolinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D005028:Ethylenebis(dithiocarbamates); D052999:Quinazolinones; C061339:4-hydroxyquinazoline