Literature DB >> 20538385

Synthesis and cytotoxic activity of N-((2-methyl-4(3H)-quinazolinon-6-yl)methyl)dithiocarbamates.

Sheng-Li Cao1, Yao Wang, Lin Zhu, Ji Liao, Yan-Wen Guo, Lin-Lin Chen, Hong-Qin Liu, Xingzhi Xu.   

Abstract

A series of N-((2-methyl-4(3H)-quinazolinon-6-yl)methyl)dithiocarbamates 5a-w were synthesized and evaluated for their cytotoxic activity against five human cancer cell lines. We found that compound 5k inhibited proliferation of A549, MCF-7, HeLa, HT29 and HCT-116 cells with IC(50) values of 5.44, 7.15, 12.16, 10.35 and 11.44 microM, respectively. Compound 5i was the most potent with an IC(50) value of 3.65 microM against proliferation of MCF-7 cells, while 5n was the most potent with an IC(50) value of 5.09 microM against proliferation of A549 cells. Cell cycle analysis showed that both 5i and 5k arrested A549 cells at S and G2/M phases, suggesting that these compounds act through mechanisms different from 5-fluorouracil, which arrests cells at S phase only. 2010 Elsevier Masson SAS. All rights reserved.

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Year:  2010        PMID: 20538385     DOI: 10.1016/j.ejmech.2010.05.038

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  3 in total

1.  Antitumor evaluation of novel phenothiazine derivatives that inhibit migration and tubulin polymerization against gastric cancer MGC-803 cells.

Authors:  Nan Liu; Zhe Jin; Jing Zhang; Jianjun Jin
Journal:  Invest New Drugs       Date:  2018-10-22       Impact factor: 3.850

2.  1-{[(2,3-Dihydro-1H-inden-2-yl)-oxy]meth-yl}quinazoline-2,4(1H,3H)-dione.

Authors:  Nasser R El-Brollosy; Necmi Dege; Güneş Demirtaş; Mohamed I Attia; Ali A El-Emam; Orhan Büyükgüngör
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2012-05-23

3.  Design, synthesis, and evaluation of novel coumarin-dithiocarbamate derivatives (IDs) as anti-colorectal cancer agents.

Authors:  Heping Zhu; Shilong Ying; Bingluo Zhou; Xinyang Hu; Xiao Liang; Wangyu Li; Dungai Wang; Hongchuan Jin; Yuanjiang Pan
Journal:  J Enzyme Inhib Med Chem       Date:  2021-12       Impact factor: 5.051

  3 in total

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