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Synthesis of Substituted Benzylamino‐ and Heterocyclylmethylamino Carbodithioate Derivatives of 4‐(3 H )‐Quinazolinone and their Cytotoxic Activity
Author(s) -
Cao ShengLi,
Feng YuPing,
Zheng XiaoLin,
Jiang YuYang,
Zhang Mei,
Wang Yue,
Xu Meng
Publication year - 2006
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.200500264
Subject(s) - quinazolinone , cytotoxicity , chemistry , cell culture , mtt assay , in vitro , cytotoxic t cell , stereochemistry , cancer cell lines , cancer cell , cancer , biochemistry , biology , medicine , genetics
A new series of substituted benzylamino‐ and heterocyclylmethylamino carbodithioate derivatives of 4‐(3 H )‐quinazolinone were synthesized via four steps starting from 2‐amino‐5‐methylbenzoic acid and initially screened against A‐549 (human non‐small cell lung cancer), HCT‐8 (human colon cancer), and Bel‐7402 (human liver cancer) cell lines at the single concentration of 5 μg/mL using the colorimetric MTT assay. The IC 50 values were determined for the compounds reaching ⪈70% inhibition in primary screening by serial dilution. Among the newly synthesized compounds, 9n exhibited potent in vitro cytotoxicity against A‐549, HCT‐8, and Bel‐7402 cell lines with the IC 50 values of 1.65, 0.93, and 1.43 μM, respectively.