Synthesis and antitumor activity evaluation in vitro of 4-aminoquinazoline derivatives containing 1,3,4-thiadiazole
نویسندگان
چکیده
In order to search for new antitumor drugs with high efficiency and low toxicity, a series of novel 4-aminoquinazoline derivatives containing 1,3,4-thiadiazole group were designed, synthesized evaluated antiproliferative activity against four human cancer cell lines (H1975, PC-3, MCF-7 HGC-27) using MTT assay in vitro. Among them, compound N-(5-((3,5-dichlorobenzyl)thio)-1,3,4-thiadiazol-2-yl)-2-((4-(phenylamino)quinazolin-2-yl)thio)acetamide (15o) showed good anti-tumor proliferation tested lines, IC50 values 1.96 ± 0.15 μM PC-3 cell. The was significantly better than that gefitinib. Further mechanism studies 15o inhibited the migration ability tumor cells concentration dependent time-dependent manner, blocked cycle S phase. At same time, cloning experiment further proved colony formation cells, inhibition rate as 92% at 2.0 μM.
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ژورنال
عنوان ژورنال: Medicinal Chemistry Research
سال: 2022
ISSN: ['1554-8120', '1054-2523']
DOI: https://doi.org/10.1007/s00044-022-02913-y