Design, synthesis and biological evaluation of novel 2,4,6-trisubstituted quinazoline derivatives as potential antitumor agents
In this study, a series of novel 2,4,6-trisubstituted quinazoline derivatives were designed, synthesized and biologically evaluated their antiproliferative activity against four human cancer cell lines (Eca-109, A549, PC-3 and MGC-803). The most of designed compounds showed considerable antiprolifer...
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Published in | Medicinal chemistry research Vol. 32; no. 8; pp. 1832 - 1850 |
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Main Authors | , , , , , , , , , , , , |
Format | Journal Article |
Language | English |
Published |
New York
Springer US
01.08.2023
Springer Nature B.V |
Subjects | |
Online Access | Get full text |
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Summary: | In this study, a series of novel 2,4,6-trisubstituted quinazoline derivatives were designed, synthesized and biologically evaluated their antiproliferative activity against four human cancer cell lines (Eca-109, A549, PC-3 and MGC-803). The most of designed compounds showed considerable antiproliferative activity against the tested four cancer cell lines, while compound
28g
displayed the best antiproliferative activity with the IC
50
values of 1.95 μM and 2.46 μM against MGC-803 cells and Eca-109 cells, respectively. Further mechanism studies indicated that
28g
significantly inhibited the cell migration and colony formation of MGC-803 cells. Besides,
28g
also dose-dependently induced cellular apoptosis and cell cycle arrest at S phase in MGC-803 cells. Overall, all these studies suggested that
28g
has the potential to act as a valuable lead compound for the development of antitumor agents.
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ISSN: | 1054-2523 1554-8120 |
DOI: | 10.1007/s00044-023-03114-x |