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Synthesis and biological evaluation of 4-amino-5-cinnamoylthiazoles as chalcone-like anticancer agents.
- Source :
-
European Journal of Medicinal Chemistry . Feb2018, Vol. 145, p404-412. 9p. - Publication Year :
- 2018
-
Abstract
- A series of 4-amino-5-cinnamoylthiazoles 3a-p were designed and synthesized as chalcone-like anticancer agents. The synthesized derivatives 3a-p were evaluated for their in vitro antiproliferative activities against three different human cancer cell lines including MCF-7, HepG2 and SW480. Most of compounds could significantly prevent proliferation of tested cell lines. In particular, the pyrrolidine derivative 3e namely ( E )-1-(4-amino-2-(pyrrolidin-1-yl)thiazol-5-yl)-3-(2,4-dichlorophenyl)prop-2-en-1-one showed promising activity, especially against HepG2 cells (IC 50 = 10.6 μg/ml). Flow cytometric analyses revealed that the prototype compound 3e can prevent the proliferation of HepG2 cells by blockade of the cell cycle at the G2 phase and induction of apoptosis. [ABSTRACT FROM AUTHOR]
- Subjects :
- *CHALCONES
*ANTINEOPLASTIC agents
*CANCER cells
*CELL proliferation
*APOPTOSIS
Subjects
Details
- Language :
- English
- ISSN :
- 02235234
- Volume :
- 145
- Database :
- Academic Search Index
- Journal :
- European Journal of Medicinal Chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 127672159
- Full Text :
- https://doi.org/10.1016/j.ejmech.2018.01.015