1. Synthesis and biological evaluation of new coumarins bearing 2,4-diaminothiazole-5-carbonyl moiety.
- Author
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Ayati, Adileh, Oghabi Bakhshaiesh, Tayebeh, Moghimi, Setareh, Esmaeili, Rezvan, Majidzadeh-A, Keivan, Safavi, Maliheh, Firoozpour, Loghman, Emami, Saeed, and Foroumadi, Alireza
- Subjects
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COUMARINS , *CHALCONE , *ANTIOXIDANTS , *CELL death , *FLOW cytometry , *CELL cycle - Abstract
A series of new coumarin-containing compounds 3a-l and 4a-c was designed and synthesized based on the chalcone-type 4-amino-5-cinnamoylthiazole scaffold 2 , and screened for their in vitro anticancer and antioxidant activities. Representatively, the 2-thiomorpholinothiazole derivative 3k with IC 50 values of 7.5–16.9 μg/ml demonstrated good cytotoxic effects against tested cell lines MCF-7, HepG2 and SW480. Further investigation by flow cytometric analysis confirmed that this compound induces apoptotic cell death in MCF-7 cells and cause G1-phase arrest in the cell cycle. Moreover, most of compounds had intrinsic potential for radical scavenging activity and ferric-reducing power as investigated by DPPH and FRAP assays. [ABSTRACT FROM AUTHOR]
- Published
- 2018
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