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Preclinical Assessment of the Bioactivity of the Anticancer Coumarin OT48 by Spheroids, Colony Formation Assays, and Zebrafish Xenografts
Published on: June 26, 2018
Synthesis of a new class of furo[3,2-c]coumarins and its anticancer activity
Mehdi Rajabi1, Zinatossadat Hossaini2, Mohammad A Khalilzadeh2
1The Pharmaceutical Research Institute, Albany College of Pharmacy and Health Sciences, Rensselaer, NY, USA.
Abstract:
A series of furo[3,2-c]coumarin derivatives 1a-d were synthesized and evaluated for their antiproliferative activity against MCF-7 breast and HCT-15 colon cancer cell lines using Sulfo-rhodamine B (SRB) assay. Compounds 1b and 1d showed higher antiproliferative activity than 1a and 1c. UV-Vis spectroscopy was used for DNA and BSA-binding affinity of the compounds 1b and 1d and gave overall affinity constants of K1b-DNA=8.1×10(3) M(-1), K1d-DNA=1.1×10(4) M(-1), K1b-BSA=5.1×10(4) M(-1), and K1d-BSA=7.6×10(4) M(-1). Our findings could provide new evidence showing the relationship between the chemical structure and anticancer activity of these new coumarin analogs.
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