Abstract
2H-chromenes and chalcones are biologically important scaffolds with applications in drug discovery. Their ease of synthesis and biological importance have attracted the attention of medicinal chemists worldwide. Inspired by this, we synthesized various substituted chalcones and dihydropyrazole derivatives bearing various aryl and hetero-aryl 2H-chromene moieties. The resulting compounds were evaluated for cytotoxicity in vitro against doxorubicin in triple-negative breast cancer cell lines (MDA-MB-231), estrogen receptor-positive breast cancer cell lines (MCF-7), and human brain glioblastoma (U-87 MG) cell lines. Compounds 6b and 6j exhibited anticancer activity against triple-negative breast cancer cell line (MDA-MB-231), with IC50 values of 4.02 µM and 3.35 µM, respectively. Further investigation involving in silico pharmacokinetic (ADME) and toxicity studies also revealed pivotal features for the favourable bioavailability of these derivatives.
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have