Novel Coumarin-furo[2,3-d]pyrimidinone hybrid derivatives as anticancer agents: Synthesis, biological evaluation and molecular docking

Latest developments in coumarin-based anticancer agents: mechanism of action and structure–activity relationship studies

“…A novel library of coumarin-furo[2,3- d ]pyrimidinone hybrid derivatives was synthesized and assessed for their antiproliferative activities against the HepG2 and HeLa cell lines in vitro . 135 Compound 76a ( Fig. 73 ) showed maximum potency against HepG2 with an IC 50 value of 4.87 μmol L −1 .…”

Coumarin–furo[2,3-d]pyrimidone hybrid molecules targeting human liver cancer cells: synthesis, anticancer effect, EGFR inhibition and molecular docking studies

“…The results of computational studies revealed that the substituents at the C-2 position of the furo [2,3-d]pyrimidinone could enhance the bioactivity and the butoxy present in the coumarin structure did not exert a significant impact on the activity. 42 In continuation of our studies to develop new cytotoxic candidates based on the naturally derived coumarin scaffold and fused heterocyclic scaffold, we intended to use the same substitution pattern on the furopyrimidone nucleus (C-2, N-3) as done in our previously published work. In the presented study, we reported the design and synthesis of new hybrid derivatives carrying furo [2,3-d]pyrimidone derivatives conjugated with non-substituted coumarin via a hydrazide linker as potential EGFR inhibitors aiming to improve their synergistic anticancer activity.…”

“…The results of computational studies revealed that the substituents at the C-2 position of the furo[2,3- d ]pyrimidinone could enhance the bioactivity and the butoxy present in the coumarin structure did not exert a significant impact on the activity. 42…”