86711-45-7Relevant academic research and scientific papers
Chalcones and bis-chalcones: As potential α-amylase inhibitors; synthesis, in vitro screening, and molecular modelling studies
Tajudeen Bale, Adebayo,Mohammed Khan, Khalid,Salar, Uzma,Chigurupati, Sridevi,Fasina, Tolulope,Ali, Farman,Kanwal,Wadood, Abdul,Taha, Muhammad,Sekhar Nanda, Sitanshu,Ghufran, Mehreen,Perveen, Shahnaz
, p. 179 - 189 (2018)
Despite of a diverse range of biological activities associated with chalcones and bis-chalcones, they are still neglected by the medicinal chemist for their possible α-amylase inhibitory activity. So, the current study is based on the evaluation of this c
Chalcones and bis-chalcones analogs as DPPH and ABTS radical scavengers
Bale, Adebayo Tajudeen,Salar, Uzma,Khan, Khalid Mohammed,Chigurupati, Sridevi,Fasina, Tolulope,Ali, Farman,Ali, Muhammad,Sekhar Nanda, Sitansu,Taha, Muhammad,Perveen, Shahnaz
, p. 249 - 257 (2021/04/21)
Background: A number of synthetic scaffolds, along with natural products, have been identified as potent antioxidants. The present study deals with the evaluation of varyingly substituted, medicinally distinct class of compounds “chalcones and bis-chalcon
Antiproliferative effects of chalcones on T cell acute lymphoblastic leukemia-derived cells: Role of PKCβ
Corsini, Emanuela,Facchetti, Giorgio,Esposito, Sara,Maddalon, Ambra,Rimoldi, Isabella,Christodoulou, Michael S.
, (2020/05/16)
In this study, a series of 20 chalcone derivatives was synthesized, and their antiproliferative activity was tested against the human T cell acute lymphoblastic leukemia-derived cell line, CCRF-CEM. On the basis of the structural features of the most active compounds, a new library of chalcone derivatives, according to the structure–activity relationship design, was synthesized, and their antiproliferative activity was tested against the same cancer cell line. Furthermore, four of these derivatives (compounds 3, 4, 8, 28), based on lower IC50 values (between 6.1 and 8.9 μM), were selected for further investigation regarding the modulation of the protein expression of RACK1 (receptor for activated C kinase), protein kinase C (PKC)α and PKCβ, and their action on the cell cycle level. The cell cycle analysis indicated a block in the G0/G1 phase for all four compounds, with a statistically significant decrease in the percentage of cells in the S phase, with no indication of apoptosis (sub-G0/G1 phase). Compounds 4 and 8 showed a statistically significant reduction in the expression of PKCα and an increase in PKCβ, which together with the demonstration of an antiproliferative role of PKCβ, as assessed by treating cells with a selective PKCβ activator, indicated that the observed antiproliferative effect is likely to be mediated through PKCβ induction.
Synthesis and biological evaluation of aromatic enones related to curcumin
Robinson, Thomas Philip,Hubbard IV, Richard B.,Ehlers, Tedman J.,Arbiser, Jack L.,Goldsmith, David J.,Bowen, J. Phillip
, p. 4007 - 4013 (2007/10/03)
Curcumin, a natural product isolated from the spice turmeric, has been shown to exhibit a wide range of pharmacological activities including certain anti-cancer properties. It has been specifically shown to be an effective inhibitor of angiogenesis both in vitro and in vivo. Using curcumin as a lead compound for anti-angiogenic analog design, a series of structurally related compounds utilizing a substituted chalcone backbone have been synthesized and tested via an established SVR cell proliferation assay. The results have yielded a wide range of compounds that equal or exceed curcumin's ability to inhibit endothelial cell growth in vitro. Due to both their commercial availability and their fairly straightforward synthetic preparation, these low molecular weight compounds are attractive leads for developing future angiogenic inhibitors.
