89121-58-4Relevant academic research and scientific papers
Computational screening of chalcones acting against topoisomerase IIα and their cytotoxicity towards cancer cell lines
Sangpheak, Kanyani,Mueller, Monika,Darai, Nitchakan,Wolschann, Peter,Suwattanasophon, Chonticha,Ruga, Ritbey,Chavasiri, Warinthon,Seetaha, Supaporn,Choowongkomon, Kiattawee,Kungwan, Nawee,Rungnim, Chompoonut,Rungrotmongkol, Thanyada
, p. 134 - 143 (2019)
Targeted cancer therapy has become one of the high potential cancer treatments. Human topoisomerase II (hTopoII), which catalyzes the cleavage and rejoining of double-stranded DNA, is an important molecular target for the development of novel cancer thera
Investigation of chalcones as selective inhibitors of the breast cancer resistance protein: Critical role of methoxylation in both inhibition potency and cytotoxicity
Valdameri, Glaucio,Gauthier, Charlotte,Terreux, Rapha?l,Kachadourian, Rémy,Day, Brian J.,Winnischofer, Sheila M. B.,Rocha, Maria E. M.,Frachet, Véronique,Ronot, Xavier,Di Pietro, Attilio,Boumendjel, Ahcène
scheme or table, p. 3193 - 3200 (2012/06/01)
ABCG2 plays a major role in anticancer-drug efflux and related tumor multidrug resistance. Potent and selective ABCG2 inhibitors with low cytotoxicity were investigated among a series of 44 chalcones and analogues (1,3-diarylpropenones), by evaluating their inhibitory effect on the transport of mitoxantrone, a known ABCG2 substrate. Six compounds producing complete inhibition with IC50 values below 0.5 μM and high selectivity for ABCG2 were identified. The number and position of methoxy substituents appeared to be critical for both inhibition and cytotoxicity. The best compounds, with potent inhibition and low toxicity, contained an N-methyl-1-indolyl (compound 38) or a 6′-hydroxyl-2′,4′-dimethoxy-1-phenyl (compound 27) moiety (A-ring) and two methoxy groups at positions 2 and 6 of the 3-phenyl moiety (B-ring). Methoxy substitution contributed to inhibition at positions 3 and 5, but had a negative effect at position 4. Finally, methoxy groups at positions 3, 4, and 5 of the B-ring markedly increased cytotoxicity and, therefore, should be avoided.
Solution phase synthesis of a combinatorial library of chalcones and flavones as potent cathepsin v inhibitors
Alvim, Joel,Severino, Richele P.,Marques, Emerson F.,Martinelli, Ariane M.,Vieira, Paulo C.,Fernandes, Joao B.,Da Silva, M. Fatima Das G. F.,Correa, Arlene G.
experimental part, p. 687 - 695 (2010/11/18)
Cathepsin V is a papain-like cysteine protease. It is involved in the control of human T cells (responsible for cell immunity), and presents the largest elastolytic activity among the proteolytic enzymes. Therefore, cathepsin V is a potential molecular ta
