36574-87-5Relevant academic research and scientific papers
Novel Butein Derivatives Repress DDX3 Expression by Inhibiting PI3K/AKT Signaling Pathway in MCF-7 and MDA-MB-231 Cell Lines
Kim, Gon Sup,Kim, Ju Hyun,Kim, Myeong Ok,Kim, Seong Min,Lee, Gihwan,Lee, Keun Woo,Rampogu, Shailima,Shaik, Baji
, (2021/09/08)
Background: Breast cancer is one of the major causes of mortalities noticed in women globally. DDX3 has emerged as a potent target for several cancers, including breast cancer to which currently there are no reported or approved drugs. Methods: To find ef
On the role of synthesized hydroxylated chalcones as dual functional amyloid-β aggregation and ferroptosis inhibitors for potential treatment of Alzheimer's disease
Cong, Lin,Dong, Xiyu,Wang, Yan,Deng, Yulin,Li, Bo,Dai, Rongji
, p. 11 - 21 (2019/01/26)
In addition to amyloid cascade hypothesis, ferroptosis – a recently identified cell death pathway associated with the accumulation of lipid hydroperoxides – was hypothesized as one of the main forms of cell death in Alzheimer's disease. Herein, a series o
Design, synthesis, and in vitro hMAO-B inhibitory evaluation of some 1-methyl-3,5-diphenyl-4,5-dihydro-1H-pyrazoles
Fioravanti, Rossella,Desideri, Nicoletta,Biava, Mariangela,Proietti Monaco, Luca,Grammatica, Laura,Yá?ez, Matilde
, p. 5128 - 5130 (2013/09/12)
A series of 1-methyl-3,5-diphenyl-4,5-dihydro-1H-pyrazoles (3a-k and 4a-u) were designed, synthesized, and evaluated for their inhibitory efficacy towards the two hMAO isoforms. Most of the derivatives were found to be potent and selective hMAO-B inhibitors. In particular, derivative 3g showed greater hMAO-B affinity than selective inhibitor selegiline coupled with high selectivity index (SI = 145). The most selective hMAO-B inhibitor was the 3-methyl analogue 3f with an SI higher than 909.
Synthesis of some pyrazole derivatives and preliminary investigation of their affinity binding to P-glycoprotein
Manna, Fedele,Chimenti, Franco,Fioravanti, Rossella,Bolasco, Adriana,Secci, Daniela,Chimenti, Paola,Ferlini, Cristiano,Scambia, Giovanni
, p. 4632 - 4635 (2007/10/03)
A series of substituted pyrazolines were synthesized and evaluated for their anticancer activity and for their ability to inhibit P-glycoprotein- mediated multidrug resistance by direct binding to a purified protein domain containing an ATP-binding site and a modulator interacting region. Compounds 2a and e have been found to bind to P-glycoprotein with greater affinity.
Inhibition of amine oxidases activity by 1-acetyl-3,5-diphenyl-4,5-dihydro-(1H)-pyrazole derivatives
Manna, Fedele,Chimenti, Franco,Bolasco, Adriana,Secci, Daniela,Bizzarri, Bruna,Befani, Olivia,Turini, Paola,Mondov, Bruno,Alcaro, Stefano,Tafi, Andrea
, p. 3629 - 3633 (2007/10/03)
A novel series of 1-acetyl-3,5-diphenyl-4,5-dihydro-(1H)-pyrazole derivatives have been synthesised and investigated for the ability to inhibit selectively monoamine oxidases, swine kidney oxidase, and bovine serum amine oxidase. The newly synthesised compounds 1-6 proved to be reversible and non-competitive inhibitors of all types of the assayed amine oxidases. Compounds inhibit monoamine oxidases potently, displaying low I50 values of particular interest. In particular 1-acetyl-3-(2,4-dihydroxyphenyl)-5-(3-methylphenyl)-4,5-dihydro-(1H)-pyrazole 6 showed to be a potent monoamine oxidase inhibitor with a Ki of about 10-8 M. Further insights in the theoretical evaluation of the possible interactions between the compounds and monoamine oxidase B have been developed through a computational approach.
