90811-67-9Relevant academic research and scientific papers
Synthesis and structure-activity relationships of chalcone derivatives as inhibitors of ovarian cancer cell growth
Tucker, Zachary D.,Barrios, Francis J.,Krzysiak, Amanda J.
, p. 1259 - 1266 (2017)
Background: Ovarian cancer remains a disease with a poor five year survival rate. As such, novel therapies are needed. Natural chalcones as well as their synthetic derivatives have shown biological activity in a number of areas including the inhibition of cancer cell growth. Objective: To synthesize a library of chalcone derivatives, including novel structures, and determiner the inhibition of ovarian cancer cell growth and Structure-activity-relationships. Methods: The Claisen-Schmidt condensation reaction between substituted acetophenones and aromatic aldehydes was used to produce a series of novel chalcones in moderate to excellent yields and good purity. Cellular proliferation of CA-OV3 cells was measured with a MTS assay. Results: Out of the thirty-four synthesized compounds, eight are new derivatives. The synthesized compounds were characterized by 1H NMR, 13C NMR, and HRMS. Biological evaluation of these β-phenylacrylophenone derivatives in CA-OV3 cells showed interesting antiproliferative activities providing initial structure – activity information. Conclusion: Fourteen of the thirty-four tested compounds showed significant activity, with several showing near complete inhibition of growth at 100 μM. The structure-activity relationships suggest that modification to the A ring is widely tolerated and that electron-donating modifications to the B ring are beneficial to activity. Electron-withdrawing modifications to the B ring did not show inhibition of cell growth.
Inhibitors of Yellow Fever Virus replication based on 1,3,5-triphenyl-4,5-dihydropyrazole scaffold: Design, synthesis and antiviral evaluation
Fioravanti, Rossella,Desideri, Nicoletta,Carta, Antonio,Atzori, Elena Maria,Delogu, Ilenia,Collu, Gabriella,Loddo, Roberta
, p. 15 - 25 (2017/10/16)
By the antiviral screening of an in house library of pyrazoline compounds, 4-(3-(4-phenoxyphenyl)-5-phenyl-4,5-dihydro-1H-pyrazol-1-yl)benzenesulfonamide (5a) was identified as a promising hit compound for the development of anti- Yellow Fever Virus (YFV)
ALLOSTERIC PROTEIN KINASE MODULATORS
-
Page/Page column 51, (2012/03/10)
The invention provides specific small molecule compounds that allosterically regulate the activity or modulate protein-protein interactions of AGC protein kinases and the Aurora family of protein kinases, methods for their production, pharmaceutical compositions comprising same, and their use for preparing medicaments for the treatment and prevention of diseases related to abnormal activities of AGC protein kinases or of protein kinases of the Aurora family.
Palladium-catalyzed oxidative carbonylative coupling reactions of arylboronic acids with styrenes to chalcones under mild aerobic conditions
Wu, Xiao-Feng,Neumann, Helfried,Beller, Matthias
experimental part, p. 282 - 285 (2012/04/18)
Do the coupling: A palladium-catalyzed oxidative carbonylative coupling process of arylboronic acid with styrenes to chalcone has been developed. The reactions proceed under mild conditions using air as the terminal oxidant reagent.
ALLOSTERIC PROTEIN KINASE MODULATORS
-
Page/Page column 106, (2010/04/30)
The invention provides specific small molecule compounds that allosterically regulate the activity or modulate protein-protein interactions of AGC protein kinases and the Aurora family of protein kinases, methods for their production, pharmaceutical compositions comprising same, and their use for preparing medicaments for the treatment and prevention of diseases related to abnormal activities of AGC protein kinases or of protein kinases of the Aurora family.
A new solvent-free synthesis of α,β-unsaturated ketones from acetals with aryl ketones under microwave irradiation
Huang, Danfeng,Wang, Jin-Xian,Hu, Yulai,Zhang, Yumei,Tang, Jing
, p. 971 - 979 (2007/10/03)
A new, rapid and efficient method for the synthesis of α,βunsaturated ketones under microwave irradiation conditions is described. The process involves the reaction of acetals with aryl ketones in the absence of solvent using Lewis acids as catalysts under microwave irradiation to afford the α,βunsaturated ketones in good to excellent isolated yields. The reaction mechanism is briefly discussed.
