3033-95-2Relevant academic research and scientific papers
Polymorphism and conformerism in chalcones
Ramos, Rafael Rodrigues,Da Silva, Cameron Capeletti,Guimar?es, Freddy Fernandes,Martins, Felipe Terra
, p. 2144 - 2154 (2016)
Herein two solid state phenomena have been observed in two chalcones. Firstly, polymorphism has been found in (E)-1-(2-aminophenyl)-3-(3,4,5-trimethoxyphenyl)prop-2-en-1-one (1). This compound crystallizes with only one conformer rather than three in the
Anti-cholinesterase activity of chalcone derivatives: Synthesis, in vitro assay and molecular docking study
Riswanto, Florentinus D. O.,Rawa, Mira S. A.,Murugaiyah, Vikneswaran,Salin, Nurul H.,Istyastono, Enade P.,Hariono, Maywan,Wahab, Habibah A.
, p. 442 - 452 (2021/03/26)
Background: Chalcones, originated from natural product, have been broadly studied their biological activity against various proteins which at the molecular level, are responsible for the progress of the diseases in cancer (e.g. kinases), inflammation (oxi
Design, synthesis and evaluation of chalcones as H1N1 Neuraminidase inhibitors
Chintakrindi, Anand S.,Gohil, Devanshi J.,Kothari, Sweta T.,Chowdhary, Abhay S.,Kanyalkar, Meena A.
, p. 1013 - 1025 (2018/02/28)
A series of chalcone derivatives (1a–2i) were designed based on isoliquiritigenin (the most active natural chalcone non-competitive neuraminidase (NA) inhibitor). Molecular modeling studies revealed that isoliquiritigenin and its designed analogs occupied
Solid-phase synthesis and biological evaluation of a parallel library of 2,3-dihydro-1,5-benzothiazepines
Ansari, Farzana Latif,Iftikhar, Fatima,Ihsan-ul-Haq,Mirza, Bushra,Baseer, Mohammad,Rashid, Umer
, p. 7691 - 7697 (2008/12/23)
Solid-phase synthesis of a parallel library of 3′-hydroxy-2,3-dihydrobenzothiazepines has been carried out through [4+3] annulation of α,β-unsaturated ketones with aminothiophenol, using Wang resin as solid support. The synthesized compounds were evaluated for their potential as antibacterial, tumor inhibitors as well as acetyl- and butyrylcholinesterase inhibitors. None of the compounds showed any significant antibacterial activity. However, quite a few compounds showed significant potential as crown gall tumor inhibitors. These results reflect a strong exploratory potential in search of new benzothiazepines as source of anticancer agents. The results of the inhibition of cholinesterase revealed that benzothiazepines have a greater potential as butyrylcholinesterase inhibitors as compared to acetylcholinesterase. Moreover, the substitution of hydroxy group at C-3 in ring A led to increased activity when compared to unsubstituted- and 2′-OH substituted benzothiazepines.
