1264066-70-7Relevant academic research and scientific papers
Design, synthesis and antiproliferative activity evaluation of fluorine-containing chalcone derivatives
Aktas Anil, Derya,Algul, Oztekin,Burmaoglu, Serdar,Duran, Nizami,Gobek, Arzu,Kilic, Deryanur,Yetkin, Derya
, (2020/11/20)
A series of new chalcones containing fluoro atom at B ring have been designed, synthesized, and evaluated to be antiproliferative activity against a panel of human tumor cell lines. Some of the analogs (8, 9, 12, 45, 46 and 48) displayed powerful antiproliferative effects to certain human tumor cells, but all of them were devoid of any cytotoxicity towards the normal HEK 293. Acridine orange staining data supported that the cytotoxic and antiproliferative effects of the synthesized analogs on tumor cells are mediated through apoptosis. The compounds 12 and 46 manifested concentration-dependent antiproliferative activity in human hepatocellular carcinoma cell lines using an xCELLigence assay. The structures and antiproliferative activity relationship were further supported by in silico molecular docking study of the compounds against tubulin protein which suggests our compounds interference to cell division. Communicated by Ramaswamy H. Sarma.
Synthesis of non-natural flavanones and dihydrochalcones in metabolically engineered yeast
Werner, Sean R.,Chen, Hao,Jiang, Hanxiao,Morgan, John A.
body text, p. 257 - 263 (2010/11/18)
Flavonoids are plant phenolic compounds that have many interesting medicinal properties. Therefore, there is interestin the synthesisof non-natural flavonoidsas they may possess neworenhanced biological activities. In this study, metabolically engineered Saccharomyces cerevisiae expressing 4-coumaroyl:CoA-ligase (4CL) and chalcone synthase (CHS)was explored as a platform for producingnon-natural flavanones and dihydrochalcones. By precursor addition of cinnamic acid analogues to the engineered yeast, numerous non-natural flavanones and dihydrochalcones were formed in vivo. Also, several CHS derailment products were formed. Of the isolated compounds, one flavanone and three derailment products were found to be novel compounds.
