1264066-68-3Relevant academic research and scientific papers
Synthesis and anti-proliferative activity of fluoro-substituted chalcones
Burmaoglu, Serdar,Algul, Oztekin,Anil, Derya Aktas,Gobek, Arzu,Duran, Gulay Gulbol,Ersan, Ronak Haj,Duran, Nizami
, p. 3172 - 3176 (2016)
A series of novel fluoro-substituted chalcone derivatives have been synthesized. All synthesized compounds were characterized by 1H nuclear magnetic resonance (NMR), 13C NMR, and elemental analysis. Their anti-proliferative activities were evaluated against five cancer cells lines, namely, A549, A498, HeLa, A375, and HepG2 using the MTT method. Most of the compounds showed moderate to high activity with IC50 values in the range of 0.029-0.729 μM. Of all the synthesized compounds, 10 and 19 exhibited the most potent anti-proliferative activities against cancer cells, and 10 was identified as the most promising compound.
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.
Design of potent fluoro-substituted chalcones as antimicrobial agents
Burmaoglu, Serdar,Algul, Oztekin,Gobek, Arzu,Aktas Anil, Derya,Ulger, Mahmut,Erturk, Busra Gul,Kaplan, Engin,Dogen, Aylin,Aslan, G?nül
, p. 490 - 495 (2017/11/10)
Owing to ever-increasing bacterial and fungal drug resistance, we attempted to develop novel antitubercular and antimicrobial agents. For this purpose, we developed some new fluorine-substituted chalcone analogs (3, 4, 9–15, and 20–23) using a structure–a
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.
