1103585-01-8Relevant academic research and scientific papers
Synthesis and biological activity of new chalcone scaffolds as prospective antimicrobial agents
Narwal, Sangeeta,Kumar, Sanjiv,Verma, Prabhakar Kumar
, p. 1625 - 1641 (2021)
Chalcones are open-chain flavonoids which contains two aromatic rings are joined by 3-carbons α-, β-unsaturated carbonyl chain. The, β-unsaturated ketonic group which is liable for the antimicrobial activity of the chalcone is additionally of vast use in
A novel series of benzothiazepine derivatives as tubulin polymerization inhibitors with anti-tumor potency
Wang, Bin,Wang, Li-Ren,Liu, Lu-Lu,Wang, Wei,Man, Ruo-Jun,Zheng, Da-Jun,Deng, Yu-Shan,Yang, Yu-Shun,Xu, Chen,Zhu, Hai-Liang
, (2021/02/02)
In this work, a series of diaryl benzo[b][1,4]thiazepine derivatives D1-D36 were synthesized and screened as tubulin polymerization inhibitors with anti-tumor potency. They were designed by introducing the seven-member ring benzothiazepine as the linker f
Chalcones bearing a 3,4,5-trimethoxyphenyl motif are capable of selectively inhibiting oncogenic K-Ras signaling
Cho, Kwang-jin,Fourman, Cody,Ketcha, Daniel M.,Kinstedt, Christine,Kovar, Sarah E.,Morris, Christopher,Williams, Brandon
supporting information, (2020/04/15)
Ras proteins are small GTPases which regulate cellular proliferation, differentiation, and apoptosis. Constitutively active mutant Ras are expressed in ~15–20% human cancers, and K-Ras mutations account for ~85% of all Ras mutations. Despite the significa
Hybrid α-bromoacryloylamido chalcones. Design, synthesis and biological evaluation
Romagnoli, Romeo,Baraldi, Pier Giovanni,Carrion, Maria Dora,Cruz-Lopez, Olga,Cara, Carlota Lopez,Balzarini, Jan,Hamel, Ernest,Canella, Alessandro,Fabbri, Enrica,Gambari, Roberto,Basso, Giuseppe,Viola, Giampietro
supporting information; experimental part, p. 2022 - 2028 (2009/11/30)
Research into the anti-tumor properties of chalcones has received significant attention over the last few years Two novel large series of α-bromoacryloylamido chalcones 1a-m and 2a-k containing a pair of Michael acceptors in their structures, corresponding to the α-bromoacryloyl moiety and the α,β-unsaturated ketone system of the chalcone framework, were synthesized and evaluated for antiproliferative activity against five cancer cell lines. Such hybrid derivatives demonstrated significantly increased anti-tumor activity compared with the corresponding amino chalcones. The most promising lead molecules were 1k, 1m and 2j, which had the highest activity toward the five cell lines. Flow cytometry with K562 cells showed that the most active compounds resulted in a large proportion of the cells entering in the apoptotic sub-G0-G1 peak. Moreover, compound 1k induced apoptosis through the mitochondrial pathway and activated caspase-3.
