127034-11-1Relevant articles and documents
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
Cytotoxic 3,4,5-trimethoxychalcones as mitotic arresters and cell migration inhibitors
Salum, Lívia B.,Altei, Wanessa F.,Chiaradia, Louise D.,Cordeiro, Marlon N.S.,Canevarolo, Rafael R.,Melo, Carolina P.S.,Winter, Evelyn,Mattei, Bruno,Daghestani, Hikmat N.,Santos-Silva, Maria Cláudia,Creczynski-Pasa, Tania B.,Yunes, Rosendo A.,Yunes, José A.,Andricopulo, Adriano D.,Day, Billy W.,Nunes, Ricardo J.,Vogt, Andreas
supporting information, p. 501 - 510 (2013/07/25)
Based on classical colchicine site ligands and a computational model of the colchicine binding site on beta tubulin, two classes of chalcone derivatives were designed, synthesized and evaluated for inhibition of tubulin assembly and toxicity in human canc
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.