770711-44-9Relevant academic research and scientific papers
Synthesis and antiproliferative activity of 6,7-disubstituted-4-phenoxyquinoline derivatives bearing the 2-oxo-4-chloro-1,2-dihydroquinoline-3-carboxamide moiety
Tang, Qidong,Zhai, Xin,Tu, Yayi,Wang, Ping,Wang, Linxiao,Wu, Chunjiang,Wang, Wenhui,Xie, Hongbo,Gong, Ping,Zheng, Pengwu
, p. 1794 - 1798 (2016/12/22)
A series of 6,7-disubstituted-4-phenoxyquinoline derivatives bearing the 2-oxo-4-chloro-1,2-dihydroquinoline-3-carboxamide moiety were synthesized, and evaluated for their antiproliferative activity against 5 cancer cell lines (H460, HT-29, MKN-45, A549, and U87MG). Most compounds showed moderate to excellent potency, and compared to foretinib, the most promising analog 42 (c-Met/Flt-3 IC50= 1.21/2.15 nM) showed a 6.1-fold increase in activity against H460 cell line in vitro. The enzymatic assays (c-Met, VEGFR-2, Flt-3, PDGFR-β, c-Kit, and EGFR) of compound 42 were evaluated in vitro. Docking analysis showed that compound 42 could form three hydrogen bonds with c-Met. Structure–activity relationship studies indicated that a more water-soluble cyclic tertiary amine and electron-withdrawing groups at 4-position of the phenyl ring contribute to the antitumour activity.
Design and synthesis of novel quinolinone-3-aminoamides and their α-lipoic acid adducts as antioxidant and anti-inflammatory agents
Detsi, Anastasia,Bouloumbasi, Dionysia,Prousis, Kyriakos C.,Koufaki, Maria,Athanasellis, Giorgos,Melagraki, Georgia,Afantitis, Antreas,Igglessi-Markopoulou, Olga,Kontogiorgis, Christos,Hadjipavlou-Litina, Dimitra J.
, p. 2450 - 2458 (2008/02/02)
A series of N-substituted-quinolinone-3-aminoamides and their hybrids containing the α-lipoic acid functionality were designed and synthesized as potential bifunctional agents combining antioxidant and anti-inflammatory activity. The new compounds were ev
A novel short-step synthesis of functionalized 4-hydroxy-2-quinolones using a 1-hydroxybenzotriazole methodology
Zikou, Lamprini,Athanasellis, Giorgos,Detsi, Anastasia,Zografos, Alexandros,Mitsos, Christos,Igglessi-Markopoulou, Olga
, p. 1505 - 1508 (2007/10/03)
A novel method for the synthesis of 3-substituted 4-hydroxy-1-methyl- and 1-phenyl-2-quinolones is presented. The compounds are produced in a one-step reaction in very good yields (51-76%). The major advantage of the methodology is the short time for the
