Based on the structure-activity relationships and antiangiogenic mechanism of RGD-containing peptides, a series of 5-amino- 1,3-dihydro-1,3-dioxo-2H-isoindole derivatives were synthesized. The structures were characte...Based on the structure-activity relationships and antiangiogenic mechanism of RGD-containing peptides, a series of 5-amino- 1,3-dihydro-1,3-dioxo-2H-isoindole derivatives were synthesized. The structures were characterized by ^1H NMR, MS and elementary analysis. There ability to inhibit angiogenesis were evaluated by chick embryo chorioallantoic membrane assay at 10^-5 mol/L. Compounds 7a and 7b displayed obvious antiangiogenic activity.展开更多
A series of novel 4-phenoxyquinoline derivatives containing 3-amino-2-cyano-acrylamide framework was designed and synthesized, and the in vitro cytotoxic activities of them against five cancer cell lines（HT-29, H460,...A series of novel 4-phenoxyquinoline derivatives containing 3-amino-2-cyano-acrylamide framework was designed and synthesized, and the in vitro cytotoxic activities of them against five cancer cell lines（HT-29, H460, A549, MKN-45, and U87MG） were evaluated. Most of the compounds exhibited moderate-to-significant cytotoxicity and high selectivity against one or more cell lines as compared with Foretinib. The studies of their preliminary structure-activity relationships（SARs） indicate that the compounds containing methyl groups, especially methyl groups at 4-position of the phenyl ring（moiety B） are more effective. Among them, compound 36 shows the most potent anti- tumor activities with IC50 values of 0.04, 0.09, 0.67, 0.39 and l. 10 μmol/L against HT-29, H460, A549, MKN-45 and U87MG cell lines, respectively.展开更多
文摘Based on the structure-activity relationships and antiangiogenic mechanism of RGD-containing peptides, a series of 5-amino- 1,3-dihydro-1,3-dioxo-2H-isoindole derivatives were synthesized. The structures were characterized by ^1H NMR, MS and elementary analysis. There ability to inhibit angiogenesis were evaluated by chick embryo chorioallantoic membrane assay at 10^-5 mol/L. Compounds 7a and 7b displayed obvious antiangiogenic activity.
文摘A series of novel 4-phenoxyquinoline derivatives containing 3-amino-2-cyano-acrylamide framework was designed and synthesized, and the in vitro cytotoxic activities of them against five cancer cell lines（HT-29, H460, A549, MKN-45, and U87MG） were evaluated. Most of the compounds exhibited moderate-to-significant cytotoxicity and high selectivity against one or more cell lines as compared with Foretinib. The studies of their preliminary structure-activity relationships（SARs） indicate that the compounds containing methyl groups, especially methyl groups at 4-position of the phenyl ring（moiety B） are more effective. Among them, compound 36 shows the most potent anti- tumor activities with IC50 values of 0.04, 0.09, 0.67, 0.39 and l. 10 μmol/L against HT-29, H460, A549, MKN-45 and U87MG cell lines, respectively.
