A novel series of 5H-pyridazino[4,5-b]indoles were designed and synthesized in order to find novel potent anticancer compounds. The structures were confirmed by ^1H NMR and MS. Their antiproliferative activities again...A novel series of 5H-pyridazino[4,5-b]indoles were designed and synthesized in order to find novel potent anticancer compounds. The structures were confirmed by ^1H NMR and MS. Their antiproliferative activities against two cancer cell lines were tested by the MTT method in vitro. Three of compounds （1e, 1g, and 1h） exhibited potent antiproliferative activities, especially compound lh （with IC50 values of 5.2 μmol/L and 1.9 μmol/L against Bel-7402 and HT-1080, respectively）. The preliminary structure-activity relationships of 5H-pyridazino[4,5-b]indole derivatives were discussed.展开更多
Twelve novel pyrazolo [4,3-d] pyrimidin-7-ones were synthesized and their structures were confirmed by IR, 1H NMR and MS. Their in vitro bronchodilatory activities were tested in guinea-pigs. The pharmacological res...Twelve novel pyrazolo [4,3-d] pyrimidin-7-ones were synthesized and their structures were confirmed by IR, 1H NMR and MS. Their in vitro bronchodilatory activities were tested in guinea-pigs. The pharmacological results show that compound 11c has more potent activity than aminophylline.展开更多
A series of pyrazolo[3,4-d]pyrimidin-4-one derivatives were synthesized and tested for vasodilatory activities. All of them were new compounds and their structures were confirmed by IR, 1H NMR, MS and elemental analy...A series of pyrazolo[3,4-d]pyrimidin-4-one derivatives were synthesized and tested for vasodilatory activities. All of them were new compounds and their structures were confirmed by IR, 1H NMR, MS and elemental analysis.展开更多
A new series of diaryl urea derivatives bearing N-acylhydrazone moiety were designed and synthesized. All the target compounds were evaluated for their antiproliferative activities against human leukemia cell line （H...A new series of diaryl urea derivatives bearing N-acylhydrazone moiety were designed and synthesized. All the target compounds were evaluated for their antiproliferative activities against human leukemia cell line （HL-60）, human lung adenocarcinoma epithelial cell line （A549） and human breast cancer cell line （MDA-MB-231） in vitro by standard MTT assay. The pharmacological results indicated that some compounds exhibited promising antitumor activities. Compound 1j showed the most potent antiproliferative activity against the tested three cell lines with IC50 values of 0.13 μmol/L, 0.7 μmol/L and 0.5μmol/L, respectively.展开更多
文摘A novel series of 5H-pyridazino[4,5-b]indoles were designed and synthesized in order to find novel potent anticancer compounds. The structures were confirmed by ^1H NMR and MS. Their antiproliferative activities against two cancer cell lines were tested by the MTT method in vitro. Three of compounds （1e, 1g, and 1h） exhibited potent antiproliferative activities, especially compound lh （with IC50 values of 5.2 μmol/L and 1.9 μmol/L against Bel-7402 and HT-1080, respectively）. The preliminary structure-activity relationships of 5H-pyridazino[4,5-b]indole derivatives were discussed.
文摘Twelve novel pyrazolo [4,3-d] pyrimidin-7-ones were synthesized and their structures were confirmed by IR, 1H NMR and MS. Their in vitro bronchodilatory activities were tested in guinea-pigs. The pharmacological results show that compound 11c has more potent activity than aminophylline.
文摘A series of pyrazolo[3,4-d]pyrimidin-4-one derivatives were synthesized and tested for vasodilatory activities. All of them were new compounds and their structures were confirmed by IR, 1H NMR, MS and elemental analysis.
基金supported by the National High Technology Research and Development Program (‘‘863’’ Program)of China (No. 2012AA020305)National Natural Science Foundation of China (No. 21002065)Shenyang Scienceand Technology Plan Projects (No. F11-151-9-00)
文摘A new series of diaryl urea derivatives bearing N-acylhydrazone moiety were designed and synthesized. All the target compounds were evaluated for their antiproliferative activities against human leukemia cell line （HL-60）, human lung adenocarcinoma epithelial cell line （A549） and human breast cancer cell line （MDA-MB-231） in vitro by standard MTT assay. The pharmacological results indicated that some compounds exhibited promising antitumor activities. Compound 1j showed the most potent antiproliferative activity against the tested three cell lines with IC50 values of 0.13 μmol/L, 0.7 μmol/L and 0.5μmol/L, respectively.
