Based on the structure-activity relationships of RGD-containing peptides, a series of 1,3-dihydro-1,3-dioxo-2H-isoindole derivatives were synthesized. All of them were first reported. Their structures were confirmed b...Based on the structure-activity relationships of RGD-containing peptides, a series of 1,3-dihydro-1,3-dioxo-2H-isoindole derivatives were synthesized. All of them were first reported. Their structures were confirmed by spectral data and elemental analysis. Their ability to inhibit angiogenesis were evaluated in the chick embryo chorioallantoic membrane assay at 10-5 mol/L. Compounds 5b and 5e displayed obviously antiangiogenic activity.展开更多
4-(1-Pyrrolyl)butanenitrile(4), the key intermediate for the synthesis of 1,2,3,4-tetrahydro-1-indolizinone, was prepared with Clauson-Kass reation. When pyrrole reacted with 4-bromobutanenitrile in PEG-400 dimethyl e...4-(1-Pyrrolyl)butanenitrile(4), the key intermediate for the synthesis of 1,2,3,4-tetrahydro-1-indolizinone, was prepared with Clauson-Kass reation. When pyrrole reacted with 4-bromobutanenitrile in PEG-400 dimethyl ether catalyzed by NaOH, 3-(1-pyrrolyl)butanenitrile was obtained. The nitriles were converted into the corresponding ketones by Hoesch reaction. Some of the ketone derivatives were prepared.展开更多
A series of 2-（arylmethylidene）-2,3-dihydro-1-benzofuran-3-one derivatives（aurones, 1–20） were synthesized and screened for their inhibitory activity against h MAO. Seventeen compounds（1–5, 7–17,19） were foun...A series of 2-（arylmethylidene）-2,3-dihydro-1-benzofuran-3-one derivatives（aurones, 1–20） were synthesized and screened for their inhibitory activity against h MAO. Seventeen compounds（1–5, 7–17,19） were found to be selective towards h MAO-B, while two were non-selective（6 and 20） and one（18）selective towards h MAO-A. Compound 17（Ki = 0.10 0.01 mmol/L） was found to be equally potent and selective towards h MAO-B, when compared with the standard drug Selegiline（Ki = 0.12 0.01 mmol/L）.Nature and position of substitution in aryl ring at 2nd position of benzofuranone influences h MAO-B inhibitory potency, while their structural bulkiness influences selectivity between h MAO-A and h MAO-B.Molecular docking simulation was also carried out to understand the interaction of inhibitor with the enzyme at molecular level, and we found the docking results were in good agreement with the experimental values. Comparison of the activity profile of the aurones with their corresponding flavones reported earlier by our group revealed that there exists no difference in potency as well as selectivity.展开更多
Nine new compounds,including five natural rarely-occurring 2,3-dihydro-1H-indene derivatives named diaporindenes E−I(1−5),and four new benzophenone analogues named tenellones J−M(6−9)were isolated from the deep-sea se...Nine new compounds,including five natural rarely-occurring 2,3-dihydro-1H-indene derivatives named diaporindenes E−I(1−5),and four new benzophenone analogues named tenellones J−M(6−9)were isolated from the deep-sea sediment-derived fungus Phomopsis lithocarpus FS508.All the structures for these new compounds were fully characterized on the basis of spectroscopic data,NMR spectra,and ECD calculation and single-crystal X-ray diffraction analysis.The potential anti-tumor activities of compounds 1−9 against four tumor cell lines SF-268,MCF-7,HepG-2,and A549 were evaluated using the SRB method.Compound 7 exhibited cytotoxic activity against the SF-268 cell line with an IC50 value of 11.36μmol·L^(−1).展开更多
文摘Based on the structure-activity relationships of RGD-containing peptides, a series of 1,3-dihydro-1,3-dioxo-2H-isoindole derivatives were synthesized. All of them were first reported. Their structures were confirmed by spectral data and elemental analysis. Their ability to inhibit angiogenesis were evaluated in the chick embryo chorioallantoic membrane assay at 10-5 mol/L. Compounds 5b and 5e displayed obviously antiangiogenic activity.
文摘4-(1-Pyrrolyl)butanenitrile(4), the key intermediate for the synthesis of 1,2,3,4-tetrahydro-1-indolizinone, was prepared with Clauson-Kass reation. When pyrrole reacted with 4-bromobutanenitrile in PEG-400 dimethyl ether catalyzed by NaOH, 3-(1-pyrrolyl)butanenitrile was obtained. The nitriles were converted into the corresponding ketones by Hoesch reaction. Some of the ketone derivatives were prepared.
基金Birla Institute of Technology for providing financial support as a prestigious Institute fellowship
文摘A series of 2-（arylmethylidene）-2,3-dihydro-1-benzofuran-3-one derivatives（aurones, 1–20） were synthesized and screened for their inhibitory activity against h MAO. Seventeen compounds（1–5, 7–17,19） were found to be selective towards h MAO-B, while two were non-selective（6 and 20） and one（18）selective towards h MAO-A. Compound 17（Ki = 0.10 0.01 mmol/L） was found to be equally potent and selective towards h MAO-B, when compared with the standard drug Selegiline（Ki = 0.12 0.01 mmol/L）.Nature and position of substitution in aryl ring at 2nd position of benzofuranone influences h MAO-B inhibitory potency, while their structural bulkiness influences selectivity between h MAO-A and h MAO-B.Molecular docking simulation was also carried out to understand the interaction of inhibitor with the enzyme at molecular level, and we found the docking results were in good agreement with the experimental values. Comparison of the activity profile of the aurones with their corresponding flavones reported earlier by our group revealed that there exists no difference in potency as well as selectivity.
基金This work was supported by Guangdong Provincial Special Fund for Marine Economic Development Project(No.GDNRC[2020]042)the National Natural Science Foundation of China(No.41906106)+2 种基金Guangdong Special Support Program(No.2019TQ05Y375)the Team Project of the Natural Science Foundation of Guangdong Province(No.2016A030312014)the GDAS'Project of Science and Technology Development(No.2019GDA-SYL-0103007).
文摘Nine new compounds,including five natural rarely-occurring 2,3-dihydro-1H-indene derivatives named diaporindenes E−I(1−5),and four new benzophenone analogues named tenellones J−M(6−9)were isolated from the deep-sea sediment-derived fungus Phomopsis lithocarpus FS508.All the structures for these new compounds were fully characterized on the basis of spectroscopic data,NMR spectra,and ECD calculation and single-crystal X-ray diffraction analysis.The potential anti-tumor activities of compounds 1−9 against four tumor cell lines SF-268,MCF-7,HepG-2,and A549 were evaluated using the SRB method.Compound 7 exhibited cytotoxic activity against the SF-268 cell line with an IC50 value of 11.36μmol·L^(−1).
