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Biomedical subjects

Li Hong Hu

Publications and source records attributed to Li Hong Hu.

4 recordsLinked to original sources

Design, synthesis, and SAR analysis of cytotoxic sinapyl alcohol derivatives.

Five series totalling 51 of sinapyl alcohol derivatives were designed and synthesized. Their cytotoxicity analyses were performed on six human tumor cell lines such as PC-3, CNE, KB, A549, BEL-7404, and HeLa. Certain sinapyl alcohol derivatives showed significant cytotoxic activities. Compound 14d exhibited especially potent cytotoxicity against the BEL-7404 cell line with an IC50 value of 0.7 microM, which showed more cytotoxic activity than the positive control, cisplatin. The structure-cytotoxicity relationships were discussed and the CoMFA analysis was performed using the cytotoxic data against HeLa cells as a template.

Antineoplastic Agents↗

Synthesis and biological evaluation of a natural ester sintenin and its synthetic analogues.

Synthesis of 3-(3,4-dimethoxyphenyl)propyl-3-(3,4-dimethoxyphenyl) propanoate (18), a cytotoxic natural ester, was carried out by a convenient synthetic path with a total yield of 49%. Sixteen of its analogues (19-34) were also prepared. Seventeen unsaturated derivatives of 18, compounds 1-17, were also synthesized to examine the structure-activity relationship of this type of ester. All of the synthetic compounds were passed through the cytotoxicity screenings on human tumor cell lines, such as PC-3, Hela, A549, BEL7404, CNE, and KB. Some of the esters exhibited moderate inhibitory effects on these tumor cell lines. The phenolic derivatives exhibited the highest cytotoxicity among these derivatives, while the unsaturated esters were more cytotoxic than the saturated analogues. Some of the compounds also exhibited inhibition on alpha-glucosidase.

Antineoplastic Agents↗

Diterpene derivative and chromone from Hypericum perforatum.

A novel diterpene derivative, 5-methyl-5-(4,8,12-trimethyl-tridecyl)-dihydro-furan-2-one (1) and a new chromone, 5-hydroxy-7-methoxy-3-methyl-chromen-4-one (2), along with a known compound, phytol (3) have been isolated from the aerial parts of Hypericum perforatum. Their structures were established on the basis of spectroscopic analysis and by comparison with published values.

Chromans↗

Natural PTP1B inhibitors from Broussonetia papyrifera.

Two new compounds, 8-(1,1-dimethylallyl)-5'-(3-methylbut-2-enyl)-3',4',5,7-tetrahydroxyflanvonol (1), 3'-(3-methylbut-2-enyl)-3',4',7-trihydroxyflavane (2) and three known compounds 3,3',4',5,7-pentahydroxyflavone (3), uralenol (4), broussochalcone A (5) were isolated from the roots of Broussonetia papyrifera, and their structures determined by spectroscopic methods. Compounds 1, 3, 4 and 5 significantly show the inhibitory activities against the PTP1B enzyme.

Enzyme Inhibitors↗