Publications by authors named "Huan-fang Guo"
[Progress in the new nonnucleoside anti-HIV reverse transcriptase inhibitor-DCK].
Yao Xue Xue Bao
October 2008
3',4'-Di-O-(S)-comphanoyl-(+)-cis-khellactone (DCK) is a synthetic khellactone ester that exhibits potent anti-HIV activity with a mechanism distinct from clinically used anti-HIV agents. Several series of DCK analoges have been synthesized and evaluated for inhibitory effects against HIV. This review article describes recent progress in the discovery, structural modification, and structure-activity relationship studies of potent anti-HIV DCK derivatives.
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- Researchers improved the synthesis process of this compound to increase its yield significantly from 7.8% to 32%.
- Pharmacokinetic studies showed that the compound has moderate absorption and retention properties, making it a strong candidate for further clinical trials as an anti-HIV treatment.
Article Synopsis
- A series of seselin and related angular pyranocoumarin compounds were successfully synthesized from 8-acetyl-7-hydroxycoumarins, achieving a total yield of over 50% through a series of chemical reactions.
- Twelve of these derivatives were evaluated for their pain-relieving effects using the writhing response assay, where seselin (4a) and another derivative (2b) exhibited significant antinociceptive activity with 85% and 50% inhibition, respectively.
- The results suggest that these seselin derivatives have potential as new pain relief medications, potentially outperforming aspirin in their effectiveness.
Twenty-six unsymmetrical biphenyls were synthesized and evaluated for cytotoxic activity against DU145, A549, KB and KB-Vin tumor cell lines. Three compounds 27, 35 and 40 showed very potent activity against the HTCL panel with an IC(50) value range of 0.04-3.
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