[Progress in the new nonnucleoside anti-HIV reverse transcriptase inhibitor-DCK].

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.

[Synthesis and antinociceptive activity of seselin derivatives].

Natural product seselin and related derivatives with an angular pyranocoumarin skeleton were synthesized from 8-acetyl-7-hydroxycoumarins by condensation with acetone, reduction, and dehydration successively under mild conditions with total yield of > 50%. Twelve seselin derivatives were tested by the writhing response assay induced by acetic acid at a dose of 40 mg x kg(-1). Seselin (4a) and 4,8,8-trimethyl-9,9-dihydro-pyran[2,3-f] chromene-2,10-dione (2b) showed obviously antinociceptive activity with inhibitory effect of 85% and 50%, respectively, more or quite potent than aspirin in the same assay, suggesting that seselin derivatives could be a novel kind of potential antinociceptive agents.

Synthesis of unsymmetrical biphenyls as potent cytotoxic agents.

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.