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A unique pentaketide dimer structure of a novel fungal metabolite with antiangiogenic activity, designated as epoxyquinol A (1), was determined on the basis of NMR spectral data as well as the X-ray crystallographic analysis. 1 inhibits the endothelial migration induced by vascular endothelial growth factor (ED100 = 3 mug/mL).

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[structure: see text] Azaspirene isolated from the fungus Neosartorya sp. is a novel angiogenesis inhibitor with a 1-oxa-7-azaspiro[4.4]non-2-ene-4,6-dione skeleton. Azaspirene inhibits the endothelial migration induced by vascular endothelial growth factor (ED100 = 27.1 microM).

Zearalenones are mycotoxins with estrogenic activity consisting of a resorcinol moiety fused to a 14-membered macrocyclic lactone and are produced by various Fusarium species. We found that Clonostachys rosea IFO 7063 was effectively capable of converting zearalenone (1) to cleavage product (2), 1-(3,5-dihydroxyphenyl)-10'-hydroxy-1'E-undecene-6'-one. Moreover, cleavage product 2 did not show potent estrogenic activity like that of 1 and 17beta-estradiol in the human breast cancer MCF-7 cell proliferation assay.

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The asymmetric total synthesis of (+)-panepophenanthrin, an inhibitor of ubiquitin-activating enzyme (E1), has been accomplished using catalytic asymmetric alpha aminoxylation of 1,4-cyclohexanedione monoethylene ketal as a key step, followed by several diastereoselective reactions. The biomimetic Diels-Alder reaction of a monomer precursor was found to proceed efficiently in water. The investigation of the biological properties of new derivatives of (+)-panepophenanthrin enabled us to develop new cell-permeable E1 inhibitors, RKTS-80, -81, and -82.

Morphological Reversion of srcts-NRK Cells Rat kidney cells infected with ts25, a T-class mutant of Rous sarcoma virus Prague strain (,srcts-NRK)3) were cultured at permissive temperature (32°C) or at nonpermissive temperature (39°C) in Eagle's minimal essential medium (MEM) supplemented with 10% fetal bovine serum (FBS, Gibco Laboratories, Grand Island, NY., U.S.A.). The cells maintained at 32°C were seeded into a 96-well microtiter plate (2 x 104cells/200/il/well) and cultured for 4 hours at 32°C in a CO2 incubator. Solutions of various concentrations of reveromycins (10 fA each) were added and morphological reversion of 5rcts-NRK cells was observed under a microscope after 18 to 20 hours incubation at 32°C. The activity was presented as ft Present address: