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Journals and Conferences
The synthesis, GSK-3β inhibitory activity, and anti-microbial activity of bicyclic and tricyclic derivatives of the 5,7-diamino-6-fluoro-4-quinolone-3-carboxylic acid scaffold were studied. Kinase selectivity profiling indicated that members of this class were potent and highly selective GSK-3 inhibitors.
We previously disclosed tricylic, 6-carboxylic acid-bearing 4-quinolones as GSK-3β inhibitors. Herein we discuss the optimization of this series to yield a series of more potent 6-nitrile analogs with insignificant anti-microbial activity. Finally, kinase profiling indicated that members of this class were highly specific GSK-3 inhibitors.
As the result of a rhJNK1 HTS, the imidazo[1,2-a]quinoxaline 1 was identified as a 1.6 μM rhJNK1 inhibitor. Optimization of this compound lead to AX13587 (rhJNK1 IC50=160 nM) which was co-crystallized with JNK1 to identify key molecular interactions. Kinase profiling against 125+ kinases revealed AX13587 was an inhibitor of JNK, MAST3, and MAST4 whereas its… (More)
Palmelloids induced in the unicellular green alga Chlamydomonas eugametos by chloroplatinic acid treatment have been studied electron microscopically. Thin-sectioned specimens revealed the multilayer nature of the cell walls after second division within the palmelloid. Although synchrony in cell division is lost, to a certain degree, within the palmelloid,… (More)
or quinolinic acid (or both). The modifying gene has no demonstrable effect on the utilization of exogenously supplied nicotinamide (K. Nakamura and C. S. Gowans, Genetics 51:931, 1965). Two observations strongly indicate that the modifying gene does not operate through a modification of the pathway of synthesis of niacin. First, the nicotinamide auxotrophs… (More)
The mutual attraction of conidia to protoperithecia of the opposite mating type was studied genetically in crosses where a mixture of conidia from two different strains, one of which was marked by an ascospore color mutant gene tan spore (ts), was applied to protoperithecia. Selective fertilization was measured as the frequency of perithecia fertilized by… (More)