Synthesis and first biological evaluation of 1-aza-9-oxafluorenes as novel lead structures for the development of small-sized cytostatics |
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| Authors: | Brachwitz Kristin Hilgeroth Andreas |
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| Affiliation: | Institute of Pharmaceutical Chemistry, Department of Pharmacy, Martin-Luther-University, Halle-Wittenberg, 4, Wolfgang-Langenbeck-Str., 06120 Halle, Germany. |
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| Abstract: | A first series of novel 1-aza-9-oxafluorenes has been prepared from 3-carbonyl substituted 1,4-dihydropyridines and p-benzoquinone as small-sized cytostatics. Biological evaluation has been carried out in various cancer cell-lines. First structure-activity relationships proved the 4-phenyl substituent to be more favorable than the 4-methyl substituent. Cytostatic properties are discussed. |
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