The synthesis and aromatase inhibitory activity of a new series of 2-benzylidene indanones is presented. The imidazolyl-substituted indanones displayed potent aromatase inhibitory activity. The vanilloid-based derivative 2-[4-(3-imidazol-1-ylpropoxy)-3-methoxybenzylidene]-indan-1-one (26) exhibited maximum inhibition of human placental aromatase and was found to be 54 times more potent as compared to aminoglutethimide.
al'ready been reduced by about 8 hours from that originally required, and a further decrease is anticipated by using higher-pressure systems and optimizing operating parameters such as tempwature and elution gradient.The capability of the system we have described is limited to the analysis of ultraviolet-absorbing constituents of urine; however, it could be extended by incorporation of additional detection systems. For example, if the ninhydrin colorimetric detection system ( 13 ) and a carbohydrate colorimetric technique recently developed by Green ( 14) could be integrated into the present analyzer (while using the same separation system) , the resulting instrument would be able to detect a much larger number of compounds.
Unexpected dimers of some 2‐substituted indan‐1‐one derivatives were isolated during aldol condensation of indan‐1‐one with various aldehydes in the presence of KOH (see Scheme). Monomeric products, usually expected from aldol condensation, further underwent a base‐catalyzed nucleophilic addition reaction to their dimeric form in some cases. The structures of these dimers were characterized by using various spectral techniques and in one case, structural details were determined from a high‐resolution crystallographic analysis.
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