Sulfamide benzodiazepines

A series of sulfamide benzodiazepines 204 have been prepared and their p5 3-murine double minute 2 (MDM2) inhibitory activity and in vitro antitumor activity were evaluated (14MI15741). These heterocycles demonstrated moderate inhibition of p53 MDM2 protein—protein interaction. Intramolecular 1,3-dipolar cycloaddition of a l-(azidoarylsulfonyl)-2-alke-nyl pyrrolidine yielded aziridino-fused pyrrolo[l,2,5]benzothiadiazepine 205 as the only isolable product this system and other henzodiazepines are under investigation for antitumor and antibiotic potential (14MOL16737). 

The relationship between the retention behavior of benzodiazepine, sulfamides, substituted anilines, barbiturates, a group of natural phenolic derivatives, diethanolamine isomers, amino acids, sulfoether, thio-alcohol, 2,4-dinitrophenylhydrazones, and their molecular connectivity indices were studied. All of the results indicate that the Rf or values are highly correlated with molecular connectivity indices. 

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See also in sourсe #XX -- [ , ]

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