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Hybrid molecules of estrone: New compounds with potential antibacterial, antifungal, and antiproliferative activities by J. Adamec; R. Beckert; D. Weiß; V. Klimešová; K. Waisser; U. Möllmann; J. Kaustová; V. Buchta is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

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New hybrid molecules of estrone were synthesized as compounds indicating promising biological activity (antibacterial, antimycobacterial, antifungal, and antiproliferative). The prepared molecules contained various heterocyclic units (pyridine, benzylsulfanyl derivatives of pyridine or derivatives of tetrazole) linked to estrone by n-heptyl bridges. The compounds with charge on molecule (the hybrid pyridinium or benzylsulfanylpyridinium salts) exhibited significant biological activity (antibacterial, antimycobacterial, antifungal, and antiproliferative). On the other hand, the compounds not in the form of salts (x-(1-phenyl-5-tetrazolylthio)heptylethers of estrone) were inactive. The antimycobacterial activities of three different series of tetrazole derivatives (i.e., the hybrid molecules with estrone, tetrazole-5-thiols, and 5-benzylsulfanyl-1-phenyltetrazoles) with the same substituents on phenyl ring were compared. Amongst them, the 5-benzylsulfanyl-1-phenyltetrazoles were the most potent.

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Author

J. Adamec; R. Beckert; D. Weiß; V. Klimešová; K. Waisser; U. Möllmann; J. Kaustová; V. Buchta

Publisher

Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0968-0896)

Published

2007

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)