59258-25-2Relevant academic research and scientific papers
Ecofriendly bromination of chalcones and synthesis of flavones using grinding technique
Jakhar, Komal,Makrandi
, p. 141 - 145 (2013/02/23)
Selective bromination of chalcones and 2'-hydroxychalcones has been carried out with ammonium bromide and ammonium persulphate using grinding technique at RT under aqueous moist condition to give α,β-dibromochalcones and α,β-dibromo-2'- hydroxychalcones respectively. α,β- Dibromo-2'-hydroxychalcones have been cyclodehydrobrominated with barium hydroxide moist and ethanol at RT to give flavones using grinding technique.
Design, synthesis and biological evaluation of bis(hydroxyphenyl) azoles as potent and selective non-steroidal inhibitors of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) for the treatment of estrogen-dependent diseases
Bey, Emmanuel,Marchais-Oberwinkler, Sandrine,Kruchten, Patricia,Frotscher, Martin,Werth, Ruth,Oster, Alexander,Alguel, Oztekin,Neugebauer, Alexander,Hartmann, Rolf W.
, p. 6423 - 6435 (2008/12/22)
The 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) catalyses the reduction of the weakly active estrone (E1) into the most potent estrogen, 17β-estradiol (E2). E2 stimulates the growth of hormone-dependent diseases via activation of the estrogen receptors (ERs). 17β-HSD1 is often over-expressed in breast cancer cells. Thus, it is an attractive target for the treatment of mammary tumours. The combination of a ligand- and a structure-based drug design approach led to the identification of bis(hydroxyphenyl) azoles as potential inhibitors of 17β-HSD1. Different azoles and hydroxy substitution patterns were investigated. The compounds were evaluated for activity and selectivity with regard to 17β-HSD2, ERα and ERβ. The most potent compound is 3-[5-(4-hydroxyphenyl)-1,3-oxazol-2-yl]phenol (18, IC50 = 0.31 μM), showing very good selectivity, high cell permeability and medium CaCo-2 permeability.
