Synthesis and binding affinity to human alpha and beta estrogen receptors of various 7-hydroxycoumarins substituted at 4- and 3,4- positions.

The study of the relative binding affinity (RBA) to the human alpha and beta estrogen receptors (ERs) of various 7-hydroxycoumarins substituted at 4- and 3,4- positions is weak and lacks in selectivity for both ERalpha and ERbeta. The 4-(4-hydroxyphenyl)-7-hydroxycoumarin shows a weak RBA to ERbeta and 3,4-diphenyl-7-hydroxycoumarin presents a stronger RBA to ERalpha than ERbeta.

Synthesis and relative binding affinity to human steroid receptors of substituted 3-aryloxycoumarins.

The synthesis of a set of substituted 3-aryloxycoumarins was performed. The study of the relations between their structure and their relative binding affinity to human androgen, progesterone, alpha and beta estrogen receptors was achieved.

Structure-activity relationships of some 3-substituted-4-hydroxycoumarins as HIV-1 protease inhibitors.

The screening of the HIV-1 protease (PR) inhibitory activity (IC-50) of various substituted 3-phenyl-4-hydroxycoumarins, 3-benzyl-4-hydroxycoumarins, 3-phenoxy-4-hydroxy-coumarins, 3-benzenesulfonyl-4-hydroxycoumarins and 3-(7-coumarinyloxy)-4-hydroxycoumarins was performed. The data indicate the importance of substituents at positions 5 and 7 of the coumarin ring on the inhibitory potency of the HIV-1-PR.