C07C245/04

COMPOSITIONS AND METHODS FOR QUADRICYCLANE MODIFICATION OF BIOMOLECULES
20190389817 · 2019-12-26 ·

The present disclosure features a strain-promoted [2+2+2] reaction that can be carried out under physiological conditions. In general, the reaction involves reacting a pi-electrophile with a low lying LUMO with a quadricyclane on a biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provides for its application in vivo and in vitro. The reaction is compatible with modification of living cells. In certain embodiments, the pi-electrophile can comprise a molecule of interest that is desired for delivery to a quadricyclane-containing biomolecule via [2+2+2] reaction.

COMPOSITIONS AND METHODS FOR QUADRICYCLANE MODIFICATION OF BIOMOLECULES
20190389817 · 2019-12-26 ·

The present disclosure features a strain-promoted [2+2+2] reaction that can be carried out under physiological conditions. In general, the reaction involves reacting a pi-electrophile with a low lying LUMO with a quadricyclane on a biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provides for its application in vivo and in vitro. The reaction is compatible with modification of living cells. In certain embodiments, the pi-electrophile can comprise a molecule of interest that is desired for delivery to a quadricyclane-containing biomolecule via [2+2+2] reaction.

Azophenols as ERG Oncogene Inhibitors

Selective azophenol inhibitors of a wild type or an altered ERG protein expression are described, where the inhibitors represent a compound of Formula (I) or Formula (II)

##STR00001##

wherein X, X.sub.1, X.sub.2, X.sub.3, X.sub.4 and X.sub.5, R.sub.1 through R.sub.4 and R.sub.9 are as described.

Azophenols as ERG Oncogene Inhibitors

Selective azophenol inhibitors of a wild type or an altered ERG protein expression are described, where the inhibitors represent a compound of Formula (I) or Formula (II)

##STR00001##

wherein X, X.sub.1, X.sub.2, X.sub.3, X.sub.4 and X.sub.5, R.sub.1 through R.sub.4 and R.sub.9 are as described.

Compositions and methods for quadricyclane modification of biomolecules

The present disclosure features a strain-promoted [2+2+2] reaction that can be carried out under physiological conditions. In general, the reaction involves reacting a pi-electrophile with a low lying LUMO with a quadricyclane on a biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provides for its application in vivo and in vitro. The reaction is compatible with modification of living cells. In certain embodiments, the pi-electrophile can comprise a molecule of interest that is desired for delivery to a quadricyclane-containing biomolecule via [2+2+2] reaction.

Compositions and methods for quadricyclane modification of biomolecules

The present disclosure features a strain-promoted [2+2+2] reaction that can be carried out under physiological conditions. In general, the reaction involves reacting a pi-electrophile with a low lying LUMO with a quadricyclane on a biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provides for its application in vivo and in vitro. The reaction is compatible with modification of living cells. In certain embodiments, the pi-electrophile can comprise a molecule of interest that is desired for delivery to a quadricyclane-containing biomolecule via [2+2+2] reaction.

Azophenols as ERG oncogene inhibitors

Selective azophenol inhibitors of a wild type or an altered ERG protein expression are described, where the inhibitors represent a compound of Formula (I) or Formula (II) ##STR00001##
wherein X, X.sub.1, X.sub.2, X.sub.3, X.sub.4 and X.sub.5, R.sub.1 through R.sub.4 and R.sub.9 are as described.

Azophenols as ERG oncogene inhibitors

Selective azophenol inhibitors of a wild type or an altered ERG protein expression are described, where the inhibitors represent a compound of Formula (I) or Formula (II) ##STR00001##
wherein X, X.sub.1, X.sub.2, X.sub.3, X.sub.4 and X.sub.5, R.sub.1 through R.sub.4 and R.sub.9 are as described.

Azophenols as ERG Oncogene Inhibitors

Selective azophenol inhibitors of a wild type or an altered ERG protein expression are described, where the inhibitors represent a compound of Formula (I) or Formula (II)

##STR00001##

wherein X, X.sub.1, X.sub.2, X.sub.3, X.sub.4 and X.sub.5, R.sub.1 through R.sub.4 and R.sub.9 are as described.

COMPOSITIONS AND METHODS FOR QUADRICYCLANE MODIFICATION OF BIOMOLECULES
20170152234 · 2017-06-01 ·

The present disclosure features a strain-promoted [2+2+2] reaction that can be carried out under physiological conditions. In general, the reaction involves reacting a pi-electrophile with a low lying LUMO with a quadricyclane on a biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provides for its application in vivo and in vitro. The reaction is compatible with modification of living cells. In certain embodiments, the pi-electrophile can comprise a molecule of interest that is desired for delivery to a quadricyclane-containing biomolecule via [2+2+2] reaction.