2-(3,4-Dimethoxyphenyl)-5,7-dimethoxy-3,8-dimethyl-4H-1-benzopyran-4-one

The crystal structure of 2-(3,4-dimethoxyphenyl)-5,7-dimethoxy-3,8-dimethyl-4H-1-benzopyran-4-one (alternatively 3\u27,4\u27-dimethoxyphenyl-5,7-dimethoxy-3,8-dimethylflavone),C21H22O6, known to be a potent and selective inhibitor of rat heart cytosolic cyclic nucleotide phosphodiesterases, has been determined. In the benzopyran ring system, the pyran ring is slightly puckered. The structure is stabilized by weak C-H...O hydrogen bonds and by π-π interactions between pyran rings

1-(2-Hydroxy-4,6-dimethoxy-3-methylphenyl)-3-(4-methoxyphenyl)-2-methyl-1,3-propanedione

The crystal structure of the title compound, C20H22O6, an intermediate in the synthesis of the flavone 2-(4-methoxy-phenyl)-5,7-dimethoxy-3,8-dimethyl-4H-1-benzopyran-4-one, has been determined. The molecules are held together by van der Waals forces. There is an intramolecular hydrogen bond between the hydroxy group and the neighbouring keto O atom. The molecules in the crystal structure are disordered, with significantly different orientations of the methyl group in the disordered 4-methoxyphenyl substituent

1-(2-Hydroxy-4,6-dimethoxy-3-methylphenyl)-3-(4-methoxyphenyl)-2-methyl-1,3-propanedione

The crystal structure of the title compound, C20H22O6, an intermediate in the synthesis of the flavone 2-(4-methoxy-phenyl)-5,7-dimethoxy-3,8-dimethyl-4H-1-benzopyran-4-one, has been determined. The molecules are held together by van der Waals forces. There is an intramolecular hydrogen bond between the hydroxy group and the neighbouring keto O atom. The molecules in the crystal structure are disordered, with significantly different orientations of the methyl group in the disordered 4-methoxyphenyl substituent

2-(3,4-Dimethoxyphenyl)-5,7-dimethoxy-3,8-dimethyl-4H-1-benzopyran-4-one

The crystal structure of 2-(3,4-dimethoxyphenyl)-5,7-dimethoxy-3,8-dimethyl-4H-1-benzopyran-4-one (alternatively 3\u27,4\u27-dimethoxyphenyl-5,7-dimethoxy-3,8-dimethylflavone),C21H22O6, known to be a potent and selective inhibitor of rat heart cytosolic cyclic nucleotide phosphodiesterases, has been determined. In the benzopyran ring system, the pyran ring is slightly puckered. The structure is stabilized by weak C-H...O hydrogen bonds and by π-π interactions between pyran rings

Nigratine as first-in-class dual inhibitor of necroptosis and ferroptosis regulated cell death

Nigratine (also known as 6E11), a natural flavanone derivative, was characterized as highly specific non-ATP competitive inhibitor of RIPK1 kinase, one of the key component of necroptotic cell death signaling. We show here that nigratine inhibited both necroptosis (induced by Tumor Necrosis Factor-α) and ferroptosis (induced by glutamate, erastin or RSL3 small chemical compounds) with EC50 in the µM range. Altogether, the data obtained showed that nigratine is the first-in-class dual inhibitor of necroptosis and ferroptosis cell death routes and opened new therapeutic avenues for treating complex necrosis-related diseases

Nigratine as dual inhibitor of necroptosis and ferroptosis regulated cell death

International audienceNigratine (also known as 6E11), a flavanone derivative of a plant natural product, was characterized as highly specific non-ATP competitive inhibitor of RIPK1 kinase, one of the key components of necroptotic cell death signaling. We show here that nigratine inhibited both necroptosis (induced by Tumor Necrosis Factor-α) and ferroptosis (induced by the small molecules glutamate, erastin, RSL3 or cumene hydroperoxide) with EC 50 in the µM range. Taken together, our data showed that nigratine is a dual inhibitor of necroptosis and ferroptosis cell death pathways. These findings open potential new therapeutic avenues for treating complex necrosis-related diseases