Kemnitzer, William published the artcileDiscovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high throughput screening assay. Structure-activity relationships of N-alkyl substituted pyrrole fused at the 7,8-positions, Application of 4-(Benzyloxy)-1-methyl-1H-indole, the main research area is aryl chromene preparation structure antitumor neoplasm.
In the continuing effort to discover and develop apoptosis inducing 4-aryl-4H-chromenes as novel anticancer agents, the authors explored the structure-activity relationship (SAR) of alkyl substituted pyrrole fused at the 7,8-positions. A Me group substituted at the nitrogen in the 7-position of the pyrrole ring led to a series of potent apoptosis inducers with potency in the low nanomolar range. These compounds were also found to be low nanomolar or subnanomolar inhibitors of cell growth, and they inhibited tubulin polymerization, indicating that methylation of the 7-position nitrogen does not change the mechanism of action of these chromenes. Compound 2 d was identified as a highly potent apoptosis inducer with an EC50 value of 2 nM and a highly potent inhibitor of cell growth with a GI50 value of 0.3 nM in T47D cells.
Journal of Medicinal Chemistry published new progress about Antitumor agents. 13523-93-8 belongs to class indole-building-block, name is 4-(Benzyloxy)-1-methyl-1H-indole, and the molecular formula is C16H15NO, Application of 4-(Benzyloxy)-1-methyl-1H-indole.
Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles