Sirisoma, Nilantha published the artcileDiscovery of substituted N’-(2-oxoindolin-3-ylidene)benzohydrazides as new apoptosis inducers using a cell- and caspase-based HTS assay, Computed Properties of 1677-47-0, the main research area is antitumor oxoindolinylidenebenzohydrazide preparation apoptosis neoplasm.
The discovery of a series of substituted N’-(2-oxoindolin-3-ylidene)benzohydrazides as inducers of apoptosis using a proprietary cell- and caspase-based ASAP HTS assay is reported. Through SAR studies, N’-(4-bromo-5-methyl-2-oxoindolin-3-ylidene)-3,4,5-trimethoxybenzohydrazide (3g) was identified as a potent apoptosis inducer with an EC50 value of 0.24 μM in human colorectal carcinoma HCT116 cells, more than a 40-fold increase in potency from the initial screening hit N’-(5-bromo-2-oxoindolin-3-ylidene)-3,4,5-trimethoxybenzohydrazide (2a). Compound 3g also was found to be highly active in a growth inhibition assay with a GI50 value of 0.056 μM in HCT116 cells. A group of potentially more aqueous soluble analogs were prepared and found to be highly active. Among them, compound 4e incorporating a Me piperazine moiety was found to have EC50 values of 0.17, 0.088 and 0.14 μM in human colorectal carcinoma cells HCT116, hepatocellular carcinoma cancer SNU398 cells and human colon cancer RKO cells, resp. Compounds 3g and 4e were found to function as inhibitors of tubulin polymerization
Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 1677-47-0 belongs to class indole-building-block, name is 4,5-Dichloroisatin, and the molecular formula is C8H3Cl2NO2, Computed Properties of 1677-47-0.
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