Novel benzofuran-3-one indole inhibitors of PI3 kinase-α and the mammalian target of rapamycin: hit to lead studies was written by Bursavich, Matthew G.;Brooijmans, Natasja;Feldberg, Lawrence;Hollander, Irwin;Kim, Stephen;Lombardi, Sabrina;Park, Kaapjoo;Mallon, Robert;Gilbert, Adam M.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2010.Safety of 5-Chloroindole-3-carboxaldehyde This article mentions the following:
A series of benzofuran-3-one indole phosphatidylinositol-3-kinases (PI3K) inhibitors identified via HTS has been prepared The optimized inhibitors possess single digit nanomolar activity against p110α (PI3K-α), good pharmaceutical properties, selectivity vs. p110γ (PI3K-γ), and tunable selectivity vs. the mammalian target of rapamycin (mTOR). Modeling of compounds I (R = H; CH2CH2CH2NMe2) in homol. models of PI3K-α and mTOR supports the proposed rationale for selectivity. Compounds show activity in multiple cellular proliferation assays with signaling through the PI3K pathway confirmed via phospho-Akt inhibition in PC-3 cells. In the experiment, the researchers used many compounds, for example, 5-Chloroindole-3-carboxaldehyde (cas: 827-01-0Safety of 5-Chloroindole-3-carboxaldehyde).
5-Chloroindole-3-carboxaldehyde (cas: 827-01-0) belongs to indole derivatives. Indole, also called Benzopyrrole, a heterocyclic organic compound occurring in some flower oils, such as jasmine and orange blossom, in coal tar, and in fecal matter. They are capable of binding to a variety of receptors with high affinity and thus have applications in a wide range of therapeutic areas.Safety of 5-Chloroindole-3-carboxaldehyde
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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