α-Arylidene Diacylglycerol-Lactones (DAG-Lactones) as Selective Ras Guanine-Releasing Protein 3 (RasGRP3) Ligands was written by Ann, Jihyae;Czikora, Agnes;Saini, Amandeep S.;Zhou, Xiaoling;Mitchell, Gary A.;Lewin, Nancy E.;Peach, Megan L.;Blumberg, Peter M.;Lee, Jeewoo. And the article was included in Journal of Medicinal Chemistry in 2018.Name: 5-Chloroindole-3-carboxaldehyde This article mentions the following:
Diacylglycerol-lactones have proven to be a powerful template for the design of potent ligands targeting C1 domains, the recognition motif for the cellular second messenger diacylglycerol. A major objective has been to better understand the structure activity relations distinguishing the seven families of signaling proteins that contain such domains, of which the protein kinase C (PKC) and RasGRP families are of particular interest. Here, we synthesize a series of aryl/alkyl substituted diacylglycerol-lactones and probe their relative selectivities for RasGRP3 vs. PKC. Compound I showed 72.6-fold selectivity relative to PKC alpha and 45.1-fold selectivity relative to PKC epsilon for in vitro binding activity. Likewise, in intact cells compound I induced Ras activation, a downstream response to RasGRP stimulation, with 8-29 fold selectivity relative to PKC delta S299 phosphorylation, a measure of PKC delta stimulation. In the experiment, the researchers used many compounds, for example, 5-Chloroindole-3-carboxaldehyde (cas: 827-01-0Name: 5-Chloroindole-3-carboxaldehyde).
5-Chloroindole-3-carboxaldehyde (cas: 827-01-0) belongs to indole derivatives. Indole could be stereoselectively alkylated with chiral cyclopentyl sulfone reagent. More than 200 indole derivatives have already been marketed as drugs or are under advanced stages of clinical trials.Name: 5-Chloroindole-3-carboxaldehyde
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Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles