408354-40-5Relevant articles and documents
Design and synthesis of (aza)indolyl maleimide-based covalent inhibitors of glycogen synthase kinase 3β
Yang, Zhimin,Liu, Hui,Pan, Botao,He, Fengli,Pan, Zhengying
supporting information, p. 4127 - 4140 (2018/06/12)
As an important kinase in multiple signal transduction pathways, GSK-3β has been an attractive target for chemical probe discovery and drug development. Compared to numerous reversible inhibitors that have been developed, covalent inhibitors of GSK-3β are
Dearomatization of tryptophols via a vanadium-catalyzed asymmetric epoxidation and ring-opening cascade
Han, Long,Liu, Chuan,Zhang, Wei,Shi, Xiao-Xin,You, Shu-Li
supporting information, p. 1231 - 1233 (2014/02/14)
An enantioselective epoxidation of tryptophols followed by an intramolecular epoxide opening reaction was realized by chiral vanadium catalysts derived from C2 symmetric bis-hydroxamic acid (BHA) ligands. 3a-Hydroxyfuroindoline derivatives with up to 89% yield and 90% ee were obtained under mild reaction conditions.
Three oxidative metabolites of indole-3-acetic acid from Arabidopsis thaliana
Kai, Kenji,Horita, Junko,Wakasa, Kyo,Miyagawa, Hisashi
, p. 1651 - 1663 (2008/02/05)
Three metabolites of indole-3-acetic acid (IAA), N-(6-hydroxyindol-3-ylacetyl)-phenylalanine (6-OH-IAA-Phe), N-(6-hydroxyindol-3-ylacetyl)-valine (6-OH-IAA-Val), and 1-O-(2-oxoindol-3-ylacetyl)-β-d-glucopyranose (OxIAA-Glc), were found by a liquid chromatography-electrospray ionization-tandem mass spectrometry (LC-ESI-MS/MS)-based search for oxidative IAA metabolites during the vegetative growth of Arabidopsis. Their structures were confirmed by making a comparison of chromatographic characteristics and mass spectra between naturally occurring compounds and synthetic standards. An incorporation study using deuterium-labeled compounds showed that 6-OH-IAA-Phe and 6-OH-IAA-Val were biosynthesized from IAA-Phe and IAA-Val, respectively, which strongly suggested the formation of these amino acid conjugates of IAA in plants. Both 6-OH-IAA-Phe and 6-OH-IAA-Val were inactive as auxins, as indicated by no significant root growth inhibition in Arabidopsis. Quantitative analysis demonstrated that OxIAA-Glc was present in the largest amount among the metabolites of IAA in Arabidopsis, suggesting that the conversion into OxIAA-Glc represents the main metabolic process regarding IAA in Arabidopsis.
Synthesis, determination of stereochemistry, and evaluation of new bisindole alkaloids from the myxomycete Arcyria ferruginea: An approach for Wnt signal inhibitor
Kaniwa, Kouken,Arai, Midori A.,Li, Xiaofan,Ishibashi, Masami
, p. 4254 - 4257 (2008/02/13)
To determine the stereochemistry of dihydroarcyriarubin C (1), new bisindole alkaloid isolated from the myxomycete Arcyria ferruginea, cis- (2) and trans-dihydroarcyriarubin C (3) were synthesized. Comparison of their NMR characteristics allowed the trans
Synthetic Approaches to Indolo[6,7-α]pyrrolo[3,4-c]carbazoles: Potent Cyclin D1/CDK4 Inhibitors
Faul, Margaret M.,Engler, Thomas A.,Sullivan, Kevin A.,Grutsch, John L.,Clayton, Marcella T.,Martinelli, Michael J.,Pawlak, Joseph M.,LeTourneau, Michael,Coffey, D. Scott,Pedersen, Steven W.,Kolis, Stanley P.,Furness, Kelly,Malhotra, Sushant,Al-Awar, Rima S.,Ray, James E.
, p. 2967 - 2975 (2008/04/18)
Synthesis of indolo[6,7-α]pyrrolo[3,4-c]carbazoles 1, a new class of cyclin D1/CDK4 inhibitors, by oxidation of the corresponding aryl indolylmaleimides 2, will be described. Two approaches to the synthesis of 2 were identified that required new methods f
Novel, potent and selective cyclin D1/CDK4 inhibitors: Indolo[6,7-a]pyrrolo[3,4-c]carbazoles
Engler, Thomas A.,Furness, Kelly,Malhotra, Sushant,Sanchez-Martinez, Concha,Shih, Chuan,Xie, Walter,Zhu, Guoxin,Zhou, Xun,Conner, Scott,Faul, Margaret M.,Sullivan, Kevin A.,Kolis, Stanley P.,Brooks, Harold B.,Patel, Bharvin,Schultz, Richard M.,DeHahn, Tammy B.,Kirmani, Kashif,Spencer, Charles D.,Watkins, Scott A.,Considine, Eileen L.,Dempsey, Jack A.,Ogg, Catherine A.,Stamm, Nancy B.,Anderson, Bryan D.,Campbell, Robert M.,Vasudevan, Vasu,Lytle, Michelle L.
, p. 2261 - 2267 (2007/10/03)
The synthesis and CDK inhibitory properties of a series of indolo[6,7-a]pyrrolo[3,4-c]carbazoles is reported. In addition to their potent CDK activity, the compounds display antiproliferative activity against two human cancer cell lines. These inhibitors also effect strong G1 arrest in these cell lines and inhibit Rb phosphorylation at Ser780 consistent with inhibition of cyclin D1/CDK4.
