5691-08-7Relevant academic research and scientific papers
Novel benzofuran-3-one indole inhibitors of PI3 kinase-α and the mammalian target of rapamycin: Hit to lead studies
Bursavich, Matthew G.,Brooijmans, Natasja,Feldberg, Lawrence,Hollander, Irwin,Kim, Stephen,Lombardi, Sabrina,Park, Kaapjoo,Mallon, Robert,Gilbert, Adam M.
scheme or table, p. 2586 - 2590 (2010/06/19)
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 versus p110γ (PI3K-γ), and tunable selectivity versus the mammalian target of rapamycin (mTOR). Modeling of compounds 9 and 32 in homology 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.
Photochemical electrocyclisation of 3-vinylindoles to pyrido[2,3-a]-, pyrido[4,3-a]- and thieno[2,3-a]-carbazoles: Design, synthesis, DNA binding and antitumor cell cytotoxicity
Lemster, Thomas,Pindur, Ulf,Lenglet, Gaelle,Depauw, Sabine,Dassi, Christelle,David-Cordonnier, Marie-Helene
experimental part, p. 3235 - 3252 (2009/12/04)
In the context of the design and synthesis of DNA ligands, some new hetarene annelated carbazoles were synthesized. As lead structure the intercalating tetracyclic systems pyrido[2,3-a]- and pyrido[4,3-a]-carbazoles and in one case a thieno[2,3-a]-carbazo
Creation of new promoters for plant's root growth: its application for the syntheses of vulcanine and borreline, and for combating desertification at gobi desert in inner mongolia 1#
Somei, Masanori,Sayama, Shinsuke,Naka, Katsumi,Shinmoto, Kotaro,Yamada, Fumio
experimental part, p. 537 - 554 (2009/09/25)
Abstract - Various new 2-substituted indole-3-carbaldehydes are prepared. Structurally related alkaloids, vulcanine and borreline, are synthesized as well. Among the compounds, 2-haloindole-3-carbaldehydes are found to be potent promoters of plant's root growth. Its successful preliminary application is reported for making Gobi desert in Inner Mongolia full of plant.
A CONVENIENT SYNTHETIC METHOD OF 2-SUBSTITUTED INDOLES AND ITS APPLICATION FOR THE SYNTHESIS OF NATURAL ALKALOID, BORRERINE
Somei, Masanori,Sayama, Shinsuke,Naka, Katsumi,Yamada, Fumio
, p. 1585 - 1588 (2007/10/02)
A simple synthetic method of 2-substituted indoles is developed.Total synthesis of natural alkaloid, borrerine, is also reported
