90347-64-1Relevant articles and documents
Dibenzofuran derivatives inspired from cercosporamide as dual inhibitors of pim and CLK1 kinases
Bach, Stéphane,Baratte, Blandine,Bazin, Marc-Antoine,Brachet-Botineau, Marie,Dao, Viet Hung,Denevault-Sabourin, Caroline,Gouilleux, Fabrice,Logé, Cédric,Marchand, Pascal,McCarthy, Florence O.,Ourliac-Garnier, Isabelle,Robert, Thomas,Thiéfaine, Jér?me,da Silva, Teresinha Gon?alves
, (2021/12/10)
Pim kinases (proviral integration site for Moloney murine leukemia virus kinases) are overexpressed in various types of hematological malignancies and solid carcinomas, and promote cell proliferation and survival. Thus, Pim kinases are validated as targets for antitumor therapy. In this context, our combined efforts in natural product-inspired library generation and screening furnished very promising dibenzo[b, d]furan derivatives derived from cercosporamide. Among them, lead compound 44 was highlighted as a potent Pim-1/2 kinases inhibitor with an additional nanomolar IC50 value against CLK1 (cdc2-like kinases 1) and displayed a low micromolar anticancer potency towards the MV4-11 (AML) cell line, expressing high endogenous levels of Pim-1/2 kinases. The design, synthesis, structure-activity relationship, and docking studies are reported herein and supported by enzyme, cellular assays, and Galleria mellonella larvae testing for acute toxicity.
Selectfluor F-TEDA-BF4 mediated and solvent directed iodination of aryl alkyl ketones using elemental iodine
Stavber, Stojan,Jereb, Marjan,Zupan, Marko
, p. 488 - 489 (2007/10/03)
Reactions of aryl alkyl ketones with methanol solution of elemental iodine and 1-fluoro-4-chloromethyl-1,4-diazonia-bicyclo[2.2.2]octane bis(tetrafluoroborate) (Selectfluor F-TEDA-BF4) result in the formation of corresponding α-iodo ketones, wh
