459133-68-7Relevant articles and documents
METHODS AND COMPOUNDS FOR RESTORING MUTANT p53 FUNCTION
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Paragraph 0169, (2022/01/06)
Mutations in oncogenes and tumor suppressors contribute to the development and progression of cancer. The present disclosure describes compounds and methods that restore DNA binding affinity of p53 mutants. The compounds of the present disclosure can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA and activate downstream effectors involved in tumor suppression. The disclosed compounds can be used to reduce the progression of cancers that contain a p53 mutation.
Suzuki-type cross-coupling reaction of unprotected 3-iodoindazoles with pinacol vinyl boronate: An expeditive C-3 vinylation of indazoles under microwave irradiation
Vera, Gonzalo,Diethelm, Benjamín,Terraza, Claudio A.,Recabarren-Gajardo, Gonzalo
, (2018/09/26)
Herein we report an expeditive C-3 vinylation of unprotected 3-iodoindazoles under microwave irradiation. Ten C-5 substituted 3-vinylindazole derivatives, nine of them novel, were synthesized through this method, which proceeds in moderate to excellent yields starting from C-5 substituted 3-iodoindazole derivatives. In all cases, the C-3 vinylated derivative was the only isolated product. This methodology allows access to 3-vinylated indazoles selectively and directly without the need of N-protection. 3-Vinylindazoles could be interesting synthetic intermediates allowing access to biologically active molecules.
SUBSTITUTED BENZOFURAN COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
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, (2013/03/26)
The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
SUBSTITUTED BENZOFURAN COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
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Page/Page column 58, (2013/03/26)
The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
NOVEL COMPOUNDS THAT ARE ERK INHIBITORS
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, (2012/05/19)
Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof, wherein: A is a five membered monocyclic heteroaryl ring; and B is a monocyclic heterocycloalkyl ring, or a monocyclic heterocycloalkenyl ring, or a bridge
5-HETEROARYL SUBSTITUTED INDAZOLES AS KINASE INHIBITORS
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Page/Page column 75, (2009/01/24)
The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A, R1, R2, R3 and m, are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as Glycogen Synthase kinase 3 (GSK-3), Rho kinase (ROCK), Janus Kinases (JAK), AKT, PAK4, PLK, CK2, KDR, MK2, JNK1, aurora, pim 1 and nek 2.
Sonogashira cross-coupling reaction of 3-iodoindazoles with various terminal alkynes: A mild and flexible strategy to design 2-aza tryptamines
Arnautu, Anca,Collot, Valérie,Ros, Javier Calvo,Alayrac, Carole,Witulski, Bernhard,Rault, Sylvain
, p. 2695 - 2697 (2007/10/03)
This paper describes a Sonogashira-type cross-coupling reaction of 3-iodoindazoles with various terminal alkynes as a general route to 3-alkynylindazoles. The coupling reaction is illustrated by the preparation of new indazolylpropiolic or propargylic derivatives. Scope and limitation of the method are outlined.
