115444-30-9Relevant articles and documents
Discovery of a First-in-Class Inhibitor of the Histone Methyltransferase SETD2 Suitable for Preclinical Studies
Lampe, John W.,Alford, Joshua S.,Boriak-Sjodin, P. Ann,Brach, Dorothy,Cosmopoulos, Kat,Duncan, Kenneth W.,Eckley, Sean T.,Foley, Megan A.,Harvey, Darren M.,Motwani, Vinny,Munchhof, Michael J.,Raimondi, Alejandra,Riera, Thomas V.,Tang, Cuyue,Thomenius, Michael J.,Totman, Jennifer,Farrow, Neil A.
, p. 1539 - 1545 (2021)
SET domain-containing protein 2 (SETD2), a histone methyltransferase, has been identified as a target of interest in certain hematological malignancies, including multiple myeloma. This account details the discovery of EPZ-719, a novel and potent SETD2 inhibitor with a high selectivity over other histone methyltransferases. A screening campaign of the Epizyme proprietary histone methyltransferase-biased library identified potential leads based on a 2-amidoindole core. Structure-based drug design (SBDD) and drug metabolism/pharmacokinetics (DMPK) optimization resulted in EPZ-719, an attractive tool compound for the interrogation of SETD2 biology that enables in vivo target validation studies.
Electroreductive 4-Pyridylation of Electron-deficient Alkenes with Assistance of Ni(acac)2
Findlater, Michael,Li, Guigen,Li, Lijun,Li, Xinru,Xu, Kun,Zhang, Junqi,Zhang, Sheng
, p. 3570 - 3575 (2020/04/21)
An electroreductive 4-pyridylation of activated alkenes was developed in an undivided cell with the assistance of Ni(acac)2 (acac = acetylacetone). This novel protocol is compatible with a broad range of electron-poor alkenes, which are commonl
Heteroarylboronates in rhodium-catalyzed 1,4-addition to enones
Albrecht, Fabian,Sowada, Oliver,Fistikci, Meryem,Boysen, Mike M.K.
supporting information, p. 5212 - 5215 (2014/12/11)
Rhodium(I)-catalyzed 1,4-addition of aryl and alkenylboronic acids to α,β-unsaturated carbonyl compounds is well established, but the transfer of heteroaryl residues in this reaction remains underdeveloped. We have studied heteroaryl MIDA and pinacol boro
