34628-36-9Relevant academic research and scientific papers
The Castagnoli–Cushman reaction of bicyclic pyrrole dicarboxylic anhydrides bearing electron-withdrawing substituents
Chizhova, Maria E.,Dar'in, Dmitry V.,Krasavin, Mikhail
, p. 496 - 497 (2020/08/07)
Four anhydrides of 1-(carboxymethyl)pyrrole-2-carboxylic acids bearing electron-withdrawing substituents at positions 6 or 7 of the bicyclic system have been investigated in the Castagnoli–Cushman reaction with imines. 6-Benzoyl- and 7-sulfamoyl-substitut
Identification of a novel orally bioavailable ERK5 inhibitor with selectivity over p38α and BRD4
Myers, Stephanie M.,Miller, Duncan C.,Molyneux, Lauren,Arasta, Mercedes,Bawn, Ruth H.,Blackburn, Timothy J.,Cook, Simon J.,Edwards, Noel,Endicott, Jane A.,Golding, Bernard T.,Griffin, Roger J.,Hammonds, Tim,Hardcastle, Ian R.,Harnor, Suzannah J.,Heptinstall, Amy B.,Lochhead, Pamela A.,Martin, Mathew P.,Martin, Nick C.,Newell, David R.,Owen, Paul J.,Pang, Leon C.,Reuillon, Tristan,Rigoreau, Laurent J.M.,Thomas, Huw D.,Tucker, Julie A.,Wang, Lan-Zhen,Wong, Ai-Ching,Noble, Martin E.M.,Wedge, Stephen R.,Cano, Celine
, p. 530 - 543 (2019/06/19)
Extracellular regulated kinase 5 (ERK5) signalling has been implicated in driving a number of cellular phenotypes including endothelial cell angiogenesis and tumour cell motility. Novel ERK5 inhibitors were identified using high throughput screening, with
High-Throughput Screening and Hit Validation of Extracellular-Related Kinase 5 (ERK5) Inhibitors
Myers, Stephanie M.,Bawn, Ruth H.,Bisset, Louise C.,Blackburn, Timothy J.,Cottyn, Betty,Molyneux, Lauren,Wong, Ai-Ching,Cano, Celine,Clegg, William,Harrington, Ross. W.,Leung, Hing,Rigoreau, Laurent,Vidot, Sandrine,Golding, Bernard T.,Griffin, Roger J.,Hammonds, Tim,Newell, David R.,Hardcastle, Ian R.
supporting information, p. 444 - 455 (2016/08/16)
The extracellular-related kinase 5 (ERK5) is a promising target for cancer therapy. A high-throughput screen was developed for ERK5, based on the IMAP FP progressive binding system, and used to identify hits from a library of 57-617 compounds. Four distinct chemical series were evident within the screening hits. Resynthesis and reassay of the hits demonstrated that one series did not return active compounds, whereas three series returned active hits. Structure-activity studies demonstrated that the 4-benzoylpyrrole-2-carboxamide pharmacophore had excellent potential for further development. The minimum kinase binding pharmacophore was identified, and key examples demonstrated good selectivity for ERK5 over p38α kinase.
Nano-copper catalysed highly regioselective synthesis of 2,4-disubstituted pyrroles from terminal alkynes and isocyanides
Tiwari, Dipak Kumar,Pogula, Jaya,Sridhar,Tiwari, Dharmendra Kumar,Likhar, Pravin R.
, p. 13646 - 13649 (2015/09/02)
Nano-copper(0) stabilized on alumina prepared from Cu-Al hydrotalcite has been reported for completely regioselective synthesis of 2,4-disubstituted pyrroles from unactivated terminal aromatic/aliphatic alkynes and isocyanides. The reaction is operational
Modular preparation of diverse dipyrrolemethanes
Pham, Cindy C.,Park, Michelle H.,Pham, Jenny Y.,Martin, Sadie G.,Schramm, Michael P.
, p. 1165 - 1173 (2013/06/05)
A modular synthesis of polyfunctional dipyrrolemethanes is presented. Diverse side chains are introduced to 2-carboxypyrrole building blocks in two to four steps, resulting in a collection of substituted pyrroles that, when condensed in one step, give ris
