606102-24-3Relevant articles and documents
Thienopyrrole amide derivative and application of thienopyrrole amide derivative in antitumor drugs
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Paragraph 0012; 0018-0021, (2021/10/27)
The invention belongs to the technical field of medicinal chemistry, and particularly relates to a thienopyrrole amide derivative and a preparation method thereof, and application of the thienopyrrole amide derivative as an MEK inhibitor in antitumor drugs. The invention provides a thienopyrrole amide derivative as shown in a general formula, and a geometric isomer or pharmaceutically acceptable salt, hydrate, solvate or prodrug thereof. The MEK inhibitor has specificity and effectiveness, and has a wider development prospect. Experimental results show that the thienopyrrole amide derivative synthesized by the research group has a prospect of developing targeted antitumor drugs.
Thieno[3,2-b]pyrrole-5-carboxamides as New Reversible Inhibitors of Histone Lysine Demethylase KDM1A/LSD1. Part 1: High-Throughput Screening and Preliminary Exploration
Sartori, Luca,Mercurio, Ciro,Amigoni, Federica,Cappa, Anna,Fagá, Giovanni,Fattori, Raimondo,Legnaghi, Elena,Ciossani, Giuseppe,Mattevi, Andrea,Meroni, Giuseppe,Moretti, Loris,Cecatiello, Valentina,Pasqualato, Sebastiano,Romussi, Alessia,Thaler, Florian,Trifiró, Paolo,Villa, Manuela,Vultaggio, Stefania,Botrugno, Oronza A.,Dessanti, Paola,Minucci, Saverio,Zagarrí, Elisa,Carettoni, Daniele,Iuzzolino, Lucia,Varasi, Mario,Vianello, Paola
, p. 1673 - 1692 (2017/03/17)
Lysine specific demethylase 1 KDM1A (LSD1) regulates histone methylation and it is increasingly recognized as a potential therapeutic target in oncology. We report on a high-throughput screening campaign performed on KDM1A/CoREST, using a time-resolved fluorescence resonance energy transfer (TR-FRET) technology, to identify reversible inhibitors. The screening led to 115 hits for which we determined biochemical IC50, thus identifying four chemical series. After data analysis, we have prioritized the chemical series of N-phenyl-4H-thieno[3, 2-b]pyrrole-5-carboxamide for which we obtained X-ray structures of the most potent hit (compound 19, IC50 = 2.9 μM) in complex with the enzyme. Initial expansion of this chemical class, both modifying core structure and decorating benzamide moiety, was directed toward the definition of the moieties responsible for the interaction with the enzyme. Preliminary optimization led to compound 90, which inhibited the enzyme with a submicromolar IC50 (0.162 μM), capable of inhibiting the target in cells.
MODULATORS OF LIPID STORAGE
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Paragraph 00114; 00115; 0208, (2013/06/06)
Disclosed are compounds of formulas I, II, and III: Formulas I, II, and III wherein R1-R19 and n are as described herein, or pharmaceutically acceptable salts thereof, or an enantiomer thereof or a conjugate thereof wherein the conju