Results 81 to 90 of about 13,855 (240)
ChemMedChem, EarlyView.Two PROTAC‐based degraders targeting the cancer‐associated transcriptional co‐activators CBP/p300 weredeveloped. These degraders, combining the CBP/p300 inhibitor C646 with the CRBN ligand thalidomide, reduced CBP/p300 levels in lymphoma cells at low‐micromolar concentration.
Francesco Fiorentino +9 more
wiley +1 more source
Synthesis and Smo Activity of Some Novel Benzamide Derivatives
Molecules, 2017 Two series of benzamides compounds bearing piperidine groups were synthesized and the Gli-luc luciferase activity was screened by Gys-luc luciferase gene detection method. Compound 5q showed promising inhibition of hedgehog (Hh) signaling pathway.
Huaiwei Ding +8 more
doaj +1 more source
ChemMedChem, EarlyView.This study introduced DCAF11 as an E3 ligase for PROTAC‐mediated histone deacetylase (HDAC) degradation. By replacing cereblon with DCAF11 as recruited E3 ligase, a selective HDAC6 degrader (A6) was transformed into pan‐HDAC degraders. The lead compound, 1j (FF2039), potently degraded HDACs from classes I, IIa, and IIb, showing strong antiproliferative
Felix Feller +5 more
wiley +1 more source
ChemMedChem, EarlyView.By N‐methylation, the intramolecular lactam formation in carborane‐substituted diclofenac analogs is prevented, yielding a series of open‐chain derivatives alongside with their phenyl analogs exhibiting anticancer activity and thus offering a promising avenue for future drug development. This study explores the anticancer potential of N‐methylated open‐
Christoph Selg +12 more
wiley +1 more source
Benzamide-4-Sulfonamides Are Effective Human Carbonic Anhydrase I, II, VII, and IX Inhibitors
Metabolites, 2018 A series of benzamides incorporating 4-sulfamoyl moieties were obtained by reacting 4-sulfamoyl benzoic acid with primary and secondary amines and amino acids. These sulfonamides were investigated as inhibitors of the metalloenzyme carbonic anhydrase (CA,
Morteza Abdoli +3 more
doaj +1 more source
Mechanochemical Generation of Active Pd/BippyPhos Catalyst for Efficient CN Cross‐Coupling in Air
ChemSusChem, EarlyView.A solvent‐free, solid‐state Buchwald–Hartwig amination is developed using [Pd(π‐cinnamyl)Cl]2 and bulky electron‐rich phosphines. The active catalyst forms without solvent or inert atmosphere, as confirmed by solid‐state 31P nuclear magnetic resonance.
Deniz Karabiyikli +7 more
wiley +1 more source
Reactivity of an ortho‐Phenylene‐bridged Al/P Frustrated Lewis Pair Towards Small Molecules
European Journal of Inorganic Chemistry, Accepted Article.Frustrated Lewis Pairs (FLPs) as ambiphilic molecules are prone to activate small molecules and are in the focus of interest for many years. In this paper, we present the first ortho‐phenylene bridged Al/P‐based FLP with only one phosphine moiety. The title compound was employed in various reactions with small molecules featuring different functional ...
Melina E. A. Dilanas, Frank Breher
wiley +1 more source
European Journal of Organic Chemistry, EarlyView.This review highlights recent advancements in the deconstructive transformation of unstrained cyclic amines, with a particular focus on the C−N bond cleavage of pyrrolidines. Various methodologies, including von Braun‐type, oxidative, and reductive approaches, facilitate the synthesis of diverse amines and the expansion of chemical space.
Eisuke Ota, Junichiro Yamaguchi
wiley +1 more source
Ars PharmaceuticaA series of 4-(2-(4-substituted phenyl)-4-oxoquinazolin-3(4H)-yl)-N-(2-(4-fluorophenyl)-4-oxo-5-(arylidene)thiazolidin-3-yl) benzamides (VIa-n) have been synthesized by condensation of N-(2-(4-fluorophenyl)-4-oxothiazolidin-3-yl)-4-(4-oxo-2-(4 ...
Sukanya Nara, Achaiah Garlapati
doaj +1 more source
Substituted Benzamides Containing Azaspiro Rings as Upregulators of Apolipoprotein A-I Transcription
Molecules, 2012 Apolipoprotein A-I (Apo A-I) is the principal protein component of high density lipoprotein (HDL), which is generally considered as a potential therapeutic target against atherosclerosis.
Bin Hong +7 more
doaj +1 more source