1001003-44-6Relevant articles and documents
Sodium Chloride Catalyzed Regioselective Trifluoromethylthiolation of Furans
Ernst, Johannes B.,Rakers, Lena,Glorius, Frank
, p. 260 - 268 (2017)
Here, we report the catalytic trifluoromethylthiolation of furans employing sodium chloride as an inexpensive, abundant and ecologically friendly catalyst. The developed method exhibits perfect regioselectivity and a high functional group tolerance. Furth
Suzuki-Miyaura Cross-Couplings under Acidic Conditions
Freese, Tyll,Kahnert, Sean-Ray,Lücke, Ana-Luiza,Mummel, Sebastian,Pruschinski, Lucas,Schmidt, Andreas
, p. 882 - 892 (2020)
Suzuki-Miyaura reactions with Pd(PPh 3) 4 have been carried out using lithium N -phenylsydnone-4-carboxylate as additive, which gave best yields at pH 5.7 in a mixture of acetic acid, water, and sodium carbonate. Reaction parameters such as the Pd source, the solvent, reaction time and temperature, acid, base and carboxylate have been varied and some representative examples of the Suzuki-Miyaura reaction have been examined.
Identification of Piperidine-3-carboxamide Derivatives Inducing Senescence-like Phenotype with Antimelanoma Activities
Oh, Sangmi,Kwon, Do Yoon,Choi, Inhee,Kim, Young Mi,Lee, Ji Young,Ryu, Jiyoung,Jeong, Hangyeol,Kim, Myung Jin,Song, Rita
, p. 563 - 571 (2021/05/06)
This study evaluated the potential use of senescence-inducing small molecules in the treatment of melanoma. We screened commercially available small-molecule libraries with high-throughput screening and high-content screening image-based technology. Our findings showed an initial hit with the embedded N-arylpiperidine-3-carboxamide scaffold-induced senescence-like phenotypic changes in human melanoma A375 cells without serious cytotoxicity against normal cells. A focused library containing diversely modified analogues were constructed and examined to evaluate the structure-activity relationship of N-arylpiperidine-3-carboxamide derivatives starting from hit 1. This work identified a novel compound with remarkable antiproliferative activity in vitro and demonstrated the key structural moieties within.
σ-Bond initiated generation of aryl radicals from aryl diazonium salts
Chan, Bun,McErlean, Christopher S. P.,Nashar, Philippe E.,Tatunashvili, Elene
supporting information, p. 1812 - 1819 (2020/03/17)
σ-Bond nucleophiles and molecular oxygen transform aryl diazonium salts into aryl radicals. Experimental and computational studies show that Hantzsch esters transfer hydride to aryl diazonium species, and that oxygen initiates radical fragmentation of the diazene intermediate to produce aryl radicals. The operational simplicity of this addition-fragmentation process for the generation of aryl radicals, by a polar-radical crossover mechanism, has been illustrated in a variety of bond-forming reactions.
Design and synthesis of boronic acid inhibitors of endothelial lipase
O'Connell, Daniel P.,Leblanc, Daniel F.,Cromley, Debra,Billheimer, Jeffrey,Rader, Daniel J.,Bachovchin, William W.
scheme or table, p. 1397 - 1401 (2012/03/26)
Endothelial lipase (EL) and lipoprotein lipase (LPL) are homologous lipases that act on plasma lipoproteins. EL is predominantly a phospholipase and appears to be a key regulator of plasma HDL-C. LPL is mainly a triglyceride lipase regulating (V)LDL levels. The existing biological data indicate that inhibitors selective for EL over LPL should have anti-atherogenic activity, mainly through increasing plasma HDL-C levels. We report here the synthesis of alkyl, aryl, or acyl-substituted phenylboronic acids that inhibit EL. Many of the inhibitors evaluated proved to be nearly equally potent against both EL and LPL, but several exhibited moderate to good selectivity for EL.
NEW COMPOUNDS
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Page/Page column 49-50, (2008/06/13)
The present invention encompasses compounds of general formula (1) wherein X and R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a pharmaceutical composition having the above-mentioned properties.