313273-62-0Relevant articles and documents
Acid-activated carbon materials: Cheaper alternative catalysts for the synthesis of substituted quinolines
Lopez-Sanz, Jesus,Perez-Mayoral, Elena,Soriano, Elena,Omenat-Moran, Delia,Duran, Carlos J.,Martin-Aranda, Rosa Maria,Matos, Ines,Fonseca, Isabel
, p. 3736 - 3742 (2013)
We describe the first examples of Friedlaender reactions efficiently catalyzed by carbon materials. We report herein a series of acidic activated carbon materials, which can be considered as an environmentally friendly, cheaper alternative to the traditional acidic mesoporous silicates or even zeolites for the synthesis of quinolines/quinolones. Textural parameters of the acidic activated carbon materials together with their acidic properties are important factors that affect the reaction selectivity. Some mechanistic details have been addressed by computational calculations. Freeloading on the Friedlaender: Acidic microporous activated carbon materials containing sulfonic acid groups can be considered environmentally friendly and cheaper catalytic alternatives for the Friedlaender reaction compared to traditional acidic solids such as zeolites or even mesoporous silicates. The textural characteristics of the most efficient materials determine the parameters for the conversion and selectivity of the reaction. Copyright
Synthetic Lethality in Pancreatic Cancer: Discovery of a New RAD51-BRCA2 Small Molecule Disruptor That Inhibits Homologous Recombination and Synergizes with Olaparib
Bagnolini, Greta,Milano, Domenico,Manerba, Marcella,Schipani, Fabrizio,Ortega, Jose Antonio,Gioia, Dario,Falchi, Federico,Balboni, Andrea,Farabegoli, Fulvia,De Franco, Francesca,Robertson, Janet,Pellicciari, Roberto,Pallavicini, Isabella,Peri, Sebastiano,Minucci, Saverio,Girotto, Stefania,Di Stefano, Giuseppina,Roberti, Marinella,Cavalli, Andrea
, p. 2588 - 2619 (2020/03/05)
Synthetic lethality is an innovative framework for discovering novel anticancer drug candidates. One example is the use of PARP inhibitors (PARPi) in oncology patients with BRCA mutations. Here, we exploit a new paradigm based on the possibility of triggering synthetic lethality using only small organic molecules (dubbed "fully small-molecule-induced synthetic lethality"). We exploited this paradigm to target pancreatic cancer, one of the major unmet needs in oncology. We discovered a dihydroquinolone pyrazoline-based molecule (35d) that disrupts the RAD51-BRCA2 protein-protein interaction, thus mimicking the effect of BRCA2 mutation. 35d inhibits the homologous recombination in a human pancreatic adenocarcinoma cell line. In addition, it synergizes with olaparib (a PARPi) to trigger synthetic lethality. This strategy aims to widen the use of PARPi in BRCA-competent and olaparib-resistant cancers, making fully small-molecule-induced synthetic lethality an innovative approach toward unmet oncological needs.
Friedl?nder annulation: Scope and limitations of metal salt Lewis acid catalysts in selectivity control for the synthesis of functionalised quinolines
Tanwar, Babita,Kumar, Dinesh,Kumar, Asim,Ansari, Md. Imam,Qadri, Mohammad Mohsin,Vaja, Maulikkumar D.,Singh, Madhulika,Chakraborti, Asit K.
, p. 9824 - 9833 (2015/12/01)
The scope and limitations of metal salt Lewis acid catalysts were examined for the selectivity control for the formation of Friedl?nder and non-Friedl?nder products during the reaction involving 2-aminobenzophenone and ethyl acetoacetate. Among a pool of
