313515-80-9Relevant academic research and scientific papers
Synthesis, antioxidative and antiproliferative activity of methoxy amidino substituted benzamides and benzimidazoles
Cindri?, Maja,Sovi?, Irena,Martin-Kleiner, Irena,Kralj, Marijeta,Ma?ek, Tomislav,Hranjec, Marijana,Star?evi?, Kristina
, p. 2024 - 2037 (2017)
Within this manuscript the synthesis and potential antioxidative and antiproliferative activity of novel methoxy amidino substituted bezamides 6–17 and benzimidazoles 23–28 and 32–35 is presented. Their antioxidative potency has been evaluated by in vitro spectrophotometric assays and preliminary structure–activity relationships among the synthesized compounds are discussed. The compound 28 bearing three methoxy groups on a phenyl ring and imidazolinyl amidine group on benzimidazole nuclei directly attached to the phenyl ring exhibited the most prominent reducing activity as well as free-radical scavenging activity. Furthermore all novel compounds were tested against three human cell lines: HCT 116 (colon carcinoma), H 460 (lung carcinoma) and MCF-7 (breast carcinoma). The most prominent antiproliferative effect in the single-digit micromolar range was observed for compound 33 on MCF-7 (IC50 = 9 μM) cell line, comparable to the standard etoposide.
Influence of polarity on the scalability and reproducibility of solvent-free microwave-assisted reactions
Diaz-Ortiz, Ange,De La Hoz, Antonio,Alcazar, Jesus,Carrillo, Jose R.,Herrero, Maria A.,Fontana, Alberto,Munoz, Juan De M.,Prieto, Pilar,De Cozar, Abel
experimental part, p. 109 - 116 (2012/04/18)
Organic reactions performed in the absence of solvent in domestic ovens without appropriate temperature control are generally considered as not reproducible, particularly when different instruments are used. For this reason, reproducibility has historically been one of the major issues associated with Microwave-Assisted Organic Synthesis (MAOS) especially when domestic ovens are involved. The lack of reproducibility limits the general applicability and the scale up of these reactions. In this work several solvent-free reactions previously carried out in domestic ovens have been translated into a single-mode microwave reactor and then scaled up in a multimode oven. The results show that most of these reactions, although not considered as reproducible, can be easily updated and applied in microwave reactors using temperature-controlled conditions. Furthermore, computational calculations can assist to explain and/or predict whether a reaction will be reproducible or not.
