diethyl malonate
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Author(s):  
Rafat Milad Mohareb ◽  
Noha M. Asaad Bagato ◽  
Ibrahim Taha Radwan

Background: Cancer is a disease illustrated by a shift in the controlled mechanisms that control both cell proliferation and differentiation. It is regarded as a prime health problem worldwide, leading cause of human death-rate exceeded only by cardiovascular diseases. Many reported work was concerned with the discovery of new antitumor compounds this encourage us to synthesis new anticancer agents. Objective: In this work, we are aiming to synthesize target molecules from 1,3-dicarbonyl compounds through many heterocyclization reactions. Method: The reaction of either 4-methylaniline (1a) or 1-naphthylamine (1b) with diethyl malonate (2) gave the anilide derivatives 3a and 3b, respectively. The latter products underwent a series of heterocyclization reactions to give the pyridine, pyran andthiazole derivatives which confirmed with the required spectral data. Results: Thein-vitro antitumor evaluations of the newly synthesized products against four cancer cell lines MCF-7, NCI-H460, SF-268 and WI 38 as normal cell line were screened and the data revealed that compounds 11a, 18b, 18c and 20d showed high antitumor activity and 20dindividualize with potential antitumor activity towards cell lines with lowest cytotoxicity effect. Both EGFR and PIM-1 enzyme inhibition were investigated for the compound 20d and his inhibition effect was promising for each enzyme showing IC50=45.67 ng and 553.3 ng for EGFR and PIM-1, respectively. Conclusion: Molecular docking results of compound 20d showed a strong binding interactions on both enzymes, where, good binding modes obtained on case of EGFR, which closely similar to the binding mode of standard Erlotinib. While, 20d showed complete superimposition binding interactions with VRV-cocrystallized ligand of PIM-1 that may expounds the in-vitro antitumor activity.


Crystals ◽  
2021 ◽  
Vol 11 (5) ◽  
pp. 565
Author(s):  
Ahmed Gaber ◽  
Walaa F. Alsanie ◽  
Majid Alhomrani ◽  
Abdulhakeem S. Alamri ◽  
Ibrahim M. El-Deen ◽  
...  

This study aimed to synthesize quinolinone derivatives and investigate their cytotoxic activity. The compound 1-azacoumarin-3-carboxylic acid (2-oxo-1H-quinoline-3-carboxylic acid) was obtained via the cyclocondensation of 2-hydroxybenzaldehyde with diethyl malonate in base catalyst to give ethyl coumarin-3-carboxylate, followed by the ammonolysis of ester (ethyl coumarin-3-carboxylate) with ammonia in the presence of anhydrous potassium carbonate. Treatment of 2-oxo-1H-quinoline-3-carboxylic acid with acetic anhydride, cinnamaldehyde, cinnamic acid and methyl 5-phenyl-2-cyano-2,4-pentadienoate under different conditions led to the formation of 1 (substituted) aza coumarin-3-carboxylic acids (1-N-(acetyl)-azacoumarin-3-carboxylic acid 1-N-(2-Formyl-1-phenyl) vinyl-azacoumarin-3-carboxylic acids 1-N-[2-(Hydroxy) carbonyl-1-(Phenyl) vinyl]-azacoumarin-3-carboxylic acid and 1-N-(4-Cyano-5-methoxy-5-oxo-1-Phenylpenta-1,3-diene-1-y)-azacoumarin-3-carboxylic 284 acid), respectively. The structures of synthesized 1-(substituted) azacoumarin-3-carboxylic acids were confirmed based on spectroscopic methods (IR and NMR), along with elemental analyses. Interestingly compound 6 demonstrated probable impacts as an anti-cancer drug against the MCF-7 cell line. The mechanism of action was assessed using a flow cytometric assay. The outcomes revealed that compound 6 could arrest the cell cycle at G2/M phase and pre-G1 apoptosis.


Author(s):  
Alexander Harter ◽  
Thomas M. Klapötke ◽  
Christian Riedelsheimer ◽  
Jörg Stierstorfer ◽  
Michael Voggenreiter

2021 ◽  
Vol 8 ◽  
Author(s):  
Jianbo Qu ◽  
Zhi-Hao Zhang ◽  
Haitao Zhang ◽  
Zhen-Tao Weng ◽  
Jian-Yong Wang

Diethyl malonate-based fluorescent probe NE-N2H4 was constructed for monitoring hydrazine (N2H4). The novel probe NE-N2H4 exhibits good properties, such as large Stokes shift (about 125 nm), good selectivity, and low cytotoxicity. This sensing probe NE-N2H4 can be operated to detect hydrazine in living HeLa cells. Especially after soaking in probe solution, the thin-layer chromatography (TLC) plate could detect the vapor of hydrazine. Therefore, the probe NE-N2H4 might be used to monitor hydrazine in biosamples and environmental problem.


2021 ◽  
Vol 129 (7) ◽  
pp. 938
Author(s):  
Д.С. Oвеченко ◽  
А.П. Бойченко ◽  
Н.А. Яковенко

On the example of esters of carboxylic and dicarboxylic acids (ethyl acetate, diethyl oxalate, diethyl malonate, diethyl phthalate and dibutyl phthalate), as well as ketones, lactams and diketones (acetone, cyclohexanone, 4-ethylpropiophenone, acetylacetone and methylpyrrolidone) studies were carried out to generate electroluminescence (EL) in them of pure aluminum (Al) and preoxidized (Al2O3) in distilled water. The absence of EL in pure Al in ethers was revealed, and the regularities of luminescence generation in them for the oxidized metal were established. It was shown that in ketones and related compounds - lactams and diketones, the appearance of EL is possible for both states of the Al anode. In this case, the EL spectra have broad bands in the range 400 - 700 nm with maxima characteristic of the carboxyl and carbonyl groups of the electrolytes used, as well as the nanoporous structure of the formed Al2O3 and carbon-containing impurities captured by it during the growth. In some ethers and ketones, the effect of transformation of the initial structure of the oxide, as well as an increase in its thickness, was found. The absence of any changes in the chemical composition of electrolytes after anodic oxidation of Al in them or transformation of Al2O3 was established by UV, IR and NMR spectroscopy.


2021 ◽  
pp. 309-328 ◽  
Author(s):  
Samy A. El-Assaly ◽  
Abd El-Hamid A. Ismail ◽  
Hamed Abdel Bary ◽  
Mohamed G. Abouelenein

A sequence of pyrano[2, 3-c]pyrazoles was constructed through promoting an eco-friendly, green, and efficient approach. M1-M25 derivatives were developed by a base-catalyzed one-pot reaction involving application of hydrazine hydrate 96%, β-keto ester as ethyl acetoacetate or diethyl malonate, aryl/heteroaryl aldehyde or isatin, and enolizable active methylene compounds with isolation of unexpected compound M2. Further on, intramolecular cyclization of compounds M10, M13 with formic acid, acetic anhydride, and formamide leads to the corresponding pyrimidine derivatives M26-M31. Afterwards, the antimicrobial activity of the compounds was evaluated and fortunately, the vast majority of the compounds showed outstanding anti-bacterial results. Besides, the potential mode of action of the synthesized compounds was determined by employing a molecular-docking study against penicillin-binding protein implicated in anti-bacterial action. Compound M21 was one of the most promising anti-bacterial agents with potential binding affinity against the penicillin-binding protein. This study shed light on novel compounds for further antimicrobial drug development.


RSC Advances ◽  
2021 ◽  
Vol 11 (61) ◽  
pp. 38691-38693
Author(s):  
Thanat Tiyasakulchai ◽  
Netnapa Charoensetakul ◽  
Thitiphong Khamkhenshorngphanuch ◽  
Chawanee Thongpanchang ◽  
Onsiri Srikun ◽  
...  

Decagram scale synthesis of favipiravir was performed in 9 steps using diethyl malonate as cheap starting material.


2020 ◽  
Author(s):  
Michael D. Lynch

AbstractTechno-economic analysis connects R&D, engineering, and business. By linking process parameters to financial metrics, it allows researchers to understand the factors controlling the potential success of their technologies. In particular, metabolic and bioprocess engineering, as disciplines, are aimed at engineering cells to synthesize products with an ultimate goal of commercial deployment. As a result it is critical to be able to understand the potential impact of strain engineering strategies and lab scale results on commercial potential. To date, while numerous techno-economic models have been developed for a wide variety of bioprocesses, they have either required process engineering expertise to adapt and/or use or do not directly connect financial outcomes to potential strain engineering results. Despite the clear value of techno-economic analysis, these challenges have made it inaccessible to many researchers. I have developed this online calculator (https://bioprocesstea.com OR http://bioprocess-tea-calculator.herokuapp.com/) to make the basic capabilities of early-stage techno-economic analysis of bioprocesses readily accessible. The tool, currently focused on aerobic fermentation processes, can be used to understand the impact of fermentation level metrics on the commercial potential of a bioprocess for the production of a wide variety of organic molecules. Using the calculator, I review the commercially relevant targets for an aerobic bioprocess for the production of diethyl malonate.HighlightsA generalized techno-economic analysis tool for aerobic fermentation based bioprocesses.Relates strain and process improvements to projected commercial financial outcomesCommercial bioprocess targets to produce diethyl malonate are estimated to include fermentation titers >150 g/L, rates > 5g/L-hr and > 90% yield, with downstream purification yields > 90% and purification costs limited to less than 20% of total.


Molecules ◽  
2020 ◽  
Vol 25 (18) ◽  
pp. 4349 ◽  
Author(s):  
Ana-Marija Jagatić Korenika ◽  
Darko Preiner ◽  
Ivana Tomaz ◽  
Ana Jeromel

Commercial sparkling wine production represents a relatively low but important part of the Croatian wine production, especially in the Zagreb county. This study presents the results of volatile aroma compounds profile and organic acid composition of commercial sparkling wine samples from three vine-growing regions in Zagreb county. In total, 174 volatile aroma compounds were identified, separated between their chemical classes (aldehydes, higher alcohols, volatile phenols, terpenes, C13-norisoprenoids, lactones, esters, fatty acids, sulfur compounds, other compounds, other alcohols). Higher alcohols such as phenylethyl and isoamyl alcohol as well as 2-methyl-1-butanol, and esters such as diethyl succinate, ethyl hydrogensuccinate, and ethyl lactate had the strongest impact on the volatile compounds profile of Zagreb county sparkling wine. The presence of diethyl glutarate and diethyl malonate, compounds whose concentrations are influenced by yeast autolysis or caused by chemical esterification during the ageing process, was also noted. The influence of every single volatile aroma compound was evaluated by discriminant analysis using forward stepwise model. The volatile profiles of traditional sparkling wines from Croatia were presented for the first time. It is hoped the results will contribute to better understanding the quality potential and to evaluate possible differences on the bases of detected aroma concentrations and multivariate analysis.


2020 ◽  
Vol 76 (10) ◽  
pp. 1605-1610 ◽  
Author(s):  
Tharangini K. Shreekanth ◽  
Hemmige S. Yathirajan ◽  
Balakrishna Kalluraya ◽  
Sabine Foro ◽  
Christopher Glidewell

Two new substituted propanedioate esters have been synthesized using a three-component solvent-free thermal reaction between diethyl propanedioate (diethyl malonate), 5-chloro-3-methyl-1-phenyl-1H-pyrazole-4-carbaldehyde and an aryl azide, forming two new C—C bonds in a single step. The products diethyl (RS)-2-[(4-bromophenyl)(5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)methyl]propanedioate, C24H25BrN2O5 (I), and diethyl (RS)-2-[(4-chlorophenyl)(5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)methyl]propanedioate, C24H25ClN2O5 (II), are isomorphous, with Z′ = 2 in space group P21/n. The two independent molecules in compound (I) are both fully ordered, while each of the independent molecules in compound (II) is disordered, but in different ways. In one molecule of (II), the N-phenyl ring is disordered over two sets of atomic sites having occupancies 0.635 (10) and 0.365 (10), and in the other molecule the ester function is disordered over two sets of atomic sites having occupancies 0.690 (5) and 0.310 (5). In both structures, the two independent molecules adopt different conformations and, in each structure, the molecules are linked into complex sheets by a combination of N—H...O, C—H...O and C—H...π(arene) hydrogen bonds. Comparisons are made with some related structures.


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