Category: 112-63-0

Garcia da Silva, Artur Christian; Rodrigues, Bruna dos Santos; Andrade, Wanessa Machado; Marques dos Santos, Thais Rosa; de Carvalho, Flavio Silva; Sanz, German; Vaz, Boniek G.; Liao, Luciano M.; Menegatti, Ricardo; Valadares, Marize Campos published the artcile< Antiangiogenic and antitumoral activity of LQFM126 prototype against B16F10 melanoma cells>, COA of Formula: C19H34O2, the main research area is Nutlin analog antiangiogenic antitumoral agent melanoma cell; Antitumor drugs; Apoptosis; LQFM126; Melanoma; Molecular simplification; Nutlins.

Inhibition of mouse double minute 2 homolog (MDM2)-p53 interaction and reactivation of p53 signaling have been explored as effective anticancer therapeutic strategy. The potent and specific antitumor activity shown by Nutlins, first class of MDM2-p53 inhibitors discovered, has made these compounds potential antitumor candidates. To this end, we synthesized Nutlin-1 and Nutlin-2 analogs through mol. simplification and selected the compound with the most efficient antitumoral activity. Cytotoxicity of Nutlin-2 analog LQFM126 on B16F10 melanoma cells induced intense cytoplasmic vacuolization, reduction of cell size, chromatin condensation, cytoplasmic degeneration and nuclear fragmentation. LQFM126 antiproliferative effects mediated cell cycle retention in G0/G1 phase and increased the levels of cell cycle regulatory proteins p21 and p27. This Nutlin analog increased mitochondrial membrane potential, activated caspase-8, -9 and -3/7 and reduced VEGF levels in B16F10 cells. Therefore, LQFM126 promoted alterations suggestive of apoptosis, G0/G1 cell cycle arrest and suppression of angiogenesis through modulation of VEGF expression in B16F10 cells. Addnl., LQFM126 was classified as UN GHS category 4 (LD50 > 300-2000 mg/kg), suggesting it has low acute systemic toxicity. LQFM126 can be a promising prototype for anticancer therapy.

Chemico-Biological Interactions published new progress about Angiogenesis. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, COA of Formula: C19H34O2.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Gao, Xing; Shan, Chunhui; Chen, Zhihao; Liu, Yan; Zhao, Xia; Zhang, Ao; Yu, Peng; Galons, Herve; Lan, Yu; Lu, Kui published the artcile< One-pot synthesis of β-lactams by the Ugi and Michael addition cascade reaction>, Application In Synthesis of 112-63-0, the main research area is lactam beta preparation chemoselective diastereoselective; heterocyclic aldehyde amine isocyanide maleic fumaric acid; tandem Ugi Michael addition.

Synthesis of β-lactams I (R1 = COOMe, COOEt; R2 = n-Pr, 4-MeC6H4, 4-O2NC6H4, 4-ClC6H4; R3 = COOEt, COPh, 2-pyridyl, etc.; R4 = n-Bu, t-Bu, c-hexyl, Bn) was achieved via Ugi/Michael reaction cascades under mild conditions. The intramol. hydrogen bonding between the heteroatom from an aldehyde component and the amide NH group controls the chemoselectivity of the Michael reaction vs. the aza-Michael reaction. DFT calculation was performed to clarify the mechanism, chemo-selectivity and diastereoselectivity of this work. This one-pot protocol offers a straightforward method to build a diversified β-lactam library for drug discovery.

Organic & Biomolecular Chemistry published new progress about Aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Application In Synthesis of 112-63-0.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Huang, Long; Wei, Yin; Shi, Min published the artcile< Asymmetric substitutions of O-Boc-protected Morita-Baylis-Hillman adducts with pyrrole and indole derivatives>, Safety of (9Z,12Z)-Methyl octadeca-9,12-dienoate, the main research area is Boc Morita Baylis Hillman adduct pyrrole indole asym substitution.

An efficient asym. substitution process of O-Boc-protected Morita-Baylis-Hillman adducts with various pyrrole and indole derivatives has been developed in the presence of (DHQD)2PYR in THF, affording the corresponding products, e.g. I, in good to high yields (up to 99% yield) and moderate to high ee values (up to 92 and 96% ee) under mild conditions.

Organic & Biomolecular Chemistry published new progress about Enantioselective synthesis. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Safety of (9Z,12Z)-Methyl octadeca-9,12-dienoate.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Palomba, Martina; Sancineto, Luca; Marini, Francesca; Santi, Claudio; Bagnoli, Luana published the artcile< A domino approach to pyrazino-indoles and -pyrroles using vinyl selenones>, Category: esters-buliding-blocks, the main research area is indolecarboxamide pyrrolocarboxamide chemoselective regioselective Michael reaction cyclization vinyl selenone; pyrazinoindolone dihydro preparation; pyrrolopyrazinone dihydro preparation.

An efficient and flexible approach to biol. relevant 3,4-dihydropyrazino[1,2-a]indol-1(2H)ones I [R1 = H, F, Cl, MeO, R2 = H; R1 = R2 = MeO; R3 = n-Bu, Ph, PhCH2, (R)-PhCHMe, etc.; R4 = H, Me, n-Bu, n-hexyl] and 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)ones through a domino Michael/intramol. nucleophilic substitution pathway using potassium hydroxide in dichloromethane is disclosed. Variously substituted vinyl selenones R4CH:CHSeO2Ph and 1H-indole-2-carboxamides II or 1H-pyrrole-2-carboxamides were employed with success in chemo- and regioselective processes. The introduction of an amino acid portion on the amidic function is well tolerated without racemization.

Tetrahedron published new progress about Aromatic amides Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Category: esters-buliding-blocks.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Yao, Tianwen; Su, Wenxiang; Han, Shisheng; Lu, Yan; Xu, Yanqiu; Chen, Min; Wang, Yi published the artcile< Recent advances in traditional Chinese medicine for treatment of podocyte injury>, COA of Formula: C19H34O2, the main research area is review podocyte injury traditional Chinese medicine treatment; active ingredient; acupuncture and moxibustion; compound prescription; herbs; podocyte injury; traditional Chinese medicine.

A review. Podocyte is also called glomerular epithelial cell, which has been considered as the final gatekeeper of glomerular filtration barrier (GFB). As a major contributor to proteinuria, podocyte injury underlies a variety of glomerular diseases and becomes the challenge to patients and their families in general. At present, the therapeutic methods of podocyte injury mainly include angiotensin-converting enzyme inhibitors or angiotensin receptor blockers, steroid and immunosuppressive medications. Nevertheless, the higher cost and side effects seriously disturb patients with podocyte injury. Promisingly, traditional Chinese medicine (TCM) has received an increasing amount of attention from different countries in the treatment of podocyte injury by invigorating spleen and kidney, clearing heat and eliminating dampness, as well enriching qi and activating blood. Therefore, we searched articles published in peer-reviewed English-language journals through Google Scholar, PubMed, Web of Science, and Science Direct. The protective effects of active ingredients, herbs, compound prescriptions, acupuncture and moxibustion for treatment of podocyte injury were further summarized and analyzed. Meanwhile, we discussed feasible directions for future development, and analyzed existing deficiencies and shortcomings of TCM in the treatment of podocyte injury. In conclusion, this paper shows that TCM treatments can serve as promising auxiliary therapeutic methods for the treatment of podocyte injury.

Frontiers in Pharmacology published new progress about Abelmoschus manihot. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, COA of Formula: C19H34O2.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Pratika, Remi Ayu; Wijaya, Karna; Trisunaryanti, Wega published the artcile< Hydrothermal treatment of SO4/TiO2 and TiO2/CaO as heterogeneous catalysts for the conversion of Jatropha oil into biodiesel>, Safety of (9Z,12Z)-Methyl octadeca-9,12-dienoate, the main research area is titania sulfur calcium oxide catalyst hydrothermal treatment Jatrophaoil biodiesel.

The conversion of Jatropha oil into biodiesel has been conducted using the SO4/TiO2 acid and TiO2/CaO base catalysts via hydrothermal treatment using an autoclave reactor. The acid catalyst was prepared with the sulfation process of TiO2 using H2SO4 (0.5; 0.8; 1.1; 1.4; 1.7 and 2 M). The base catalyst was initiated by dispersing TiO2 (1, 5, 10, 15, and 20 wt%) on CaO. The aims of this research were to obtain the catalyst with the highest acidity and basicity from SO4/TiO2 acid and TiO2/CaO catalysts, resp. Afterward, apply them to the esterification to reduce the free fatty acid of Jatropha oil and the transesterification of the esterified of Jatropha oil into biodiesel. Among the SO4/TiO2 catalysts, the ST-2-400 catalyst exhibits an optimum total acidity of 6.93 mmol NH3/g. This catalyst was able to reduce the FFA level of Jatropha oil from 1.22% to 0.59% with catalyst weight of 3%, ratio oil to methanol of 1:15, and reaction time of 90 min. The optimum total basicity from TiO2/CaO catalysts was achieved by TC-20-800 with the total basicity of 28.67 mmol HCl/g. The conversion of esterified Jatropha oil into biodiesel was performed using 3% of TC-20-800 catalyst at 65°C for 90 min. The TC-20-800 catalyst was able to produce biodiesel up to 79.68%.

Journal of Environmental Chemical Engineering published new progress about Acid number. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Safety of (9Z,12Z)-Methyl octadeca-9,12-dienoate.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Tran-Thi, T.-H.; Prayer, C.; Millie, Ph.; Uznanski, P.; Hynes, James T. published the artcile< Substituent and Solvent Effects on the Nature of the Transitions of Pyrenol and Pyranine. Identification of an Intermediate in the Excited-State Proton-Transfer Reaction>, Product Details of C19H34O2, the main research area is solvent effect electronic transition pyrenol pyranine intermediate proton transfer; substituent effect electronic transition pyrenol pyranine intermediate proton transfer.

A comparative study of pyrenol and its trisulfonated derivative, pyranine, is undertaken to provide new clues for the understanding of the excited-state proton-transfer reaction (ESPT) of hydroxyarenes (ArOH*). A particular goal is to elucidate the nature of a transient intermediate involved in a three step mechanism of ESPT, as recently revealed in a dynamical study of excited pyranine in water. The present focus is on the reactant side, before the proton transfer occurs, and particular attention is given to the anal. of the nature of the electronic transitions and to the solute-solvent interactions in the ground and excited states of the ArOHs. Using both quantum chem. calculations and solvatochromism analyses, both (a) the role of electron-withdrawing substituents and H-bond interaction with the solvent in stabilizing the two lowest excited states, 1Lb and 1La, and (b) their relevance to the inversion of these two states are studied. The results allow the identification of the intermediate species in the three step mechanism of the ESPT of excited pyranine in water as a 1La state acid form, with appreciable charge-transfer character, as distinct from the 1Lb acid form reached in absorption. The results, which differ from more standard pictures of ESPT, are discussed within the perspective of a three valence bond form model for the ESPT process.

Journal of Physical Chemistry A published new progress about AM1 (molecular orbital method). 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Product Details of C19H34O2.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Sheppard, George S.; Wang, Jieyi; Kawai, Megumi; Fidanze, Steve D.; BaMaung, Nwe Y.; Erickson, Scott A.; Barnes, David M.; Tedrow, Jason S.; Kolaczkowski, Lawrence; Vasudevan, Anil; Park, David C.; Wang, Gary T.; Sanders, William J.; Mantei, Robert A.; Palazzo, Fabio; Tucker-Garcia, Lora; Lou, Pingping; Zhang, Qian; Park, Chang H.; Kim, Ki H.; Petros, Andrew; Olejniczak, Edward; Nettesheim, David; Hajduk, Phillip; Henkin, Jack; Lesniewski, Richard; Davidsen, Steven K.; Bell, Randy L. published the artcile< Discovery and Optimization of Anthranilic Acid Sulfonamides as Inhibitors of Methionine Aminopeptidase-2: A Structural Basis for the Reduction of Albumin Binding>, COA of Formula: C19H34O2, the main research area is anthranilic acid sulfonamide derivative preparation methionine aminopeptidase inhibitor albumin.

Methionine aminopeptidase-2 (MetAP2) is a novel target for cancer therapy. As part of an effort to discover orally active reversible inhibitors of MetAP2, a series of anthranilic acid sulfonamides with micromolar affinities for human MetAP2 were identified using affinity selection by mass spectrometry (ASMS) screening. These micromolar hits were rapidly improved to nanomolar leads on the basis of insights from protein crystallog.; however, the compounds displayed extensive binding to human serum albumin and had limited activity in cellular assays. Modifications based on structural information on the binding of lead compounds to both MetAP2 and domain III of albumin allowed the identification of compounds with significant improvements in both parameters, which showed good cellular activity in both proliferation and methionine processing assays.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, COA of Formula: C19H34O2.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

McDonald, Ivar M.; Mate, Robert; Ng, Alicia; Park, Hyunsoo; Olson, Richard E. published the artcile< Novel tricyclic diamines 2. Synthesis of 1,7-diazaisoadamantane, 1,5-diazaisoadamantane and 1,6-diazahomobrendane>, Quality Control of 112-63-0, the main research area is azaisoadamantane synthesis azaindole; azahomobrendane synthesis azaindole; azaindole synthesis tandem Sonogashira coupling intramol cyclization.

Three novel tricyclic diamines (1,7-diazaisoadamantane, 1,5-diazaisoadamantane and 1,6-diazahomobrendane) were prepared (isoadamantane and homobrendane numbering systems are shown as I and II, resp.). A flexible synthetic strategy was employed which used flat, aromatic azaindoles as the starting materials. The requisite azaindoles were prepared by a tandem Sonogashira coupling/intramol. cyclization reaction. Ring saturation, appropriate functionalization and intramol. alkylation provided the three novel tricyclic diamines cores.

Tetrahedron Letters published new progress about Chromatographic chiral resolution (of diazaisoadamantane precursors). 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Quality Control of 112-63-0.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Kaku, Tomohiro; Tsujimoto, Saori; Matsunaga, Nobuyuki; Tanaka, Toshimasa; Hara, Takahito; Yamaoka, Masuo; Kusaka, Masami; Tasaka, Akihiro published the artcile< 17,20-Lyase inhibitors. Part 3: Design, synthesis, and structure-activity relationships of biphenylylmethylimidazole derivatives as novel 17,20-lyase inhibitors>, Recommanded Product: (9Z,12Z)-Methyl octadeca-9,12-dienoate, the main research area is prostate cancer lyase inhibitor biphenylylmethylimidazole preparation SAR.

A novel series of biphenylylmethylimidazole derivatives and related compounds were synthesized as inhibitors of 17,20-lyase, a key enzyme in the production of steroid hormones, and their biol. activities were evaluated. In an attempt to identify potent and selective inhibitors of 17,20-lyase over the related CYP3A4 enzyme, a homol. model for human 17,20-lyase was developed using the X-ray crystallog. structure of the mammalian CYP2C5 enzyme. With the aid of mol. modeling, optimization of the biphenyl moiety was performed to give an acetamide derivative, which was resolved by HPLC to give the active (-)-enantiomer. The obtained active enantiomer showed not only potent inhibition of both rat and human 17,20-lyase,with IC50 values of 14 and 26 nM, resp., but also excellent selectivity (>300-fold) for inhibition of 17,20-lyase over CYP3A4. Moreover, the active enantiomer significantly reduced both serum testosterone and DHEA concentrations in a monkey model after single oral administration. Asym. synthesis of the active enantiomer was also developed via a chiral intermediate using a diastereoselective Grignard reaction.

Bioorganic & Medicinal Chemistry published new progress about Diastereoselective synthesis. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Recommanded Product: (9Z,12Z)-Methyl octadeca-9,12-dienoate.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics