Tag: M.W=250-300

Simsek, Rahime; Safak, Cihat; Erol, Kevser; Ataman, Sule; Ulgen, Mert; Linden, Anthony published the artcile< Synthesis, evaluation of the calcium antagonistic activity and biotransformation of hexahydroquinoline and furoquinoline derivatives>, Application In Synthesis of 112-63-0, the main research area is calcium antagonist hexahydroquinoline furoquinoline structure activity.

The objective of this study was to synthesize new condensed 1,4-dihydropyridine derivatives and investigate their calcium channel blocking activity. In addition, the in vitro hepatic microsomal biotransformation of one hexahydroquinoline derivative was studied. 2,6,6-Trimethyl-3-carbmethoxy(carbethoxy)-4-aryl-5-oxo-1,4,5,6,7,8-hexahydroquinoline derivatives were synthesized by modified Hantzsch synthesis and 1,3,4,5,6,7,8,9-octahydro-7,7-dimethyl-9-arylfuro[3,4-b]quinoline-1,8-dione derivatives were synthesized the reaction of hexahydroquinoline derivatives with pyridinium bromide perbromide. The calcium antagonistic activities of the compounds were determined by tests performed on isolated rat ileum and lamb carotid artery. In vitro hepatic biotransformation of one compound was studied in rat microsomes. Some of these compounds showed high tissue selectivity compared with nicardipine. In the hexahydroquinoline series, the compounds having ortho substituted Ph substituent were more active than the meta isomers. Lactone derivatives were found less active than hexahydroquinoline derivatives in respect to calcium antagonistic activity.

Arzneimittel-Forschung published new progress about Calcium channel blockers. 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

Zheng, Litong; Ma, Wenfang; Deng, Jiahui; Peng, Yunjing; Tian, Rui; Yuan, Yangyang; Li, Baiyun; Ma, Fengwang; Li, Mingjun; Ma, Baiquan published the artcile< A MdMa13 gene encoding tonoplast P3B-type ATPase regulates organic acid accumulation in apple>, Recommanded Product: (9Z,12Z)-Methyl octadeca-9,12-dienoate, the main research area is apple gene encoding tonoplast ATPase organic acid accumulation.

The organic acid content is one of the important factors that determine fruit quality. In this study, one gene encoding a P3B-ATPase (designated as MdMa13) was identified as a determinant of fruit acidity in apple. Subcellular localization indicated that MdMa13 was located in the tonoplast. Overexpression of MdMa13 in apple calli, tomato or apples led to increased malic acid contents. In the transgenic apple calli, the expression levels of seven acid-related genes were higher than that in the wild-type apple calli, including MdMa1, MdtDT, MdDTC1, MdDTC2, MdVHA-A3, MdVHA-D, and MdMa11. The expression level of MdMa10 was lower in transgenic lines than that in wild-type apple calli. Together, these findings implied that MdMa13 has important functions related to apple fruit acidity. The results of this study will strengthen the characterization for the complex mol. regulation of fruit acidity.

Scientia Horticulturae (Amsterdam, Netherlands) published new progress about Acidity. 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

Halland, Nis; Schmidt, Friedemann; Weiss, Tilo; Saas, Joachim; Li, Ziyu; Czech, Joerg; Dreyer, Matthias; Hofmeister, Armin; Mertsch, Katharina; Dietz, Uwe; Struebing, Carsten; Nazare, Marc published the artcile< Discovery of N-[4-(1H-Pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides as Highly Active and Selective SGK1 Inhibitors>, SDS of cas: 112-63-0, the main research area is pyrazolopyrazinyl sulfonamide preparation SGK kinase inhibitor; AGC kinase; Serum glucocorticoid regulated kinase; WNT signaling; virtual screening.

From a virtual screening starting point, inhibitors of the serum and glucocorticoid regulated kinase 1 were developed through a combination of classical medicinal chem. and library approaches. This resulted in highly active small mols., e.g. I, with nanomolar activity and a good overall in vitro and ADME profile. Furthermore, the compounds exhibited unusually high kinase and off-target selectivity due to their rigid structure.

ACS Medicinal Chemistry Letters published new progress about Homo sapiens. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, SDS of cas: 112-63-0.

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

Metts, Jonathan; Harrington, Brittany; Salman, Emad; Bradfield, Scott M; Flanary, Jennifer; Mosha, Maua; Amankwah, Ernest; Stapleton, Stacie published the artcile< A phase I study of irinotecan and temozolomide with bevacizumab in children with recurrent/refractory central nervous system tumors.>, COA of Formula: C19H34O2, the main research area is Bevacizumab; Brain tumor; Irinotecan; Pediatric; Phase I; Temozolomide.

PURPOSE: Children with relapsed/refractory central nervous system (CNS) tumors require novel combinations of therapies. Irinotecan and temozolomide (IT) is a frequently used therapy with an established toxicity profile. Bevacizumab is an anti-VEGF monoclonal antibody with demonstrated activity in CNS tumors. Therefore, the combination of these agents has therapeutic potential in CNS tumors. The objective of this study was to determine the maximum tolerated dose (MTD) of escalating dose IT combined with a fixed dose of bevacizumab (BIT) in children with relapsed/refractory CNS tumors. METHODS: A phase I trial was performed in a 3 + 3 design. Therapy toxicities and radiologic responses to treatment were described. RESULTS: One hundred eighty cycles of therapy were administered to 26 patients. The MTD of BIT was dose level 1, (bevacizumab 10 mg/kg on days 1 and 15, irinotecan 125 mg/m2 on days 1 and 15, and temozolomide 125 mg/m2 on days 1-5 of 28-day cycles). The regimen was well tolerated with primarily hematologic toxicity, which was not dose limiting. Among 22 response-evaluable patients, there was 1 complete response (CR), 6 partial responses (PR), and 10 stable diseases (SD) with an overall response rate (ORR: CR + PR) of 31.8%. CONCLUSION: At the MTD, BIT therapy was well tolerated, and prolonged treatment courses of up to 24 cycles were feasible, with radiographic responses observed. Further evaluation is needed for efficacy in a phase II trial (NCT00876993, registered April 7, 2009, www. CLINICALTRIALS: gov ).

Child’s nervous system : ChNS : official journal of the International Society for Pediatric Neurosurgery published new progress about 112-63-0. 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, Xiaoqing; Zhu, Shanhui; Dong, Mei; Wang, Jianguo; Fan, Weibin published the artcile< Ru/CeO2 catalyst with optimized CeO2 morphology and surface facet for efficient hydrogenation of ethyl levulinate to γ-valerolactone>, Computed Properties of 112-63-0, the main research area is ruthenium ceria catalyst surface facet ethyl levulinate hydrogenation valerolactone.

Three Ru/CeO2 catalysts with different CeO2 morphol. (nanorod, nanocube and nano-octahedra) mainly exposed (1 1 0) + (1 0 0), (1 0 0) and (1 1 1) facets for hydrogenation of biomass-derived Et levulinate (EL) to valuable γ-valerolactone (GVL). Ru/CeO2-rod with exposed (1 1 0) crystal plane obtained the highest GVL yield (99.4%) and best productivity (13140 h-1). The surface facets of CeO2 supports not only affect the chem. states of Ru species but also tune the concentration of oxygen vacancy in Ru-CeO2 interface. The concentration of oxygen vacancy shows a linear relationship with GVL production rate. DFT calculations indicate that the lactonization of CH3CHOCH2CH2CO* to produce GVL is the rate-determining step in EL hydrogenation, and Ru10/CeO2 (1 1 0) with more oxygen vacancy has low activation energy barrier, compared to Ru10/CeO2 (1 0 0) and Ru10/CeO2 (1 1 1).

Journal of Catalysis published new progress about Adsorption. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Computed Properties of 112-63-0.

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

Kandeepan, C.; Sabitha, M.; Parvathi, K.; Senthilkumar, N.; Ramya, S.; Boopathi, N. M.; Jayakumararaj, R. published the artcile< Phytochemical screening, GCMS profile, and in-silico properties of bioactive compounds in methanolic leaf extracts of Moringa oleifera>, Category: esters-buliding-blocks, the main research area is Moringa leaf methanol phytochem screening.

Plant Based Natural Products (PBNPs) have been subject of interest since ancient time due to their use in food, industrial and biomedical applications. Research attention has further augmented to explore their phytochem. composition, properties, and potential application in the post-COVID era. In the present study phytochem. screening has been carried out with Methanolic Leaf Extracts of Moringa oleifera (MLEMO) followed by Gas Chromatog.-Mass Spectrometry (GCMS) anal. Phytochem. anal. of MLEMO revealed the presence of Alkaloids, Carbohydrates, Coumarins, Flavonoids, Glycosides, Phenol, Proteins, Quinones, Saponins, Steroids, Tannins and Terpenoids. Further, GCMS anal. revealed the presence of 41 compounds of which Dihydroxyacetone; Monomethyl malonate; 4H-Pyran-4-one,2,3-dihydro3,5-dihydroxy-6-methyl; 1,3-Propanediol, 2-ethyl-2-(hydroxymethyl); Propanoic acid, 2- methyl-, octyl ester; 3-Deoxy-d-mannoic lactone; Sorbitol; Inositol; Cyclohexanemethanol, alpha-methyl-4-(1-methylethyl), Hexadecanoic acid, Me palmitate; n-Hexadecanoic acid (Palmitic acid); 9-Octadecenoic acid, Me ester; Phytol; 9,12,15-Octadecatrienoic acid; Octadecanoic acid; 9-Octadecenamide were prominent. Most of the compounds in the list are bioactive and possess medicinal properties that are expected to serve as a baseline lead for the development of therapeutic agents.

Journal of Drug Delivery and Therapeutics published new progress about Alkaloids Role: ANT (Analyte), BSU (Biological Study, Unclassified), PRP (Properties), THU (Therapeutic Use), ANST (Analytical Study), BIOL (Biological Study), USES (Uses). 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

Garcia, Catherine R.; Myint, Zin W.; Jayswal, Rani; Wang, Chi; Morgan, Rachael M.; Butts, Allison R.; Weiss, Heidi L.; Villano, John L. published the artcile< Hematological adverse events in the management of glioblastoma>, Name: (9Z,12Z)-Methyl octadeca-9,12-dienoate, the main research area is hematol adverse event management glioblastoma; Bevacizumab; Glioblastoma; Hematologic adverse events; Management; Outcomes; Temozolomide.

Hematol. adverse events (HAEs) are common during treatment for glioblastoma (GBM), usually associated with temozolomide (TMZ). Their clin. value is uncertain, as few investigations have focused on outcomes for HAEs during GBM treatment. We combined data from two randomized clin. trials, RTOG 0525 and RTOG 0825, to analyze HAEs during treatment for GBM. We investigated differences between chemoradiation and adjuvant therapy, and by regimen received during adjuvant treatment. 1454 Patients participated in these trials, of which 1154 (79.4%) developed HAEs. During chemoradiation, 44.4% of patients developed HAEs (54% involving more than one cell line), and were most commonly lymphopenia (50.6%), and thrombocytopenia (47.5%). During adjuvant treatment, 45% of patients presented HAEs (78.6% involving more than one cell line), and were more commonly leukopenia (62.7%), and thrombocytopenia (62.3%). Median overall survival (OS) and progression free survival (PFS) were longer in patients with HAEs (OS 19.4 mo and PFS 9.9 mo) compared to those with other or no adverse events (OS 14.1 mo and PFS 5.9 mo). There was no significant difference in survival between grade 1 and/or 2 vs. grade 3 and/or 4 HAEs. History of HAEs during chemoradiation was a protective factor for presentation of HAEs during adjuvant therapy. HAEs are common during GBM treatment, and often involve more than one cell line (more likely during adjuvant therapy). HAEs may be associated with prolonged OS and PFS, particularly during adjuvant therapy. HAEs during chemoradiation was a protective factor for HAEs during adjuvant therapy.

Journal of Neuro-Oncology published new progress about Age groups. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Name: (9Z,12Z)-Methyl octadeca-9,12-dienoate.

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

Collett, Christopher J.; Young, Claire M.; Massey, Richard S.; O’Donoghue, AnnMarie C.; Smith, Andrew D. published the artcile< Kinetic and Structure-Activity Studies of the Triazolium Ion- Catalyzed Intramolecular Stetter Reaction>, Reference of 112-63-0, the main research area is ethyl formylphenoxy butenoate heterocyclic carbene Stetter reaction mechanism kinetics.

Mechanistic studies of the triazolium ion-catalyzed intramol. Stetter reaction using initial rates anal. in NEt3/NEt3 · HCl buffered methanol showed the reaction to be first-order in catalyst and zero-order in aldehyde over a broad range of aldehyde concentrations The observed reaction rate is higher for catalysts bearing N-aryl substituents with electron-withdrawing groups. A concurrent, NHC-independent substrate isomerization was also observed and found to demonstrate a first-order dependence on aldehyde concentration The reported data are consistent with deprotonation to form the Breslow intermediate being turnover-limiting in this process.

European Journal of Organic Chemistry published new progress about Cis-trans isomerization. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Reference of 112-63-0.

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

Makida, Yusuke; Saita, Masahiro; Kuramoto, Takahiro; Ishizuka, Kentaro; Kuwano, Ryoichi published the artcile< Asymmetric Hydrogenation of Azaindoles: Chemo- and Enantioselective Reduction of Fused Aromatic Ring Systems Consisting of Two Heteroarenes>, Name: (9Z,12Z)-Methyl octadeca-9,12-dienoate, the main research area is enantioselective hydrogenation azaindole ruthenium phosphine catalyst; asymmetric catalysis; azaindoles; chemoselectivity; hydrogenation; ruthenium.

High enantioselectivity was achieved for the hydrogenation of azaindoles by using the chiral catalyst, which was prepared from [Ru(η3-methallyl)2(cod)] and a trans-chelating bis(phosphine) ligand (PhTRAP). The dearomative reaction exclusively occurred on the five-membered ring, thus giving the corresponding azaindolines with up to 97:3 enantiomer ratio.

Angewandte Chemie, International Edition published new progress about Enantioselective synthesis. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Name: (9Z,12Z)-Methyl octadeca-9,12-dienoate.

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

Choi-Sledeski, Yong Mi; Kearney, Robert; Poli, Gregory; Pauls, Henry; Gardner, Charles; Gong, Yong; Becker, Michael; Davis, Roderick; Spada, Alfred; Liang, Guyan; Chu, Valeria; Brown, Karen; Collussi, Dennis; Leadley, Robert Jr.; Rebello, Sam; Moxey, Phillip; Morgan, Suzanne; Bentley, Ross; Kasiewski, Charles; Maignan, Sebastien; Guilloteau, Jean-Pierre; Mikol, Vincent published the artcile< Discovery of an orally efficacious inhibitor of coagulation factor Xa which incorporates a neutral P1 ligand>, Category: esters-buliding-blocks, the main research area is ketopiperazino methylazaindole factor Xa inhibitor structure thrombolytic.

The discovery and SAR of ketopiperazino methylazaindole factor Xa inhibitors are described. Structure-activity data suggesting that this class of inhibitors does not bind in the canonical mode were confirmed by an X-ray crystal structure showing the neutral haloarom. bound in the S1 subsite. The most potent azaindole (I, RPR209685) is selective against related serine proteases and attains higher levels of exposure upon oral dosing than comparable benzamidines and benzamidine isosteres. Compound I was efficacious in the canine AV model of thrombosis.

Journal of Medicinal Chemistry published new progress about Crystal structure. 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