Author: Jessica.F

Shueng, Pei-Wei; Chan, Hui-Wen; Lin, Wei-Chan; Kuo, Deng-Yu; Chuang, Hui-Yen published the artcile< Orlistat Resensitizes Sorafenib-Resistance in Hepatocellular Carcinoma Cells through Modulating Metabolism>, Application In Synthesis of 96829-58-2, the main research area is fatty acid synthase; hepatocellular carcinoma; metabolism; sorafenib resistance.

Sorafenib is one of the options for advanced hepatocellular carcinoma treatment and has been shown to extend median overall survival. However, sorafenib resistance often develops a few months after treatment. Hence, developing various strategies to overcome sorafenib resistance and understand the possible mechanisms is urgently needed. We first established sorafenib-resistant hepatocellular carcinoma (HCC) cells. Then, we found that sorafenib-resistant Huh7 cells (Huh7/SR) exhibit higher glucose uptakes and express elevated fatty acid synthesis and glucose metabolism-related proteins than their parental counterparts (Huh7). The current study investigated whether sorafenib resistance could be reversed by suppressing fatty acid synthesis, using a fatty acid synthase (FASN) inhibitor, orlistat, in HCC cells. FASN inhibition-caused changes in protein expressions and cell cycle distribution were analyzed by Western blot and flow cytometry, and changes in glucose uptakes were also evaluated by 18F-FDG uptake. Orlistat remarkably enhanced the cytotoxicity of sorafenib in both Huh7 and Huh7/SR cells, and flow cytometry showed that combination treatment significantly increased the sub-G1 population in both cell lines. Western blot revealed that the combination treatment effectively increased the ratio of Bax/Bcl-2 and decreased expressions of pERK; addnl., the combination treatment also strongly suppressed fatty acid synthesis-related proteins (e.g., FASN and SCD) in both cell lines. Lastly, the 18F-FDG uptake was repressed by the combination treatment in both cell lines. Our results indicated that orlistat-mediated FASN inhibition could overcome sorafenib resistance and enhance cell killing in HCC by changing cell metabolism

International Journal of Molecular Sciences published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Application In Synthesis of 96829-58-2.

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

Wang, Lei; Riel, Louis P.; Bajrami, Bekim; Deng, Bin; Howell, Amy R.; Yao, Xudong published the artcile< α-Methylene-β-Lactone Scaffold for Developing Chemical Probes at the Two Ends of the Selectivity Spectrum>, Computed Properties of 96829-58-2, the main research area is chemical proteomics; glutathione S-transferase; methylenelactone; orlistat; parthenolide.

The utilities of an α-methylene-β-lactone (MeLac) moiety as a warhead composed of multiple electrophilic sites are reported. We demonstrate that a MeLac-alkyne not only reacts with diverse proteins as a broadly reactive measurement probe, but also recruits reduced endogenous glutathione (GSH) to assemble a selective chemical probe of GSH-β-lactone (GSH-Lac)-alkyne in live cells. Tandem mass spectrometry reveals that MeLac reacts with nucleophilic cysteine, serine, lysine, threonine, and tyrosine residues, through either Michael or acyl addition. A peptide-centric proteomics platform demonstrates that the proteomic selectivity profiles of orlistat and parthenolide, which have distinct reactivities, are measurable by MeLac-alkyne as a high-coverage probe. The GSH-Lac-alkyne selectively probes the glutathione S-transferase P responsible for multidrug resistance. The assembly of the GSH-Lac probe exemplifies a modular and scalable route to develop selective probes with different recognizing moieties.

ChemBioChem published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Computed Properties of 96829-58-2.

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

Cope, Rebecca J.; Fischetti, Briann S.; Kavanagh, Rebecca K.; Lepa, Trisha M.; Sorbera, Maria A. published the artcile< Safety and Efficacy of Weight-Loss Pharmacotherapy in Persons Living with HIV: A Review of the Literature and Potential Drug-Drug Interactions with Antiretroviral Therapy>, Application In Synthesis of 96829-58-2, the main research area is review immunodeficiency virus pharmacotherapy weight loss; HIV; antiretroviral; drug-drug interaction; obesity; weight loss.

A review. The prevalence of obesity among persons living with human immunodeficiency virus (HIV) has increased significantly and may be linked to the use of antiretroviral therapy. Although weight-loss medications approved by the U.S. Food and Drug Administration are recommended as an adjunct to diet and exercise to treat obesity in the general population, little is known about the safety and efficacy of these drugs specifically in persons living with HIV. We review the available evidence regarding the effective use of weight-loss pharmacotherapy in persons living with HIV and its potential to interact with antiretroviral therapy. Persons living with HIV are frequently not reported or included in clin. trials for weight-loss medications; however, treatment efficacy is likely similar to the general population. Several important reported or theor. drug-drug interactions exist between antiobesity pharmacotherapy and antiretroviral therapy. Orlistat is a weight-loss drug available in the United States without a prescription and was linked to HIV viral rebound in several case reports. Clinicians should be aware of the potential for loss of HIV viremia control when certain weight-loss pharmacotherapies are used in combination with antiretrovirals.

Pharmacotherapy published new progress about Antiobesity agents. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Application In Synthesis of 96829-58-2.

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

Hou, Hongcen; Zhao, Yongli; Sheng, Shouri; Chen, Junmin published the artcile< Iridium-Catalyzed ortho-C-H Amidation of Benzenesulfonamides with Sulfonyl Azides>, Safety of o-Chlorobenzenesulfonamide, the main research area is aminobenzesulfonamide preparation regioselective; benzenesulfonamide sulfonyl azide amidation iridium catalyst.

An iridium-catalyzed direct C-H activation/C-N bond formation reaction of benzenesulfonamides RS(O)2NHR1 (R = Ph, 2-methyl-4-fluorophenyl, 3-chlorophenyl, etc.) with sulfonyl azides R2C6H4S(O)2N3 (R2 = H, 4-Me, 2-Me, 4-OMe) was developed. The amidation reaction provides a protocol for the synthesis of 2-aminobenzenesulfonamides I (R3 = H, 2-Me-4-F, 3-Cl, 4-Ph, etc.) in good to excellent yields. This strategy features a wide substrate scope, tolerates a broad range of functional groups under external oxidant-free conditions and only releases mol. nitrogen as the sole byproduct. Moreover, the preliminary mechanism was investigated and the proposed reaction pathway was provided.

Advanced Synthesis & Catalysis published new progress about Amidation (C-H, regioselective). 6961-82-6 belongs to class amides-buliding-blocks, and the molecular formula is C6H6ClNO2S, Safety of o-Chlorobenzenesulfonamide.

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

Suvada, Kara; Plantinga, Laura; Vaughan, Camille P.; Markland, Alayne D.; Mirk, Anna; Burgio, Kathryn L.; Erni, Susanne M.; Ali, Mohammed K.; Okosun, Ike; Young, Henry; Goode, Patricia S.; Johnson, Theodore M. published the artcile< Comorbidities, Age, and Polypharmacy Limit the Use by US Older Adults with Nocturia of the Only FDA-approved Drugs for the Symptom>, Related Products of 94-20-2, the main research area is nocturia desmopressin acetate comorbidity polypharmacy aging United States; aged or elderly; comorbidity; medications; polypharmacy; risk factors; safety.

The goal of this study was to determine if the US adult population with nocturia (waking from sleep at night to void) can easily take medications (desmopressin acetate) approved by the US Food and Drug Administration for nocturia. Using a cross-sectional anal. of four US National Health and Nutrition Examination Survey (NHANES) waves (2005-2012), a total of 4111 participants aged ≥50 years who reported ≥2 nightly episodes of nocturia were identified. The main outcome was frequency of contraindications and drug interactions as described in US Food and Drug Administration-approved prescribing information. Desmopressin prescribing concerns were present in 80.5% (95% CI, 78.0-82.9) of those ≥50 years of age with nocturia; 50.0% (95% CI, 47.0-53.0) had contraindications, and 41.6% (95% CI, 39.3-44.0) took a concomitant drug that could increase risk of low serum sodium. Desmopressin contraindications were higher with older age (P < 0.001) and present in 73.2% (95% CI, 69.3-77.1) of those ≥80 years of age. This study showed that older US adults with nocturia have a high prevalence of medical conditions, concomitant medications, and baseline laboratory abnormalities that likely increase the risk of potentially severe adverse side effects from desmopressin use. A medication designed and approved for a clin. symptom that is most common in older adults could not be taken by most of the older adults with the symptom. Clinical Therapeutics published new progress about 5-HT reuptake inhibitors. 94-20-2 belongs to class amides-buliding-blocks, and the molecular formula is C10H13ClN2O3S, Related Products of 94-20-2.

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

Venkateswarlu, Somepalli; Satyanarayana, Meka; Murthy, Gandrothu Narasimha; Siddaiah, Vidavalur published the artcile< Cyclisation of 2-(2-aminophenyl)quinazolin-4(3H)-one reexamined: formation of isomeric angular fused quinazolinoquinazolinones and their spectroscopic identification>, Reference of 5004-88-6, the main research area is aminophenylquinazolinone acetic anhydride cyclization; isomeric angular fused quinazolinoquinazolinone preparation IR NMR.

Cyclization of 2-(2-aminophenyl)quinazolin-4(3H)-ones on N3 and on N1 leading to 6-alkyl-(8H)-quinazolino[4,3-b]quinazolin-8-ones and 6-alkyl-(13H)-quinazolino[3,4-a]quinazolin-13-ones, resp. was described for the first time. The differences in the IR and carbon NMR data of these isomeric fused quinazolinoquinazolinones afford a useful method for distinguishing between the two series.

Tetrahedron Letters published new progress about Anhydrides Role: RCT (Reactant), RACT (Reactant or Reagent). 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, Reference of 5004-88-6.

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

Chen, Jun; Shi, Zhan; Lu, Ping published the artcile< Enantioselective Synthesis of Indanes with a Quaternary Stereocenter via Diastereoselective C(sp3)-H Functionalization>, Electric Literature of 1192620-83-9, the main research area is bromofluorodihydroindenol enantioselective preparation crystal structure; chiral bromobenzoyldihydroindene enantioselective preparation crystal structure; mol structure chiral bromobenzoyldihydroindene bromofluorodihydroindenol; indane enantioselective preparation; indanone preparation diastereoselective carbon hydrogen bond activation reaction.

A practical synthesis of enantioenriched indane derivatives with quaternary stereocenters was developed via sequential enantioselective reduction and C-H functionalization. Good to excellent enantioselectivity could be achieved by either the CuH-catalyzed asym. reduction or the Corey-Bakshi-Shibata (CBS) reduction of indanone derivatives The subsequent diastereospecific and regioselective Rh-catalyzed silylation of the Me C-H bond led to indane derivatives with quaternary centers. This strategy was further applied in syntheses of (nor)illudalane and botryane sesquiterpenoids.

Organic Letters published new progress about C-H bond activation. 1192620-83-9 belongs to class amides-buliding-blocks, and the molecular formula is C30H31ClN2O2RuS, Electric Literature of 1192620-83-9.

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

Wang, Yu-Wei; Zheng, Lei; Jia, Feng-Cheng; Chen, Yun-Feng; Wu, An-Xin published the artcile< Oxidative ring-opening of isatins for the synthesis of 2-aminobenzamides and 2-aminobenzoates>, Recommanded Product: 2-Amino-4-bromobenzamide, the main research area is aminobenzamide aminobenzoate preparation; isatin alc ammonia tandem oxidative ring opening.

An efficient and practical isatin-based oxidative domino protocol has been developed for the facile synthesis of 2-aminobenzamides and 2-aminobenzoates. The robust nature of this reaction system is reflected by accessible starting materials, room temperature and high-yield gram-scale synthesis.

Tetrahedron published new progress about Aromatic esters Role: SPN (Synthetic Preparation), PREP (Preparation). 112253-70-0 belongs to class amides-buliding-blocks, and the molecular formula is C7H7BrN2O, Recommanded Product: 2-Amino-4-bromobenzamide.

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

Shcherbakova, I. published the artcile< Product subclass 2: arenesulfonic acid derivatives>, HPLC of Formula: 1524-40-9, the main research area is review arenesulfonic acid derivative preparation organic synthesis.

A review of methods to prepare arenesulfonic acid derivatives

Science of Synthesis published new progress about Arenesulfonic acids Role: SPN (Synthetic Preparation), PREP (Preparation). 1524-40-9 belongs to class amides-buliding-blocks, and the molecular formula is C6H6FNO2S, HPLC of Formula: 1524-40-9.

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

Liu, Yi-Chun; Nguyen, Phung-Anh; Humayun, Ayesha; Chien, Shuo-Chen; Yang, Hsuan-Chia; Asdary, Rahma Novita; Syed-Abdul, Shabbir; Hsu, Min-Huei; Moldovan, Max; Yen, Yun; Li, Yu-Chuan; Jian, Wen-Shan; Iqbal, Usman published the artcile< Does long-term use of antidiabetic drugs changes cancer risk?>, Synthetic Route of 94-20-2, the main research area is pioglitazone anticancer agent liver lung cancer.

Antidiabetic medications are commonly used around the world, but their safety is still unclear. The aim of this study was to investigate whether long-term use of insulin and oral antidiabetic medications is associated with cancer risk.We conducted a well-designed case-control study using 12 years of data from Taiwans National Health Insurance Research Database and investigated the association between antidiabetic medication use and cancer risk over 20 years. We identified 42,500 patients diagnosed with cancer and calculated each patients exposure to antidiabetic drugs during the study period. We matched cancer and noncancer subjects matched 1:6 by age, gender, and index date, and used Cox proportional hazard regression and conditional logistic regression, adjusted for potential confounding factors, i.e., medications and comorbid diseases that could influence cancer risk during study period.Pioglitazone (adjusted odds ratio [AOR], 1.20; 95% confidence interval [CI], 1.05-1.38); and insulin and its analogs for injection, intermediate or long acting combined with fast acting (AOR, 1.22; 95% CI, 1.05-1.43) were significantly associated with a higher cancer risk. However, metformin (AOR, 1.00; 95% CI, 0.93-1.07), glibenclamide (AOR, 0.98; 95% CI, 0.92-1.05), acarbose (AOR, 1.06; 95% CI, 0.96-1.16), and others do not show evidence of association with cancer risk. Moreover, the risk for specific cancers among antidiabetic users as compared with nonantidiabetic medication users was significantly increased for pancreas cancer (by 45%), liver cancer (by 32%), and lung cancer (by 18%).Antidiabetic drugs do not seem to be associated with an increased cancer risk incidence except for pioglitazone, insulin and its analogs for injection, intermediate or long acting combined with fast acting.

Medicine (Philadelphia, PA, United States) published new progress about Antidiabetic agents. 94-20-2 belongs to class amides-buliding-blocks, and the molecular formula is C10H13ClN2O3S, Synthetic Route of 94-20-2.

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