Month: October 2022

Hess, Stephan N.; Mo, Xiaobin; Wirtz, Conny; Fuerstner, Alois published the artcile< Total Synthesis of Limaol>, Product Details of C4H8O, the main research area is limaol total synthesis Stille asym propargylation spirocyclization.

A nonthermodynamic array of four skipped methylene substituents on the hydrophobic tail renders limaol (I), a C40-polyketide of marine origin, unique in structural terms. This conspicuous segment was assembled by a two-directional approach and finally coupled to the polyether domain by an allyl/alkenyl Stille reaction under neutral conditions. The core region itself was prepared via a 3,3′-dibromo-BINOL-catalyzed asym. propargylation, a gold-catalyzed spirocyclization, and introduction of the southern sector via substrate-controlled allylation as the key steps.

Journal of the American Chemical Society published new progress about Diastereoselective synthesis. 627-27-0 belongs to class alcohols-buliding-blocks, and the molecular formula is C4H8O, Product Details of C4H8O.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Vervandier-Fasseur, Dominique; Latruffe, Norbert published the artcile< The potential use of resveratrol for cancer prevention>, Application of C14H12O3, the main research area is review resveratrol anticancer agent cancer; approach strategies; cancer; innovative formulations; mechanisms; prevention; resveratrol.

A review. In addition to the traditional treatments of cancer and cancer prevention, the use of natural compounds, especially those found in food, should be considered. To clarify if resveratrol has the potential for cancer prevention and the possibility of use in therapy, the following must be taken into account: data from epidemiol., clin. protocol (case and control), preclin. studies (lab animals), use of established cell lines as models of cancer cells, test tube assays (enzymes activities), and requirements of nanotechnologies in order to discover new drugs to fight cancer. From this perspective and future expected advances, more information is needed such as improved efficacy, methods of application, and the synergistic sensitization of resveratrol as an adjuvant. In addition, resveratrol nanoformulation is considered to overcome its weak bioavailability.

Molecules published new progress about Antitumor agents. 501-36-0 belongs to class alcohols-buliding-blocks, and the molecular formula is C14H12O3, Application of C14H12O3.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Chaudhari, Chandan; Sato, Katsutoshi; Ogura, Yuta; Miayahara, Shin-Ichiro; Nagaoka, Katsutoshi published the artcile< Pr2O3 Supported Nano-layered Ruthenium Catalyzed Acceptorless Dehydrogenative Synthesis of 2-Substituted Quinolines and 1,8-Naphthyridines from 2-Aminoaryl Alcohols and Ketones>, Quality Control of 5344-90-1, the main research area is quinoline naphthyridine preparation; aminoaryl alc ketone dehydrogenation ruthenium nanocatalyst.

Pr2O3 supported Ru nanolayers and Ru nanoparticles catalysts were examined for the synthesis of quinolines I (R = Me, Ph, pyridin-3-yl, etc.; R1 = H, Me; RR1 = -(CH2)4-). The Ru nanolayer was most active catalyst and showed a broad substrate scope. Structure-activity relationship demonstrated that the metallic state and morphol. of Ru as well as the basic site of Pr2O3 were indispensable factors of this catalytic system.

ChemCatChem published new progress about Amino alcohols Role: RCT (Reactant), RACT (Reactant or Reagent) (aryl). 5344-90-1 belongs to class alcohols-buliding-blocks, and the molecular formula is C7H9NO, Quality Control of 5344-90-1.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Yang, Zeyu; Fu, Hengwei; Ye, Wenjie; Xie, Youyu; Liu, Qinghai; Wang, Hualei; Wei, Dongzhi published the artcile< Efficient asymmetric synthesis of chiral alcohols using high 2-propanol tolerance alcohol dehydrogenase SmADH2 via an environmentally friendly TBCR system>, Name: (R)-Butane-1,3-diol, the main research area is asym synthesis chiral alc propanol oxidation alc dehydrogenase; thermostatic bubble column reactor system alc dehydrogenase ketone reduction.

Alc. dehydrogenases (ADHs) together with the economical substrate-coupled cofactor regeneration system play a pivotal role in the asym. synthesis of chiral alcs.; however, severe challenges concerning the poor tolerance of enzymes to 2-propanol and the adverse effects of the byproduct, acetone, limit its applications, causing this strategy to lapse. Herein, a novel ADH gene smadh2 was identified from Stenotrophomonas maltophilia by traditional genome mining technol. The gene was cloned into Escherichia coli cells and then expressed to yield SmADH2. SmADH2 has a broad substrate spectrum and exhibits excellent tolerance and superb activity to 2-propanol even at 10.5 M (80%, volume/volume) concentration Moreover, a new thermostatic bubble column reactor (TBCR) system is successfully designed to alleviate the inhibition of the byproduct acetone by gas flow and continuously supplement 2-propanol. The organic waste can be simultaneously recovered for the purpose of green synthesis. In the sustainable system, structurally diverse chiral alcs. are synthesized at a high substrate loading (>150 g L-1) without adding external coenzymes. Among these, about 780 g L-1 (6 M) Et acetoacetate is completely converted into Et (R)-3-hydroxybutyrate in only 2.5 h with 99.9% ee and 7488 g L-1 d-1 space-time yield. Mol. dynamics simulation results shed light on the high catalytic activity toward the substrate. Therefore, the high 2-propanol tolerance SmADH2 with the TBCR system proves to be a potent biocatalytic strategy for the synthesis of chiral alcs. on an industrial scale.

Catalysis Science & Technology published new progress about Alcohols, chiral Role: BPN (Biosynthetic Preparation), BIOL (Biological Study), PREP (Preparation). 6290-03-5 belongs to class alcohols-buliding-blocks, and the molecular formula is C4H10O2, Name: (R)-Butane-1,3-diol.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Han, Xiaoxu; An, Hualiang; Zhao, Xinqiang; Wang, Yanji published the artcile< Influence of acid-base properties on the catalytic performance of Ni/hydroxyapatite in n-butanol Guerbet condensation>, Category: alcohols-buliding-blocks, the main research area is acid base catalytic nickel hydroxyapatite butanol Guerbet condensation.

A series of supported Ni-based multifunctional catalysts were prepared and their catalytic performances for n-butanol Guerbet condensation reaction were evaluated. Ni/hydroxyapatite (HAP) shows the best catalytic performance: a selectivity of 2-ethylhexanol reaches 52.4% at an n-butanol conversion of 29.6% at 230°C. The activity evaluation results indicate that Ni/HAP with both high-d. of acid sites and high-d. of base sites have higher catalytic performance. Furthermore, the importance of acid-base synergistic catalysis was proved by evaluating the change of the catalytic performance of Ni/HAP catalyst after poisoning the acidic or basic sites using an acid or a base probe mol.

Catalysis Communications published new progress about Catalyst poisoning. 104-76-7 belongs to class alcohols-buliding-blocks, and the molecular formula is C8H18O, Category: alcohols-buliding-blocks.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Pena-Cabia, Silvia; Royuela Vicente, Ana; Ramos Diaz, Ruth; Gutierrez Nicolas, Fernando; Penalver Vera, Angela; Siso Garcia, Isabel; Hitt Sabag, Ricardo; Garcia Lacalle, Concepcion; Pena-Cabia, Ana; Iglesias-Peinado, Irene; Garcia Diaz, Benito; Lopez-Martin, Ana published the artcile< Assessment of exposure-response relationship for bevacizumab in patients with metastatic colorectal cancer>, Recommanded Product: Calcium folinate, the main research area is human bevacizumab metastatic colorectal cancer exposure response relationship; Bevacizumab; Colorectal neoplasms; Drug monitoring; Exposure-response relationship; Treatment outcome.

Limited literature is available for bevacizumab exposure-response relationship and there is not a concentration threshold associated with an optimal disease control. This prospective observational study in patients with metastatic colorectal cancer (mCRC) aims to evaluate, in a real-life setting, the relationship between bevacizumab through concentrations at steady state (Ctrough, SS) and disease control. Ctrough, SS were drawn, coinciding with the radiol. evaluation of the response (progression or clin. benefit). Generalized estimating equations (GEE) anal. was performed. To test the association between Ctrough, SS in each patient with overall survival (OS) or progression-free survival (PFS), Cox proportional hazard models were developed. Data included 50 bevacizumab Ctrough, SS from 27 patients. The GEE model did not suggest any pos. association between bevacizumab Ctrough, SS and clin. benefit (OR 0.99, 95% CI: 0.98-1.02, p = 0.863). The Cox regression showed association between higher median Ctrough, SS with better OS (HR 0.86, 95% CI: 0.73-1.01, p = 0.060), but not with PFS. We cannot confirm a relationship between bevacizumab Ctrough, SS and clin. benefit but this is the first real-world study trying to show a relationship between bevacizumab Ctrough, SS and disease control in mCRC. It was conducted in a small sample size which reduces the level of evidence. Further controlled randomized studies with a sufficient number of patients are required.

Biomedicine & Pharmacotherapy published new progress about Body weight. 1492-18-8 belongs to class alcohols-buliding-blocks, and the molecular formula is C20H21CaN7O7, Recommanded Product: Calcium folinate.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Ahmadi, Reza; Ebrahimzadeh, Mohammad Ali published the artcile< Resveratrol - A comprehensive review of recent advances in anticancer drug design and development>, Recommanded Product: (E)-5-(4-Hydroxystyryl)benzene-1,3-diol, the main research area is review resveratrol derivative cancer drug design development; Anticancer; Antitumor; Chemotherapy; Phytoalexin; Polyphenol; Resveratrol; Stilbenoid.

A review. Resveratrol is a natural polyphenolic stilbene isolated from various plants, foods and beverages with a broad spectrum of biol. and pharmacol. properties through modulating diverse targets and signaling pathways. Particularly, it has attracted a great deal of attention as a promising and multitarget anticancer agent due to its potential use in chemoprevention and chemotherapy of various tumors. However, unfavorable pharmacokinetics/pharmacodynamics profile such as poor bioavailability restricted its applications. Therefore, medicinal chemists have synthesized a lot of novel derivatives and analogs of resveratrol using different modification strategies to overcome these limitations and improve anticancer efficacy. Herein, we reviewed the design, synthesis, structure-activity relationship and mechanism of the most potent and privileged resveratrol-based compounds that showed promising anticancer activities in the last five years. We classified these compounds into the ten different categories based on their chem. structure similarities.

European Journal of Medicinal Chemistry published new progress about Antitumor agents. 501-36-0 belongs to class alcohols-buliding-blocks, and the molecular formula is C14H12O3, Recommanded Product: (E)-5-(4-Hydroxystyryl)benzene-1,3-diol.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Yamaji-Hasegawa, Akiko; Murate, Motohide; Inaba, Takehiko; Dohmae, Naoshi; Sato, Masayuki; Fujimori, Fumihiro; Sako, Yasushi; Greimel, Peter; Kobayashi, Toshihide published the artcile< A novel sterol-binding protein reveals heterogeneous cholesterol distribution in neurite outgrowth and in late endosomes/lysosomes>, Recommanded Product: (3S,9S,10R,13R,14R,17R)-10,13-Dimethyl-17-((R)-6-methylheptan-2-yl)-2,3,4,9,10,11,12,13,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-ol, the main research area is cholesterol affinity neurite outgrowth endosome endocytosis; Endocytosis; Lipid domains; Lipid imaging; Lipid-binding protein; Membrane lipids.

We identified a mushroom-derived protein, maistero-2 that specifically binds 3-hydroxy sterol including cholesterol (Chol). Maistero-2 bound lipid mixture in Chol-dependent manner with a binding threshold of around 30%. Changing lipid composition did not significantly affect the threshold concentration EGFP-maistero-2 labeled cell surface and intracellular organelle Chol with higher sensitivity than that of well-established Chol probe, D4 fragment of perfringolysin O. EGFP-maistero-2 revealed increase of cell surface Chol during neurite outgrowth and heterogeneous Chol distribution between CD63-pos. and LAMP1-pos. late endosomes/lysosomes. The absence of strictly conserved Thr-Leu pair present in Chol-dependent cytolysins suggests a distinct Chol-binding mechanism for maistero-2.

Cellular and Molecular Life Sciences published new progress about Affinity. 434-16-2 belongs to class alcohols-buliding-blocks, and the molecular formula is C27H44O, Recommanded Product: (3S,9S,10R,13R,14R,17R)-10,13-Dimethyl-17-((R)-6-methylheptan-2-yl)-2,3,4,9,10,11,12,13,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-ol.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Verdura, Sara; Cuyas, Elisabet; Cortada, Eric; Brunet, Joan; Lopez-Bonet, Eugeni; Martin-Castillo, Begona; Bosch-Barrera, Joaquim; Encinar, Jose Antonio; Menendez, Javier A. published the artcile< Resveratrol targets PD-L1 glycosylation and dimerization to enhance antitumor T-cell immunity>, HPLC of Formula: 501-36-0 , the main research area is PD-L1; T cells; glycosylation; immunotherapy; resveratrol.

New strategies to block the immune evasion activity of programmed death ligand-1 (PD-L1) are urgently needed. When exploring the PD-L1-targeted effects of mechanistically diverse metabolism-targeting drugs, exposure to the dietary polyphenol resveratrol (RSV) revealed its differential capacity to generate a distinct PD-L1 electrophoretic migration pattern. Using biochem. assays, computer-aided docking/mol. dynamics simulations, and fluorescence microscopy, we found that RSV can operate as a direct inhibitor of glyco-PD-L1-processing enzymes (α-glucosidase/α-mannosidase) that modulate N-linked glycan decoration of PD-L1, thereby promoting the endoplasmic reticulum retention of a mannose-rich, abnormally glycosylated form of PD-L1. RSV was also predicted to interact with the inner surface of PD-L1 involved in the interaction with PD-1, almost perfectly occupying the target space of the small compound BMS-202 that binds to and induces dimerization of PD-L1. The ability of RSV to directly target PD-L1 interferes with its stability and trafficking, ultimately impeding its targeting to the cancer cell plasma membrane. Impedance-based real-time cell anal. (xCELLigence) showed that cytotoxic T-lymphocyte activity was notably exacerbated when cancer cells were previously exposed to RSV. This unforeseen immunomodulating mechanism of RSV might illuminate new approaches to restore T-cell function by targeting the PD-1/PD-L1 immunol. checkpoint with natural polyphenols.

Aging published new progress about 501-36-0 . 501-36-0 belongs to class alcohols-buliding-blocks, and the molecular formula is C14H12O3, HPLC of Formula: 501-36-0 .

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Zoetemelk, Marloes; Ramzy, George M.; Rausch, Magdalena; Koessler, Thibaud; van Beijnum, Judy R.; Weiss, Andrea; Mieville, Valentin; Piersma, Sander R.; de Haas, Richard R.; Delucinge-Vivier, Celine; Andres, Axel; Toso, Christian; Henneman, Alexander A.; Ragusa, Simone; Petrova, Tatiana V.; Docquier, Mylene; McKee, Thomas A.; Jimenez, Connie R.; Daali, Youssef; Griffioen, Arjan W.; Rubbia-Brandt, Laura; Dietrich, Pierre-Yves; Nowak-Sliwinska, Patrycja published the artcile< Optimized low-dose combinatorial drug treatment boosts selectivity and efficacy of colorectal carcinoma treatment>, Safety of Calcium folinate, the main research area is colorectal carcinoma drug treatment optimized low dose combinatorial; colorectal carcinoma; combination treatment; drug-drug interactions; drug-target interactions; phosphoproteomics; synergy.

The current standard of care for colorectal cancer (CRC) is a combination of chemotherapeutics, often supplemented with targeted biol. drugs. An urgent need exists for improved drug efficacy and minimized side effects, especially at late-stage disease. We employed the phenotypically driven therapeutically guided multidrug optimization (TGMO) technol. to identify optimized drug combinations (ODCs) in CRC. We identified low-dose synergistic and selective ODCs for a panel of six human CRC cell lines also active in heterotypic 3D co-culture models. Transcriptome sequencing and phosphoproteome analyses showed that the mechanisms of action of these ODCs converged toward MAP kinase signaling and cell cycle inhibition. Two cell-specific ODCs were translated to in vivo mouse models. The ODCs reduced tumor growth by ∼80%, outperforming standard chemotherapy (FOLFOX). No toxicity was observed for the ODCs, while significant side effects were induced in the group treated with FOLFOX therapy. Identified ODCs demonstrated significantly enhanced bioavailability of the individual components. Finally, ODCs were also active in primary cells from CRC patient tumor tissues. Taken together, we show that the TGMO technol. efficiently identifies selective and potent low-dose drug combinations, optimized regardless of tumor mutation status, outperforming conventional chemotherapy.

Molecular Oncology published new progress about Animal gene, c-kit Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 1492-18-8 belongs to class alcohols-buliding-blocks, and the molecular formula is C20H21CaN7O7, Safety of Calcium folinate.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts