Month: September 2021

Authors Toth, S; Szepesi, A; Tran-Nguyen, VK; Sarkadi, B; Nemet, K; Falson, P; Di Pietro, A; Szakacs, G; Boumendjel, A in MDPI published article about COLLATERAL SENSITIVITY; CANCER; THIOSEMICARBAZONES; AURONES in [Toth, Szilard; Szepesi, Aron; Sarkadi, Balazs; Nemet, Katalin; Szakacs, Gergely] Hungarian Acad Sci, Res Ctr Nat Sci, Inst Enzymol, H-1117 Budapest, Hungary; [Tran-Nguyen, Viet-Khoa; Boumendjel, Ahcene] Univ Grenoble Alpes, Dept Pharmacochim Mol, UMR 5063, F-38041 Grenoble, France; [Nemet, Katalin] Creat Cell Ltd, H-1119 Budapest, Hungary; [Falson, Pierre; Di Pietro, Attilio] Univ Lyon, CNRS UMR 5086, Mol Microbiol & Struct Biochem Lab, Drug Resistance & Membrane Prot Grp,IBCP, 7 Passage Vercors, F-69367 Lyon, France; [Szakacs, Gergely] Med Univ Vienna, Inst Canc Res, Borschkegasse 8A, A-1090 Vienna, Austria in 2020, Cited 30. COA of Formula: C15H12O. The Name is Chalcone. Through research, I have a further understanding and discovery of 94-41-7

The resistance of tumors against anticancer drugs is a major impediment for chemotherapy. Tumors often develop multidrug resistance as a result of the cellular efflux of chemotherapeutic agents by ABC transporters such as P-glycoprotein (ABCB1/P-gp), Multidrug Resistance Protein 1 (ABCC1/MRP1), or Breast Cancer Resistance Protein (ABCG2/BCRP). By screening a chemolibrary comprising 140 compounds, we identified a set of naturally occurring aurones inducing higher cytotoxicity against P-gp-overexpressing multidrug-resistant (MDR) cells versus sensitive (parental, non-P-gp-overexpressing) cells. Follow-up studies conducted with the P-gp inhibitor tariquidar indicated that the MDR-selective toxicity of azaaurones is not mediated by P-gp. Azaaurone analogs possessing pronounced effects were then designed and synthesized. The knowledge gained from structure-activity relationships will pave the way for the design of a new class of anticancer drugs selectively targeting multidrug-resistant cancer cells.

About Chalcone, If you have any questions, you can contact Toth, S; Szepesi, A; Tran-Nguyen, VK; Sarkadi, B; Nemet, K; Falson, P; Di Pietro, A; Szakacs, G; Boumendjel, A or concate me.. Application In Synthesis of Chalcone

Reference:
Thiazolidine – Wikipedia,
,Thiazolidine – ScienceDirect.com

Authors Sochacka-Cwikla, A; Regiec, A; Zimecki, M; Artym, J; Zaczynska, E; Kocieba, M; Kochanowska, I; Bryndal, I; Pyra, A; Maczynski, M in MDPI published article about 5-AMINO-3-METHYL-4-ISOXAZOLECARBOXYLIC ACID HYDRAZIDE; IMMUNE-RESPONSE; ACTIVATION; INHIBITORS; PARALLEL; KINASES; JNK in [Sochacka-Cwikla, Aleksandra; Regiec, Andrzej; Maczynski, Marcin] Wroclaw Med Univ, Dept Organ Chem, Fac Pharm, 211A Borowska St, PL-50556 Wroclaw, Poland; [Zimecki, Michal; Artym, Jolanta; Zaczynska, Ewa; Kocieba, Maja; Kochanowska, Iwona] Polish Acad Sci, Dept Expt Therapy, Inst Immunol & Expt Therapy, 12 Rudolf Weigl St, PL-53114 Wroclaw, Poland; [Bryndal, Iwona] Wroclaw Med Univ, Dept Drug Technol, Fac Pharm, 211A Borowska St, PL-50556 Wroclaw, Poland; [Pyra, Anna] Univ Wroclaw, Fac Chem, 14 Joliot Curie, PL-50383 Wroclaw, Poland in 2020.0, Cited 51.0. Quality Control of 1,1,1-Triethoxyethane. The Name is 1,1,1-Triethoxyethane. Through research, I have a further understanding and discovery of 78-39-7

The synthesis of a series of novel 7-aminooxazolo[5,4-d]pyrimidines5, transformations during their synthesis and their physicochemical characteristics have been described. Complete detailed spectral analysis of the intermediates2-4, theN ‘-cyanooxazolylacetamidine by-products7and final compounds5has been carried out using MS, IR, 1D and 2D NMR spectroscopy. Theoretical research was carried out to explain the privileged formation of 7-aminooxazolo[5,4-d]pyrimidines in relation to the possibility of their isomer formation and the related thermodynamic aspects. Additionally, the single-crystal X-ray diffraction analysis for5hwas reported. Ten 7-aminooxazolo[5,4-d]pyrimidines5(SCM1-10) were biologically tested in vitro to preliminarily evaluate their immunological, antiviral and anticancer activity. CompoundsSCM5andSCM9showed the best immunoregulatory profile. The compounds displayed low-toxicity and strongly inhibited phytohemagglutinin A-induced proliferation of human peripheral blood lymphocytes and lipopolysaccharide-induced proliferation of mouse splenocytes. CompoundSCM9caused also a moderate suppression of tumor necrosis factor alpha (TNF-alpha) production in a human whole blood culture. Of note, the compounds also inhibited the growth of selected tumor cell lines and inhibited replication of human herpes virus type-1 (HHV-1) virus in A-549 cell line. Molecular investigations showed that the compounds exerted differential changes in expression of signaling proteins in Jurkat and WEHI-231 cell lines. The activity ofSCM5is likely associated with elicitation of cell signaling pathways leading to cell apoptosis. The compounds may be of interest in terms of therapeutic utility as inhibitors of autoimmune disorders, virus replication and antitumor agents.

Quality Control of 1,1,1-Triethoxyethane. About 1,1,1-Triethoxyethane, If you have any questions, you can contact Sochacka-Cwikla, A; Regiec, A; Zimecki, M; Artym, J; Zaczynska, E; Kocieba, M; Kochanowska, I; Bryndal, I; Pyra, A; Maczynski, M or concate me.

Reference:
Thiazolidine – Wikipedia,
,Thiazolidine – ScienceDirect.com

An article TMPE Derived from Saffron Natural Monoterpene as Cytotoxic and Multidrug Resistance Reversing Agent in Colon Cancer Cells WOS:000585561500001 published article about P-GLYCOPROTEIN; DOXORUBICIN; DITERPENES; TERPENOIDS; COMBINATIONS; DIGITONIN; THYMOL in [Sroda-Pomianek, Kamila; Palko-Labuz, Anna; Pola, Andrzej; Wesolowska, Olga] Wroclaw Med Univ, Dept Biophys & Neurobiol, Ul Chalubinskiego 3, PL-50368 Wroclaw, Poland; [Ferens-Sieczkowska, Miroslawa; Koziol, Agata] Wroclaw Med Univ, Dept Chem & Immunochem, Ul M Sklodowskiej Curie 48-50, PL-50369 Wroclaw, Poland in 2020.0, Cited 52.0. Product Details of 78-39-7. The Name is 1,1,1-Triethoxyethane. Through research, I have a further understanding and discovery of 78-39-7

Terpenes constitute one of the largest groups of natural products. They exhibit a wide range of biological activities including antioxidant, anticancer, and drug resistance modulating properties. Saffron extract and its terpene constituents have been demonstrated to be cytotoxic against various types of cancer cells, including breast, liver, lung, pancreatic, and colorectal cancer. In the present work, we have studied anticancer properties of TMPE, a newly synthesized monoterpene derivative of beta-cyclocitral-the main volatile produced by the stigmas of unripe crocuses. TMPE presented selective cytotoxic activity to doxorubicin-resistant colon cancer cells and was identified to be an effective MDR modulator in doxorubicin-resistant cancer cells. Synergy between this derivative and doxorubicin was observed. Most probably, TMPE inhibited transport activity of ABCB1 protein without affecting its expression level. Analysis of TMPE physicochemical parameters suggested it was not likely to be transported by ABCB1. Molecular modeling showed TMPE being more reactive molecule than the parental compound-beta-cyclocitral. Analysis of electrostatic potential maps of both compounds prompted us to hypothesize that reduced reactivity as well as susceptibility to electrophilic attack were related to the lower general toxicity of beta-cyclocitral. All of the above pointed to TMPE as an interesting candidate molecule for MDR reversal in cancer cells.

Product Details of 78-39-7. About 1,1,1-Triethoxyethane, If you have any questions, you can contact Sroda-Pomianek, K; Palko-Labuz, A; Pola, A; Ferens-Sieczkowska, M; Wesolowska, O; Koziol, A or concate me.

Reference:
Thiazolidine – Wikipedia,
,Thiazolidine – ScienceDirect.com

Name: Chalcone. In 2020.0 ORGANOMETALLICS published article about ASYMMETRIC REDUCTION; EFFICIENT CATALYST; KETONES; ALDEHYDES; HYDROSILYLATION; COMPLEXES; HYDRIDE; RUTHENIUM; POLY(SILYLETHER)S; HYDROGENATION in [Vijjamarri, Srikanth; O’Denius, Timothy M.; Yao, Bin; Kubatov, Alena; Du, Guodong] Univ North Dakota, Dept Chem, Grand Forks, ND 58202 USA in 2020.0, Cited 81.0. The Name is Chalcone. Through research, I have a further understanding and discovery of 94-41-7.

Hydroboration of carbonyl compounds is an important transformation in organic chemistry, and a growing interest in catalysis has focused on abundant and nontoxic base metals. Herein we describe an efficient salen manganese catalyst for the hydroboration of a broad range of carbonyl compounds with pinacolborane. The catalytic reactions proceeded rapidly (>99% conversion in <5 min) at room temperature with very low catalyst loadings. High turnover frequency (up to 5700 h(-1)) was observed under these conditions. Several synthetically important functional groups were tolerated, and chemoselective hydroboration of aldehydes over ketones was achieved. The H/D kinetic isotopic effect of borane was determined to be 2.3. The Hammett correlation plot of a series of para-substituted acetophenone substrates, p-X-C6H6COCH3 (X = H, Me, OMe, NO2, Cl, Br, and CF3) yielded a positive slope of rho = +0.99. The crossover products were detected in the competition reaction of catecholborane and deuterated pinacolborane with acetophenone. The findings indicated a potential borane-mediated pathway that could account for the observation of the crossover products. About Chalcone, If you have any questions, you can contact Vijjamarri, S; O'Denius, TM; Yao, B; Kubatov, A; Du, GD or concate me.. Name: Chalcone

Reference:
Thiazolidine – Wikipedia,
,Thiazolidine – ScienceDirect.com

Name: 1,1,1-Triethoxyethane. I found the field of Chemistry; Pharmacology & Pharmacy very interesting. Saw the article Synthesis and biological activity of new derivatives with the preserved carane system published in 2020.0, Reprint Addresses Koziol, A (corresponding author), Wroclaw Univ Sci & Technol, Fac Chem, Dept Bioorgan Chem, Wroclaw, Poland.; Koziol, A (corresponding author), Acad Physiotherapy Wroclaw, Inst Cosmetol, Wroclaw, Poland.. The CAS is 78-39-7. Through research, I have a further understanding and discovery of 1,1,1-Triethoxyethane.

Terpenoid derivatives, which contain a preserved carane system in their structure, exhibit a broad spectrum of biological activities. Among them, we can distinguish insecticides, structures with pharmacological application etc. In the presented paper, the substrate – (-)-cis-caran-trans-4-ol was transformed using the reactions of typical organic synthesis to obtain novel derivatives. Most importantly, bromolactone ((-)-(1R,4R,6S)-2′-(bromomethyl)-4,7,7-trimethylspiro[bicyclo[4.1.0]heptan-3,3′-furan]-5′(4’H)-one) with the preserved carane system was synthesized. This bromolactone was tested for antifeedant activity against the lesser mealworm, Alphitobius diaperinus Panzer, and peach potato aphid (Myzus persicae). In addition, its moderate antibacterial activity was observed against the Bacillus subtilis strain (with Minimal Inhibitory Concentration of 200 mu g/mL).

Name: 1,1,1-Triethoxyethane. About 1,1,1-Triethoxyethane, If you have any questions, you can contact Koziol, A; Fratczak, J; Grela, E; Szczepanik, M; Gabrys, B; Dancewicz, K; Lochynski, S or concate me.

Reference:
Thiazolidine – Wikipedia,
,Thiazolidine – ScienceDirect.com

I found the field of Chemistry very interesting. Saw the article Cascade cyclization versus chemoselective reduction: a solvent-controlled product divergence published in 2020.0. Name: Chalcone, Reprint Addresses Jafarpour, F (corresponding author), Univ Tehran, Sch Chem, Coll Sci, Tehran 141556455, Iran.. The CAS is 94-41-7. Through research, I have a further understanding and discovery of Chalcone

A simple and efficient strategy for the assembly of polysubstituted thiophenes and the chemoselective reduction of alpha,beta-unsaturated ketones via the reaction of enones with elemental sulfur and by a simple switching of the reaction solvent is described. Mechanistic studies revealed that both the reactions proceeded via radical pathways, and two hydrogen atoms came from H2O in the reduction course.

Name: Chalcone. About Chalcone, If you have any questions, you can contact Jafarpour, F; Rajai-Daryasarei, S; Gohari, MH or concate me.

Reference:
Thiazolidine – Wikipedia,
,Thiazolidine – ScienceDirect.com

I found the field of Radiology, Nuclear Medicine & Medical Imaging very interesting. Saw the article Preventive Effect of Changing Contrast Media in Patients With A Prior Mild Immediate Hypersensitivity Reaction to Gadolinium-Based Contrast Agent published in 2019.0. Safety of 1,1,1-Triethoxyethane, Reprint Addresses Choi, YH (corresponding author), Seoul Natl Univ Hosp, Dept Radiol, 101 Daehak Ro, Seoul 03080, South Korea.. The CAS is 78-39-7. Through research, I have a further understanding and discovery of 1,1,1-Triethoxyethane

Objectives Currently, the prevention of recurrent immediate hypersensitivity reactions (HSRs) to contrast media (CM) requests premedication and changing the culprit contrast agent. However, strategies for the prevention of immediate HSRs to gadolinium-based magnetic resonance contrast agents (GBCAs) have not yet been established. This study aimed to evaluate the effectiveness of changing the contrast agent and single-dose premedication for HSR recurrence prevention in patients with a history of mild immediate HSR to GBCA. Materials and Methods The outcomes of patients with mild immediate HSR to GBCA who subsequently underwent enhanced magnetic resonance imaging between October 2012 and July 2017 were analyzed. The institutional CM monitoring system was retrospectively reviewed, and data on the application of premedication and choice of CM were obtained. Gadolinium-based magnetic resonance contrast agents were classified into 3 classes according to their molecular structure (macrocyclic ionic, macrocyclic nonionic, and linear ionic). Intravenous chlorpheniramine 4 mg, 30 minutes before the GBCA administration, or intravenous methylprednisolone sodium succinate 40 mg plus chlorpheniramine 4 mg, 1 hour before the GBCA administration, was administrated as premedication regimen. Recurrence rates of immediate HSR were compared according to prevention strategies. Results A total of 185 patients with a history of mild immediate HSR to GBCA were re-exposed to GBCA 397 times during the study period. The overall recurrence rate was 19.6% (78/397). Changing the culprit GBCA significantly reduced the recurrence rate, compared with reusing the culprit GBCA (6.9%, 9/130 and 25.8%, 69/267; P < 0.001). The recurrence rate was lowest when the GBCA was changed to a different molecular structure class from the culprit agent, followed by changing to CM with the same molecular structure and reusing the culprit GBCA (6.2%, 7/113 vs 11.8%, 2/17 vs 25.8%, 69/267; P < 0.001 with chi(2) test for trend). Single-dose premedication demonstrated no significant prophylactic effect on recurrence (20.4%, 17/98 vs 17.3%, 61/299 with and without premedication, respectively; P = 0.509). Premedication in addition to changing CM also showed no additional prophylactic effect (7.2%, 7/97 and 6.1%, 2/33, respectively; P = 0.821). Conclusions Changing the CM from the culprit agent could reduce the chance of HSR recurrence in patients with prior mild immediate HSR to GBCA, especially when the CM was changed to one of a different molecular structure class. However, single-dose premedication administration did not show significant HSR recurrence rate difference. Safety of 1,1,1-Triethoxyethane. About 1,1,1-Triethoxyethane, If you have any questions, you can contact Ryoo, CH; Choi, YH; Cheon, JE; Yoon, SH; Kang, HR; Park, SJ; Lee, W or concate me.

Reference:
Thiazolidine – Wikipedia,
,Thiazolidine – ScienceDirect.com

An article Novel pyrazolo[3,4-d]pyrimidine derivatives inhibit human cancer cell proliferation and induce apoptosis by ROS generation WOS:000518148300001 published article about PLASMA-MEMBRANE; IN-VITRO; ANTICANCER; PHOSPHATIDYLSERINE; CYCLE; DAMAGE; DNA in [Gaonkar, Supreet; Nadaf, AfraQuasar A.; Najare, Mahesh S.; Mantur, Shivaraj; Garbhagudi, Manjunatha; Khazi, Imtiyaz Ahmed M.] Karnatak Univ, Dept Studies Chem, Dharwad 580003, Karnataka, India; [Savanur, Mohammed Azharuddin] Indian Inst Sci, Dept Biochem, Bangalore 560012, Karnataka, India; [Mulla, Sikandar I.] REVA Univ, Sch Appl Sci, Dept Biochem, Bangalore, Karnataka, India in 2020.0, Cited 36.0. The Name is 1,1,1-Triethoxyethane. Through research, I have a further understanding and discovery of 78-39-7. Recommanded Product: 78-39-7

The paucity of effective anticancer drugs for successful treatment is a major concern, indicating the strong need for novel therapeutic compounds. In the quest of new molecules, the present study aimed to explore the potential of pyrazolo[3,4-d]pyrimidine derivatives as antiproliferative agents. In vitro anticancer screening of selected compounds was done by the National Cancer Institute’s Developmental Therapeutics Programme against a panel of 60 cancer cell lines. The lead compound PP-31d considerably inhibited the growth of cancer cells, such as NCI-H460 (non-small-cell lung cancer), OVCAR-4 (ovarian cancer), 786-0 (renal cancer), A549 (non-small-cell lung cancer), and ACHN (renal cancer), showing strong anticancer potential, among other derivatives. Kinetic studies of PP-31d on NCI-H460 cells revealed a dose-dependent effect with an IC50 of 2 mu M. The observed inhibition by PP-31d is attributed to the generation of reactive oxygen species and the subsequent induction of cellular apoptosis, as evidenced by the increase in the hypodiploid (subG1) population, the early apoptotic cell population, and caspase-3/7 activity, the loss of the mitochondrial membrane potential, and the degradation of nuclear DNA. Collectively, our results demonstrated that pyrazolo[3,4-d]pyrimidine derivatives inhibit cancer cell proliferation by inducing apoptosis and, thus, have the potential to be further explored for anticancer properties.

Recommanded Product: 78-39-7. About 1,1,1-Triethoxyethane, If you have any questions, you can contact Gaonkar, S; Savanur, MA; Nadaf, AA; Najare, MS; Mantur, S; Garbhagudi, M; Mulla, SI; Khazi, IAM or concate me.

Reference:
Thiazolidine – Wikipedia,
,Thiazolidine – ScienceDirect.com

An article Synthesis of novel 2-(1-adamantanylcarboxamido)thiophene derivatives. Selective cannabinoid type 2 (CB2) receptor agonists as potential agents for the treatment of skin inflammatory disease WOS:000451498200016 published article about POSITIVE ALLOSTERIC MODULATORS; HIGH-AFFINITY; PHARMACOLOGICAL EVALUATION; DISCOVERY; LIGANDS; PAIN; IDENTIFICATION; INHIBITORS; SCAFFOLDS in [Mugnaini, Claudia; Brizzi, Antonella; Palombi, Nastasja; Corelli, Federico] Univ Siena, Dipartimento Biotecnol Chim & Farm, Via Aldo Moro 2, I-53100 Siena, Italy; [Rabbito, Alessandro; Petrosino, Stefania; Verde, Roberta; Di Marzo, Vincenzo; Ligresti, Alessia] CNR, Ist Chim Biomol, Endocannabinoid Res Grp, Via Campi Flegrei 34, I-80078 Naples, Italy in 2019.0, Cited 55.0. The Name is 1,1,1-Triethoxyethane. Through research, I have a further understanding and discovery of 78-39-7. Product Details of 78-39-7

A set of CB2R ligands, based on the thiophene scaffold, was synthesized and evaluated in in vitro assays. Compounds 8c-i, k, 1, bearing the 3-carboxylate and 2-(adamantan-1-yl)carboxamido groups together with apolar alkyl/aryl substituents at 5-position or at 4- and 5-positions of the thiophene ring possess high CB2R affinity at low nanomolar concentration, good receptor selectivity, and agonistic functional activity. The full agonist 8g, showing the best balance between receptor affinity and selectivity, was tested in vitro in an experimental model of allergic contact dermatitis and proved to be able to block the release of MCP-2 in HaCaT cells at 10 mu M concentration. (C) 2018 Elsevier Masson SAS. All rights reserved.

About 1,1,1-Triethoxyethane, If you have any questions, you can contact Mugnaini, C; Rabbito, A; Brizzi, A; Palombi, N; Petrosino, S; Verde, R; Di Marzo, V; Ligresti, A; Corelli, F or concate me.. Computed Properties of C8H18O3

Reference:
Thiazolidine – Wikipedia,
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Computed Properties of C8H18O3. In 2020.0 ORG BIOMOL CHEM published article about COPPER-CATALYZED CYCLOISOMERIZATION; FACE-SELECTIVE PLATINUM; ALPHA-AMINO-ACIDS; MARINE SPONGE; ENANTIOSELECTIVE SYNTHESIS; MULTICOMPONENT REACTIONS; CLAISEN REARRANGEMENT; 1ST SYNTHESIS; SESQUITERPENES; CYCLOPROPANES in [Hosokawa, Seijiro; Nakanishi, Keisuke; Udagawa, Yutaro] Waseda Univ, Fac Adv Sci & Engn, Dept Appl Chem, Shinjuku Ku, 3-4-1 Ohkubo, Tokyo 1698555, Japan; [Maeda, Mitsutoshi; Sato, Seiya; Nakano, Keiji; Ichikawa, Yoshiyasu] Kochi Univ, Fac Sci, Akebono Cho, Kochi 7808520, Japan; [Masuda, Toshiya] Osaka City Univ, Grad Sch Human Lift Sci, Osaka 5588585, Japan in 2020.0, Cited 59.0. The Name is 1,1,1-Triethoxyethane. Through research, I have a further understanding and discovery of 78-39-7.

The first total synthesis of a marine natural product, exigurin, has been accomplished in 13 steps starting from (+)-menthone. The key intermediate (-)-10-epi-axisonitrile-3 was prepared by stereoselective intramolecular cyclopropanation followed by a cyclopropane ring opening reaction by the azide anion. The bioinspired Ugi reaction of (-)-10-epi-axisonitrile-3, formaldehyde, sarcosine and methanol successfully constructed the target exigurin in which its terpene and amino acid units were linked through an amide bond.

Computed Properties of C8H18O3. About 1,1,1-Triethoxyethane, If you have any questions, you can contact Hosokawa, S; Nakanishi, K; Udagawa, Y; Maeda, M; Sato, S; Nakano, K; Masuda, T; Ichikawa, Y or concate me.

Reference:
Thiazolidine – Wikipedia,
,Thiazolidine – ScienceDirect.com