Day: October 11, 2022

Huang, David S.; Wong, Henry L.; Georg, Gunda I. published the artcile< Synthesis and evaluation of C2 functionalized analogs of the α-tubulin-binding natural product pironetin>, Related Products of 171877-39-7, the main research area is pironetin analog preparation anticancer structure activity ovarian cancer; Cytotoxicity; Pironetin; Structure-activity; Synthesis; Tubulin.

Pironetin is an α-tubulin-binding natural product with potent antiproliferative activity against several cancer cell lines that inhibits cell division by forming a covalent adduct with α-tubulin via a Michael addition into the natural product’s α,β-unsaturated lactone. We designed and prepared analogs carrying electron-withdrawing groups at the α-position (C2) of the α,β-unsaturated lactone with the goal to generate potent and selective binding analogs. We prepared derivatives I (R = F, Me, Cl, Br, Ph) containing halogens, a Ph, and a Me group at the C2 position to evaluate the structure-activity relationship at this position. Testing of the analogs in ovarian cancer cell lines demonstrated 100-1000-fold decreased antiproliferative activity.

Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, Related Products of 171877-39-7.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Ren, Qi; Dai, Lu; Zhang, Hui; Tan, Wenfei; Xu, Zhengshuang; Ye, Tao published the artcile< Total synthesis of largazole>, Recommanded Product: Ethyl 2-(((tert-butoxycarbonyl)amino)methyl)thiazole-4-carboxylate, the main research area is largazole asym total synthesis.

The stereocontrolled total synthesis of largazole was accomplished starting from 3-[(tert-butyldimethylsilyl)oxy]propanol in 5.8% overall yield, unambiguously confirming its structure. Key steps included the use of the Nagao thiazolidinethione auxiliary for a diastereoselective acetate aldol reaction, thiazoline-thiazole formation, and macrolactamization by use of the Mukaiyama reagent.

Synlett published new progress about Aldol addition, stereoselective. 96929-05-4 belongs to class thiazole, and the molecular formula is C12H18N2O4S, Recommanded Product: Ethyl 2-(((tert-butoxycarbonyl)amino)methyl)thiazole-4-carboxylate.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Love, Anna C.; Prescher, Jennifer A. published the artcile< Seeing (and Using) the Light: Recent Developments in Bioluminescence Technology>, Application In Synthesis of 2591-17-5, the main research area is review luciferase luciferin bioluminescence optical imaging; bioluminescence; imaging; luciferase; luciferin; optogenetics.

A review. Bioluminescence has long been used to image biol. processes in vivo. This technol. features luciferase enzymes and luciferin small mols. that produce visible light. Bioluminescent photons can be detected in tissues and live organisms, enabling sensitive and noninvasive readouts on physiol. function. Traditional applications have focused on tracking cells and gene expression patterns, but new probes are pushing the frontiers of what can be visualized. The past few years have also seen the merger of bioluminescence with optogenetic platforms. Luciferase-luciferin reactions can drive light-activatable proteins, ultimately triggering signal transduction and other downstream events. This review highlights these and other recent advances in bioluminescence technol., with an emphasis on tool development. We showcase how new luciferins and engineered luciferases are expanding the scope of optical imaging. We also highlight how bioluminescent systems are being leveraged not just for sensing-but also controlling-biol. processes.

Cell Chemical Biology published new progress about Bioluminescence. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Application In Synthesis of 2591-17-5.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Schmidt, Ulrich; Utz, Roland; Lieberknecht, Albrecht; Griesser, Helmut; Potzolli, Bernd; Bahr, Johanna; Wagner, Karin; Fischer, Peter published the artcile< Amino acids and peptides. 60. Synthesis of biologically active cyclopeptides. 10. Synthesis of 16 structural isomers of dolastatin 3. II. Synthesis of the linear educts and the cyclopeptides>, Category: thiazole, the main research area is dolastatin 3 isomer; structure dolastatin 3 NMR.

Sixteen isomers (I and II) of the cancerostatic cyclopeptide dolastatin 3 were synthesized. The proposed structure of dolastatin 3 is shown by 1H NMR spectrometry to be incorrect.

Synthesis published new progress about Isomers. 96929-05-4 belongs to class thiazole, and the molecular formula is C12H18N2O4S, Category: thiazole.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Tungen, Joern E.; Aursnes, Marius; Hansen, Trond Vidar published the artcile< Stereoselective synthesis of maresin 1>, Application of C10H11NS2, the main research area is maresin 1 stereoselective preparation diastereoselective Evans Nagao aldol.

Maresin 1 (I) is a potent anti-inflammatory and pro-resolving lipid mediator derived from docosahexaenoic acid. The total synthesis of maresin 1 is achieved in 10 steps and in 7% overall yield. The Evans-Nagao aldol reaction between (2E,4E)-5-bromopenta-2,4-dienal and different chiral auxiliaries is investigated. The reported synthesis is efficient and highly stereoselective, affording multi-milligram quantities of this biol. interesting lipid mediator.

Tetrahedron Letters published new progress about Aldol addition, stereoselective. 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, Application of C10H11NS2.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Sun, Ping; Wang, Chunlei; Padivitage, Nilusha Lasanthi Thilakarathna; Nanayakkara, Yasith S.; Perera, Sirantha; Qiu, Haixiao; Zhang, Ying; Armstrong, Daniel W. published the artcile< Evaluation of aromatic-derivatized cyclofructans 6 and 7 as HPLC chiral selectors>, Formula: C10H11NS2, the main research area is aromatic derivatized cyclofructan HPLC chiral selector stationary phase.

The two best aromatic-functionalized cyclofructan chiral stationary phases, R-naphthylethyl-carbamate cyclofructan 6 (RN-CF6) and dimethylphenyl-carbamate cyclofructan 7 (DMP-CF7), were synthesized and evaluated by injecting various classes of chiral analytes. They provided enantioselectivity toward a broad range of compounds, including chiral acids, amines, metal complexes, and neutral compounds It is interesting that they exhibited complementary selectivities and the combination of two columns provided enantiomeric separations for 43% of the test analytes. These extensive chromatog. results provided useful information about method development of specific analytes, and also gave some insight as to the enantioseparation mechanism.

Analyst (Cambridge, United Kingdom) published new progress about Alcohols Role: ANT (Analyte), ANST (Analytical Study) (analytes). 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, Formula: C10H11NS2.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Agrawal, Madhavi; Kharkar, Prashant; Moghe, Sonali; Mahajan, Tushar; Deka, Vaishali; Thakkar, Chandni; Nair, Amrutha; Mehta, Chirag; Bose, Julie; Kulkarni-Almeida, Asha; Bhedi, Dilip; Vishwakarma, Ram A. published the artcile< Discovery of thiazolyl-phthalazinone acetamides as potent glucose uptake activators via high-throughput screening>, Category: thiazole, the main research area is thiazolylphthalazinone acetamide preparation SAR glucose uptake activator; Glucose uptake activators; Obesity; PPAR-γ; Thiazolyl-phthalazinone acetamides; Type 2 diabetes.

With the aim to discover orally active small mols. that stimulate glucose uptake, high throughput screening of a library of 5000 drug-like compounds was conducted in differentiated skeletal muscle cells in presence of insulin. N-Substituted phthalazinone acetamide was identified as a potential glucose uptake modulator. Several novel derivatives were synthesized to establish structure activity relationships. Identified lead thiazolyl-phthalazinone acetamide (7114863; I) increased glucose uptake (EC50 of 0.07±0.02 μM) in differentiated skeletal muscle cells in presence of insulin. Furthermore, I was superior to rosiglitazone under similar exptl. conditions without inducing PPAR-γ agonist activity thus making it a very interesting scaffold.

Bioorganic & Medicinal Chemistry Letters published new progress about Structure-activity relationship. 72054-60-5 belongs to class thiazole, and the molecular formula is C7H10N2O2S, Category: thiazole.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Thakur, Nimisha; Patil, Rahul A.; Talebi, Mohsen; Readel, Elizabeth R.; Armstrong, Daniel W. published the artcile< Enantiomeric impurities in chiral catalysts, auxiliaries, and synthons used in enantioselective syntheses. Part 5>, SDS of cas: 171877-39-7, the main research area is chiral catalyst synthon enantioselective enantiomeric impurity; chiral separation; enantiomeric excess; enantiomeric impurity; enantioselective syntheses.

The enantiomeric excess of chiral starting materials is one of the important factors determining the enantiopurity of products in asym. synthesis. Fifty-one com. available chiral reagents used as building blocks, catalysts, and auxiliaries in various enantioselective syntheses were assayed for their enantiomeric purity. The test results were classified within five impurities level (ie, <0.01%, 0.01%-0.1%, 0.1%-1%, 1%-10%, >10%). Previously from 1998 to 2013, several reports have been published on the enantiomeric composition of more than 300 chiral reagents. This series of papers is necessitated by the fact that new reagents are forthcoming and that the enantiomeric purity of the same reagent can vary from batch to batch and/or from supplier to supplier. This report presents chiral liquid chromatog. (LC) and gas composition(GC) methods to sep. enantiomers of chiral compounds and evaluate their enantiomeric purities. The accurate and efficient LC anal. was done using newly introduced superficially porous particle (SPP 2.7μm) based chiral stationary phases (TeicoShell, VancoShell, LarihcShell-P, and NicoShell).

Chirality published new progress about Enantioselective synthesis. 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, SDS of cas: 171877-39-7.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Schramm, Stefan; Al-Handawi, Marieh B.; Karothu, Durga Prasad; Kurlevskaya, Anastasiya; Commins, Patrick; Mitani, Yasuo; Wu, Chun; Ohmiya, Yoshihiro; Naumov, Pance published the artcile< Mechanically Assisted Bioluminescence with Natural Luciferase>, Electric Literature of 2591-17-5, the main research area is mechanic bioluminescence luciferase; Cypridina; bioluminescence; luciferase; mechanochemistry; solvent-assisted reactions.

Mechanochem. analogs have recently been established for several enzymic reactions, but they require periodic interruption of the reaction for sampling, dissolution, and (bio)chem. anal. to monitor their progress. By applying a mechanochem. procedure to induce bioluminescence analogous to that used by the marine ostracod Cypridina (Vargula) hilgendorfii, the light emitted by a bioluminescent reaction can be used to directly monitor the progress of a mechanoenzymic reaction without sampling. Mech. treatment of Cypridina luciferase with luciferin generates bright blue light which can be readily detected and analyzed spectroscopically. This mech. assisted bioluminescence proceeds through a mechanism identical to that of bioluminescence in solution, but has higher activation energy due to being diffusion-controlled in the viscous matrix. The results suggest that luciferases could be used as light-emissive reporters of mechanoenzymic reactions.

Angewandte Chemie, International Edition published new progress about Bioluminescence. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Electric Literature of 2591-17-5.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Martin-Burgos, Blanca; Wang, Wanqi; William, Ivana; Tir, Selma; Mohammad, Innus; Javed, Reja; Smith, Stormi; Cui, Yilin; Arzavala, Jessica; Mora, Dalilah; Smith, Ciearra B.; van der Vinne, Vincent; Molyneux, Penny C.; Miller, Stephen C.; Weaver, David R.; Leise, Tanya L.; Harrington, Mary E. published the artcile< Methods for detecting PER2:LUCIFERASE bioluminescence rhythms in freely moving mice>, Category: thiazole, the main research area is circadian rhythm bioluminescence gene expression photomultiplier tube; CycLuc1; PERIOD2; bioluminescence; circadian; in vivo; luciferase; peripheral oscillators; reporter gene.

Circadian rhythms are driven by daily oscillations of gene expression. An important tool for studying cellular and tissue circadian rhythms is the use of a gene reporter, such as bioluminescence from the reporter gene luciferase controlled by a rhythmically expressed gene of interest. Here we describe methods that allow measurement of circadian bioluminescence from a freely moving mouse housed in a standard cage. Using a LumiCycle In Vivo (Actimetrics), we determined conditions that allow detection of circadian rhythms of bioluminescence from the PER2 reporter, PER2::LUC, in freely behaving mice. The LumiCycle In Vivo applies a background subtraction that corrects for effects of room temperature on photomultiplier tube (PMT) output. We tested delivery of d-luciferin via a s.c. minipump and in the drinking water. We demonstrate spikes in bioluminescence associated with drinking bouts. Further, we demonstrate that a synthetic luciferase substrate, CycLuc1, can support circadian rhythms of bioluminescence, even when delivered at a lower concentration than d-luciferin, and can support longer-term studies. A small difference in phase of the PER2::LUC bioluminescence rhythms, with females phase leading males, can be detected with this technique. We share our anal. scripts and suggestions for further improvements in this method. This approach will be straightforward to apply to mice with tissue-specific reporters, allowing insights into responses of specific peripheral clocks to perturbations such as environmental or pharmacol. manipulations.

Journal of Biological Rhythms published new progress about Biological oscillations. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Category: thiazole.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica