Month: October 2022

Pan, Qingqing; Deng, Xin; Gao, Wenxia; Chang, Jing; Pu, Yuji; He, Bin published the artcile< ROS triggered cleavage of thioketal moiety to dissociate prodrug nanoparticles for chemotherapy>, Application In Synthesis of 96-53-7, the main research area is cancer doxorubicin PEG nanoparticle delivery ROS; Cancer therapy; Dissociation; Prodrug nanoparticle; ROS-responsive; Thioketal.

With the utilization of high concentration reactive oxygen species (ROS) in tumor microenvironment, PEG-doxorubicin (PEG-DOX) prodrug was synthesized via a thioketal moiety as the linker, which was ROS cleavable to trigger DOX release from the self-assembled prodrug nanoparticles. The in vitro ROS sensitivity of prodrug nanoparticles (NPs) was investigated in Fenton agent and H2O2, and the disassembly of NPs was more sensitive to Fenton reagent. After internalized in HepG2 cells via endocytosis, the cellular ROS consuming test revealed intracellular DOX release. The pharmacokinetics and biodistribution study demonstrated that the in vivo elimination of NPs was significantly improved and the NPs were passively targeted to tumor tissues via EPR effect. The ROS-responsive prodrug NPs exhibited excellent antitumor activity in HepG2 tumor-bearing nude mice, remarkably induced tumor cells apoptosis and reduced the systemic toxicity of DOX. Our study revealed the ROS responsive prodrug nanoparticle is an effective strategy to fabricate nanomedicine for cancer chemotherapy.

Colloids and Surfaces, B: Biointerfacespublished new progress about Aggregation. 96-53-7 belongs to class thiazole, and the molecular formula is C3H5NS2, Application In Synthesis of 96-53-7.

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

Chen, Ning; Jia, Weiyi; Xu, Jiaxi published the artcile< A Versatile Synthesis of Various Substituted Taurines from Vicinal Amino Alcohols and Aziridines>, Reference of 171877-39-7, the main research area is taurine substituted preparation amino alc aziridine carbon disulfide; oxidation thiazolidinethione.

Taurine and structurally diverse substituted taurines have been synthesized by peroxyformic acid oxidation of the thiazolidine-2-thione intermediates generated from vicinal amino alcs. or aziridines and carbon disulfide. The stereochem. and mechanisms of the reactions are discussed. The method is a salt-free and versatile route, convenient in terms of purification, and can be used to synthesize optically active substituted taurines. (© Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2009).

European Journal of Organic Chemistrypublished new progress about Amino alcohols Role: RCT (Reactant), RACT (Reactant or Reagent). 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, Reference of 171877-39-7.

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

Crimmins, Michael T.; Christie, Hamish S.; Hughes, Colin O. published the artcile< Synthesis and diastereoselective aldol reactions of a thiazolidinethione chiral auxiliary>, Name: (S)-4-Benzylthiazolidine-2-thione, the main research area is thiazolidinethione chiral auxiliary; propanoyl thiazolidinethione syn aldol.

Thiazolidinethione chiral auxiliary I (R = H) is prepared from (S)-phenylalaninol and carbon disulfide. Propanoylated I [R = C(O)CH2CH3] can be used for either Evans syn aldol reactions or non-Evans syn aldol reactions with a variety of aldehydes, in good yield with good stereoselectivity.

Organic Synthesespublished new progress about Aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, Name: (S)-4-Benzylthiazolidine-2-thione.

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

Singh, Sarangthem Joychandra; Devi, Nepram Sushuma published the artcile< Diacetoxyiodobenzene mediated oxidative dethionation of N-substituted 5-arylmethylidene rhodanines: an efficient synthesis of N-substituted 5-arylmethylidene thiazolidine-2,4-diones>, Recommanded Product: 3-Benzyl-2-thioxothiazolidin-4-one, the main research area is arylmethylidene thiazolidine dione preparation; rhodanine arylmethylidene oxidative dethionation.

A simple and efficient synthesis of N-substituted-5-arylmethylidene thiazolidine-2,4-diones I (R1 = Ph, 2-fluorophenyl, 4-methoxyphenyl, 2-furyl, etc.; R2 = CH3, C6H5CH2, CH2=CHCH2; X = S) has been developed via oxidative dethionation of N-substituted-5-arylmethylidene rhodanines I (R1 = Ph, 2-fluorophenyl, 4-methoxyphenyl, 2-furyl, etc.; R2 = CH3, C6H5CH2, CH2=CHCH2; X = O) using diacetoxyiodobenzene (DIB) in ethanol at room temperature This protocol is simple, mild and column free, and obviates the need of acids and bases, and offers a broad substrate scope.

ARKIVOC (Gainesville, FL, United States)published new progress about Aryl aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, Recommanded Product: 3-Benzyl-2-thioxothiazolidin-4-one.

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

Wang, Xinmou; Chen, Yuming; Song, Hongjian; Liu, Yuxiu; Wang, Qingmin published the artcile< Construction of 2-(2-Arylphenyl)azoles via Cobalt-Catalyzed C-H/C-H Cross-Coupling Reactions and Evaluation of Their Antifungal Activity>, Name: Ethyl 4-methylthiazole-5-carboxylate, the main research area is biaryl azole cobalt catalyst agrochem fungicide; azole biphenyl amide cross coupling reaction.

Although compounds with a 2-(2-arylphenyl) benzoxazole motif are biol. important, there are only a few methods for synthesizing them. Herein, authors report an efficient method for synthesis of such compounds by means of cobalt-catalyzed C-H/C-H cross-coupling reactions. This method has a broad substrate scope and good tolerance for sensitive functional groups. In addition, authors demonstrate that introducing a heteroarene moiety to biphenyl compounds enhanced their antifungal activity.

Organic Letterspublished new progress about Agrochemical fungicides. 20582-55-2 belongs to class thiazole, and the molecular formula is C7H9NO2S, Name: Ethyl 4-methylthiazole-5-carboxylate.

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

Bi, Huihua; Zhou, Yu; Jiang, Wei; Liu, Jie published the artcile< Electrophotocatalytic C-H Hydroxyalkylation of Heteroaromatics with Aldehydes>, Formula: C7H9NO2S, the main research area is heteroarene electrochem photochem Minisci hydroxyalkylation aldehyde; alc heteroaryl preparation.

A radical hydroxyalkylation of N-heteroaromatics with aldehydes is reported. The constructive merging of photochem. and electrochem. is the key for the success of this atom-economical Minisci method. This protocol highlights the utility of electrophotocatalysis to promote a practical and general synthesis of secondary alcs. in good yields from readily available N-heteroaromatics and aldehydes under mild reaction conditions.

Advanced Synthesis & Catalysispublished new progress about Aldehydes Role: PRP (Properties), RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 20582-55-2 belongs to class thiazole, and the molecular formula is C7H9NO2S, Formula: C7H9NO2S.

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

Zhou, Renwu; Zhou, Rusen; Zhang, Xianhui; Fang, Zhi; Wang, Xiaoxiang; Speight, Robert; Wang, Hongxia; Doherty, William; Cullen, Patrick J.; Ostrikov, Kostya; Bazaka, Kateryna published the artcile< High-Performance Plasma-Enabled Biorefining of Microalgae to Value-Added Products>, Application In Synthesis of 57493-24-0, the main research area is microalgae biorefining high performance plasma; biomass; biorefining; liquefaction; microalgae; plasma chemistry.

Conversion of renewable biomass by time- and energy-efficient techniques remains an important challenge. Herein, plasma catalytic liquefaction (PCL) is employed to achieve rapid liquefaction of microalgae under mild conditions. The choice of the catalyst affects both the liquefaction efficiency and the yield of products. The acid catalyst is more effective and gave a liquid yield of 73.95 wt % in 3 min, as opposed to 69.80 wt % obtained with the basic catalyst in 7 min. Analyses of the thus-formed products and the processing environment reveal that the enhanced PCL performance is linked to the rapid increase in temperature under the effect of plasma-induced elec. fields and the generation of large quantities of reactive species. Moreover, the obtained solid residue can be simply upgraded to a carbon product suitable for supercapacitor applications. Therefore, the proposed strategy may provide a new avenue for fast and comprehensive utilization of biomass under benign conditions.

ChemSusChempublished new progress about Alcohols Role: IMF (Industrial Manufacture), PREP (Preparation). 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Application In Synthesis of 57493-24-0.

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

Singh, Kamaljit; Singh, Sarbjit; Taylor, John A. published the artcile< Monoazo disperse dyes-part 1: synthesis, spectroscopic studies and technical evaluation of monoazo disperse dyes derived from 2-aminothiazoles>, Recommanded Product: 2-Amino-4-(3-nitrophenyl)thiazole, the main research area is aminothiazole diazo aminoacetanilide coupling component disperse azo dye; polyester fabric disperse dyeing thiadiazole azo dye preparation.

Novel disperse dyes have been prepared from thiazolyl diazonium salts and coupling components based on m-aminoacetanilide derivatives Depending upon various substituents incorporated into the chromophore, absorption maxima varied from 495 to 591 nm in various organic solvents. These dyes were chromophorically strong as evidenced both by molar extinction coefficient in solvent and by strength and build-up on polyester.

Dyes and Pigmentspublished new progress about Disperse azo dyes. 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Recommanded Product: 2-Amino-4-(3-nitrophenyl)thiazole.

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

Richter, Anja; Rose, Rolf; Hedberg, Christian; Waldmann, Herbert; Ottmann, Christian published the artcile< An Optimised Small-Molecule Stabiliser of the 14-3-3-PMA2 Protein-Protein Interaction>, Formula: C10H7NOS, the main research area is pyrrolidone derivative stabilizer PMA2 protein interaction crystal structure.

Modulation of protein-protein interactions (PPIs) is a highly demanding, but also a very promising approach in chem. biol. and targeted drug discovery. In contrast to inhibiting PPIs with small, chem. tractable mols., stabilization of these interactions can only be achieved with complex natural products, like rapamycin, FK506, taxol, forskolin, brefeldin and fusicoccin. Fusicoccin stabilizes the activatory complex of the plant H+-ATPase PMA2 and 14-3-3 proteins. Recently, the stabilizing effect of fusicoccin could be mimicked by a trisubstituted pyrrolinone (pyrrolidone1, 1). Here, the authors report the synthesis, functional activity and crystal structure of derivatives of 1 that stabilize the 14-3-3-PMA2 complex. With a limited compound collection three modifications that are important for activity enhancement could be determined: (1) conversion of the pyrrolinone scaffold into a pyrazole, (2) introduction of a tetrazole moiety to the Ph ring that contacts PMA2, and (3) addition of a bromine to the Ph ring that exclusively contacts the 14-3-3 protein. The crystal structure of a pyrazole derivative of 1 in complex with 14-3-3 and PMA2 revealed that the more rigid core of this mol. positions the stabilizer deeper into the rim of the interface, enlarging especially the contact surface to PMA2. Combination of the aforementioned features gave rise to a mol. (I) that displays a threefold increase in stabilizing the 14-3-3-PMA2 complex over 1. Compound I and the other active derivatives show no effect on two other important 14-3-3 protein-protein interactions, i.e., with CRaf and p53. This is the first study that describes the successful optimization of a PPI stabilizer identified by screening.

Chemistry – A European Journalpublished new progress about 14-3-3 Proteins Role: BSU (Biological Study, Unclassified), PEP (Physical, Engineering or Chemical Process), BIOL (Biological Study), PROC (Process). 198904-53-9 belongs to class thiazole, and the molecular formula is C10H7NOS, Formula: C10H7NOS.

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

Lam, P. Y. S.; Deudon, S.; Hauptman, E.; Clark, C. G. published the artcile< α-Nitrogen-activating effect in the room temperature copper-promoted N-arylation of heteroaryl carboxamides with phenylsiloxane or 4-tolylboronic acid>, Application In Synthesis of 31825-95-3, the main research area is nitrogen heteroaromatic carboxamide phenylsiloxane arylation; tolylboronate nitrogen heteroaromatic carboxamide arylation; cross coupling nitrogen heteroaromatic carboxamide phenylsiloxane.

α-N-containing heteroaryl carboxamides undergo Cu-promoted N-phenylation with hypervalent PhSi(OMe)3 at room temperature, in the absence of base and in air. Arylboronic acid can substitute for PhSi(OMe)3 as the organometalloid. The α-heteroatom chelating effect is in the decreasing order of N > O, S. This discovery opens up the possibility of using other α-N functional groups to direct the N-arylation of peptides and simple amides under conditions as mild as that of amide bond formation.

Tetrahedron Letterspublished new progress about Amides Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation) (heteroaromatic). 31825-95-3 belongs to class thiazole, and the molecular formula is C5H6N2OS, Application In Synthesis of 31825-95-3.

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