Tag: M.W=200-250

Pierre, Fabrice; Chua, Peter C.; O’Brien, Sean E.; Siddiqui-Jain, Adam; Bourbon, Pauline; Haddach, Mustapha; Michaux, Jerome; Nagasawa, Johnny; Schwaebe, Michael K.; Stefan, Eric; Vialettes, Anne; Whitten, Jeffrey P.; Chen, Ta Kung; Darjania, Levan; Stansfield, Ryan; Anderes, Kenna; Bliesath, Josh; Drygin, Denis; Ho, Caroline; Omori, May; Proffitt, Chris; Streiner, Nicole; Trent, Katy; Rice, William G.; Ryckman, David M. published the artcile< Discovery and SAR of 5-(3-Chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic Acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer>, Reference of 53636-56-9, the main research area is naphthyridinecarboxylic acid derivative CX4945 preparation antitumor structure activity; protein kinase CK2 target antitumor CX 4945 preparation.

Herein we chronicle the discovery of CX-4945 (I), a first-in-class, orally bioavailable ATP-competitive inhibitor of protein kinase CK2 in clin. trials for cancer. CK2 has long been considered a prime cancer drug target because of the roles of deregulated and overexpressed CK2 in cancer-promoting pro-survival and antiapoptotic pathways. These biol. properties as well as the suitability of CK2’s small ATP binding site for the design of selective inhibitors, led us to fashion novel therapeutic agents for cancer. The optimization leading to I (Ki = 0.38 nM) was guided by mol. modeling, suggesting a strong binding of I resulting from a combination of hydrophobic interactions, an ionic bridge with Lys68, and hydrogen bonding with the hinge region. I was highly selective, orally bioavailable across species (20-51%) and efficacious in xenograft models. The discovery of I will allow the therapeutic targeting of CK2 in humans for the first time.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 53636-56-9 belongs to class pyridine-derivatives, and the molecular formula is C7H6BrNO2, Reference of 53636-56-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Shi, Buyin; Xu, Yang; Wang, Tianqi; Gao, Shengguang; Meng, Guojie; Huang, Kun published the artcile< Ag nanoparticles encapsulated in carboxyl-functionalized hollow microporous organic nanospheres for highly efficient catalysis applications>, Recommanded Product: 1,2-Di(pyridin-2-yl)disulfane, the main research area is carboxyl functionalized hollow microporous organic nanosphere silver nanoparticle; catalysis application.

In this work, we present a novel synthesis of Ag nanoparticles encapsulated in carboxyl-functionalized hollow microporous organic nanospheres (Ag@COOH-HMONs) by a combination of hyper-crosslinking mediated self-assembly and simply impregnation method, in which the COOH-HMONs supports were prepared via a Friedel-Crafts alkylation reaction by using polylactide-b-poly(tertbutyl acrylate)-b-polystyrene (PLA-b-PtBA-b-PS) triblock copolymer as precursors. Owing to the abundant carboxyl groups in the cavity of COOH-HMONs, highly dispersed silver nanoparticles can be successfully anchored into COOH-HMONs to produce Ag@COOH-HMONs via an ion exchange with AgNO3 following by an in-situ reduction of sodium borohydride (NaBH4). The obtained Ag@COOH-HMONs exhibit the high catalytic activities for the reduction of MB and nitroarom. compounds as well as selective oxidation of thiol and styrene due to their high surface area, hierarchical porosity and yolk-shell nanostructure. This approach of constructing novel metal@porous organic polymers is expected to open doors for new types of yolk-shell structural catalysts for practical applications.

Applied Catalysis, A: General published new progress about Aromatic nitro compounds Role: RCT (Reactant), RACT (Reactant or Reagent). 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Recommanded Product: 1,2-Di(pyridin-2-yl)disulfane.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Cheng, Xiayun; Taylor, Alexandria P.; Zhu, Kaicheng published the artcile< Synthesis of Substituted 2-Pyridones via 6π-Electrocyclization of Dienyl Isocyanates>, Name: Methyl 3-bromo-2-pyridinecarboxylate, the main research area is substituted pyridone preparation; dienyl isocyanate pi electrocyclization Curtius.

A one-pot Curtius rearrangement of dienyl carboxylic acids followed by a 6π-electrocyclization process to form substituted 2-pyridone products was developed. Dienyl isocyanates generated from aliphatic acids were more reactive than their aromatic counterparts. Addnl., substitution patterns of the carboxylic acids had an impact on the efficiency of the cyclization.

Journal of Organic Chemistry published new progress about Alkenes Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 53636-56-9 belongs to class pyridine-derivatives, and the molecular formula is C7H6BrNO2, Name: Methyl 3-bromo-2-pyridinecarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Kuehn, Laura; Jammal, Dominik G.; Lubitz, Katharina; Marder, Todd B.; Radius, Udo published the artcile< Stoichiometric and Catalytic Aryl-Cl Activation and Borylation using NHC-stabilized Nickel(0) Complexes>, Related Products of 329214-79-1, the main research area is bond activation aryl chloride borylation nickel NHC complex catalyst; crystal structure mol nickel heterocyclic carbene complex preparation; bond activation; boronates; borylation; carbene ligands; homogeneous catalysis; nickel.

NHC-nickel (NHC = N-heterocyclic carbene) complexes are efficient catalysts for the C-Cl bond borylation of aryl chlorides using NaOAc as a base and B2pin2 (pin = pinacolato) as the boron source. The catalysts [Ni2(ICy)4(μ-(η2:η2)-COD)] (1, ICy = 1,3-dicyclohexylimidazolin-2-ylidene; COD = 1,5-cyclooctadiene), [Ni(ICy)2(η2-C2H4)] (2), and [Ni(ICy)2(η2-COE)] (3, COE = cyclooctene) compare well with other nickel catalysts reported previously for aryl-chloride borylation with the advantage that no further ligands had to be added to the reaction. Borylation also proceeded with B2neop2 (neop = neopentylglycolato) as the boron source. Stoichiometric oxidative addition of different aryl chlorides to complex 1 was highly selective affording trans-[Ni(ICy)2(Cl)(Ar)] (Ar = 4-(F3C)C6H4, 11; 4-(MeO)C6H4, 12; C6H5, 13; 3,5-F2C6H3, 14).

Chemistry – A European Journal published new progress about Aryl chlorides Role: RCT (Reactant), RACT (Reactant or Reagent). 329214-79-1 belongs to class pyridine-derivatives, and the molecular formula is C11H16BNO2, Related Products of 329214-79-1.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Wang, Dan-Yang; Si, Yubing; Li, Junjie; Fu, Yongzhu published the artcile< Tuning the electrochemical behavior of organodisulfides in rechargeable lithium batteries using N-containing heterocycles>, Electric Literature of 2127-03-9, the main research area is organodisulfide tuning electrochem behavior rechargeable lithium battery.

S-S bonds in organodisulfides can break and obtain Li+ and e- in the discharge of lithium batteries. Organodisulfides provide precise lithiation sites, and therefore are valuable models for the study of redox reactions in lithium batteries. To understand their electrochem. behavior, we investigate three disulfides with different N-containing heterocycles including 2,2′-dipyridyl disulfide (2,2′-DpyDS), 4,4′-dipyridyl disulfide (4,4′-DpyDS), and 2,2′-dipyridyl disulfide-N,N’-dioxide (DpyDSDO). The three disulfides all show higher discharge voltage plateaus due to the electron-withdrawing groups: DPDS (2.20 V) < 2,2'-DpyDS (2.45 V) = 4,4'-DpyDS (2.45 V) < DpyDSDO (2.80 V). In particular, 2,2'-DpyDS exhibits an outstanding 69% capacity retention over 500 cycles. Our theor. simulations show that lithium pyridine-2-thiolate, the discharge product of 2,2'-DpyDS, forms compact clusters via N···Li···S bridges coordinated by lithium ions, which can help reduce its dissolution in liquid electrolyte, and therefore increase the cycle life. Liquid chromatog.-mass spectrometry is demonstrated to be a powerful tool for the investigation of discharge/recharge products of soluble organodisulfides in rechargeable lithium batteries. Journal of Materials Chemistry A: Materials for Energy and Sustainability published new progress about Battery cathodes. 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Electric Literature of 2127-03-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Kang, Yan-Shang; Zhang, Ping; Li, Min-Yan; Chen, You-Ke; Xu, Hua-Jin; Zhao, Jing; Sun, Wei-Yin; Yu, Jin-Quan; Lu, Yi published the artcile< Ligand-Promoted RhIII-Catalyzed Thiolation of Benzamides with a Broad Disulfide Scope>, Reference of 2127-03-9, the main research area is benzamide pentafluorophenyl disulfide rhodium amino acid regioselective thiolation catalyst; arylthio pentafluorophenyl benzamide preparation; amino acids; directing groups; disulfides; rhodium; thiolation.

A ligand-promoted RhIII-catalyzed C(sp2)-H activation/thiolation of benzamides has been developed. Using bidentate mono-N-protected amino acid ligands led to the first example of RhIII-catalyzed aryl thiolation reactions directed by weakly coordinating directing amide groups. The reaction tolerates a broad range of amides and disulfide reagents.

Angewandte Chemie, International Edition published new progress about Amino acids Role: CAT (Catalyst Use), USES (Uses). 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Reference of 2127-03-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Dong, Yuman; Liu, Peng published the artcile< Reduction-triggered di-block copolymer prodrug for high-performance long-acting tumor-selective killing>, Related Products of 2127-03-9, the main research area is acrylic polyoxyalkylene diblock progrug antitumor agent; Long-acting prodrug; Reduction-triggered drug delivery; Solubility-controlled release; Tumor-selective killing; Tumor-specific.

Long-acting drug delivery systems (DDSs) have attracted interests for tumor chemotherapy. Here, novel reduction-triggered polymer prodrug was designed by conjugation of a high-performance thiolated doxorubicin (DOX-SH) onto the diblock copolymer PEG43-PPDSM43 via the bioreducible cleavable disulfide bond. The resultant polymer prodrug PEG43-PPDSM43-DOX with a DOX content of 33% could be easily self-assembled into nanoparticles of 146 nm. They showed a slow solubility-controlled sustained drug release with a cumulative release of 30.13% within 84 h in the simulated tumor intracellular microenvironment but an ultra-low premature drug leakage of 4.01% in the simulated normal physiol. media. Such slow sustained release is expected to prolong the action time of the active drug. The MTT assays demonstrated the tumor-selective killing performance of the proposed prodrug nanoparticles with an enhanced antitumor efficacy on the tumor HepG2 cells than the free DOX, but no obvious cytotoxicity on the normal L20 cells at the lower dosages.

Colloids and Surfaces, B: Biointerfaces published new progress about Antitumor agents. 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Related Products of 2127-03-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Harenberg, Johannes H.; Weidmann, Niels; Knochel, Paul published the artcile< Preparation of Functionalized Aryl, Heteroaryl, and Benzylic Potassium Organometallics Using Potassium Diisopropylamide in Continuous Flow>, SDS of cas: 2127-03-9, the main research area is metalation continuous flow generation organopotassium aromatic hetaryl nucleophile; electrophile addition coupling organopotassium aromatic heterocyclic compound; alc ketone thioether silane preparation organopotassium nucleophile addition coupling; arenes; flow chemistry; heteroarenes; lateral metalation; potassium.

Heterocyclic and aromatic compounds were metalated by lithium-free potassium diisopropylamide serving as nucleophiles in carbonyl group addition and coupling reactions, providing access to versatile substituted benzothiazoles, benzothiophenes, benzofurans and functionalized aromatic compounds We report the preparation of lithium-salt-free KDA (potassium diisopropylamide; 0.6 M in hexane) complexed with TMEDA (N,N,N’,N’-tetramethylethylenediamine) and its use for the flow-metalation of (hetero)arenes between -78° and 25° with reaction times between 0.2 s and 24 s and a combined flow rate of 10 mL min-1 using a com. flow setup. The resulting potassium organometallics react instantaneously with various electrophiles, such as ketones, aldehydes, alkyl and allylic halides, disulfides, Weinreb amides, and Me3SiCl, affording functionalized (hetero)arenes in high yields. This flow procedure is successfully extended to the lateral metalation of methyl-substituted arenes and heteroaromatics, resulting in the formation of various benzylic potassium organometallics. A metalation scale-up was possible without further optimization.

Angewandte Chemie, International Edition published new progress about Alcohols Role: SPN (Synthetic Preparation), PREP (Preparation). 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, SDS of cas: 2127-03-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Liu, Juan; Yu, Yuhua; Zhao, Jie; Zhao, Peng; Wen, Xuejun; Zhuang, Zhigang; Lin, Chao published the artcile< Integrating disulfides into a polyethylenimine gene carrier selectively boosts significant transfection activity in lung tissue enabling robust IL-12 gene therapy against metastatic lung cancers>, HPLC of Formula: 2127-03-9, the main research area is integrating disulfide polyethylenimine interleukin human metastatic lung cancer; Disulfide; Interleukin-12; Metastatic lung cancer; Polyethylenimine; Transfection.

Bioreducible polyethylenimines (SSPEIs) are promising non-viral carriers for cancer gene therapy. However, the availability of significant gene transfection activity by SSPEIs remains a challenge. Herein, an essential step was taken to ascertain whether or not the disulfide bonds of SSPEIs play a critical role in promoting significant gene transfection activity in different tissues. Initially, a disulfide-linked linear polyethylenimine (denoted as SSLPEI) consisting of one 5.0 kDa LPEI main chain and three disulfide-linked 5.7 kDa LPEI grafts was designed and prepared to possess similar mol. weight with commercialized 25 kDa LPEI as a pos. control. The SSLPEI could induce superior in vitro transfection activity in different cells to the LPEI control as well as low cytotoxicity. Notably, such enhanced in vitro transfection effect by the SSLPEI was more marked in type-II alveolar epithelial cells compared to different cancer cells. In a Balb/c nude mouse model bearing SKOV-3 tumor, the SSLPEI caused parallel level of transgene expression with the LPEI control in the tumor but significantly higher level in the mouse lung. Furthermore, the SSLPEI and LPEI groups afforded an identical antitumor efficacy against the SKOV-3 tumor via i.v. delivery of a shRNA for silencing VEGF expression in the tumor. However, via i.v. delivery of an interleukin-12 (IL-12) gene into metastatic lung cancers in a C57BL/6 mouse model, the SSLPEI group exerted markedly higher IL-12 expression level in the mouse lung and peripheral blood as compared to the LPEI group, thereby boosting IL-12 immunotherapy against the lung metastasis with longer medium survival time. The results of this work elicit that the disulfide bonds of SSPEIs play a pivotal role in enhancing gene transfection activity selectively in the lung tissue rather than solid tumor, enabling high translational potential of SSPEIs for non-viral gene therapy against metastatic lung cancers.

Materials Science & Engineering, C: Materials for Biological Applications published new progress about Alveolar epithelium. 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, HPLC of Formula: 2127-03-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Nagata, Kojiro; Otsuji, Naoko; Akagi, Soichiro; Fujii, Sho; Kitamura, Noboru; Yoshimura, Takashi published the artcile< Synthesis, Structures, and Photoluminescent Properties of Tricyanidonitridorhenium(V) Complexes with Bipyridine-Type Ligands>, Application of C10H6Cl2N2, the main research area is crystal structure rhenium nitrido cyano substituted bipyridine; rhenium tricyanidonitrido bipyridine preparation electrochem redox luminescence charge transfer.

Tricyanidonitridorhenium(V) complexes with 2,2′-bipyridine (bpy) derivatives in which the 4 and 4′ positions were substituted by X, [ReN(CN)3(X2bpy)]- (X = NMe2, NH2, OMe, Me, Cl, and Br), were newly synthesized and characterized. The structures of the new complexes were determined by single-crystal x-ray anal. UV-visible spectra of the complexes in DMSO showed that the peak maximum wavelengths of Re-to-π* bpy-type-ligand charge transfer were at 474-542 nm. Cyclic voltammograms in Bu4NPF6-DMSO showed 1-electron oxidation and reduction waves corresponding to the Re(VI/V) and X2bpy0/- processes, resp. The new complexes and [ReN(CN)3bpy]- showed photoluminescence in the crystalline phase at 295 and 80 K and in DMSO at 295 K. The origin of the emission in DMSO was attributed to the triplet nature of the Re-to-π* bpy-type-ligand charge-transfer transition. D. functional theory calculations showed that the highest occupied and lowest unoccupied MOs were primarily localized on the dxy orbital of the Re and π* orbitals of the bpy-type ligand, resp. Tricyanidonitridorhenium(V) complexes with 2,2′-bipyridine (bpy) derivatives were newly synthesized and characterized. The new complexes and [ReN(CN)3bpy]- showed photoluminescence. The origin of the emission was attributed to the triplet nature of the Re-to-π* bpy-derivative charge-transfer transition.

Inorganic Chemistry published new progress about Charge transfer transition. 1762-41-0 belongs to class pyridine-derivatives, and the molecular formula is C10H6Cl2N2, Application of C10H6Cl2N2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem