Day: October 14, 2022

Lam, Hung Thanh; Le-Vinh, Bao; Phan, Thi Nhu Quynh; Bernkop-Schnuerch, Andreas published the artcile< Self-emulsifying drug delivery systems and cationic surfactants: do they potentiate each other in cytotoxicity>, Computed Properties of 123-03-5, the main research area is self emulsifying drug delivery system cationic surfactant; alkyltrimethylammonium bromide; benzalkonium chloride; cationic surfactant; cytotoxicity; self-emulsifying drug delivery systems.

The aim of this study was to evaluate the cytotoxicity of self-emulsifying drug delivery systems (SEDDS) containing five different cationic surfactants. Cationic surfactants were added in a concentration of 1% and 5% (m/m) to SEDDS comprising 30% Capmul MCM, 30% Captex 355, 30% Cremophor EL and 10% propylene glycol. The resulting formulations were characterized in terms of size, zeta potential, in-vitro haemolytic activity and toxicity on Caco-2 via MTT assay and lactate dehydrogenase release assay. The evaluated surfactants had in both concentrations a minor impact on the size of SEDDS ranging from 30.2 ± 0.6 to 55.4 ± 1.1 nm, whereas zeta potential changed significantly from -9.0 ± 0.3 to +28.8 ± 1.6 mV. The overall cytotoxicity of cationic surfactants followed the rank order: hexadecylpyridinium chloride > benzalkonium chloride > alkyltrimethylammonium bromide > octylamine > 1-decyl-3-methylimidazolium. The haemolytic activity of the combination of cationic surfactants and SEDDS on human red blood cells was synergistic. Furthermore, cationic SEDDS exhibited higher cytotoxicity of Caco-2 cells compared to SEDDS without cationic surfactants. According to these results, SEDDS and cationic surfactants seem to bear an additive up to synergistic toxic risk.

Journal of Pharmacy and Pharmacology published new progress about Castor oil, ethoxylated Role: MOA (Modifier or Additive Use), USES (Uses). 123-03-5 belongs to class pyridine-derivatives, and the molecular formula is C21H38ClN, Computed Properties of 123-03-5.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Ziolkowska, Dorota; Syrotynska, Iryna; Shyichuk, Alexander; Lamkiewicz, Jan published the artcile< Determination of SLES in personal care products by colloid titration with light reflection measurements>, Quality Control of 3811-73-2, the main research area is sodium laureth sulfate personal care product colloid titration; PDADMAC; PDDA; cationic polymer; polyDADMAC; quantitation of surfactants; turbidity.

The method of colloid titration with poly(diallyldimethylammonium) chloride has been improved to detect the endpoint with an off-vessel light reflectance sensor. The digital color sensor used measures light reflectance by means of light guides, with no immersion into the reaction solution In such a method, the optical signal is free of disturbances caused by sticky flocs in the solution The improved automatic titration set was applied for the determination of sodium laureth sulfate (SLES) in industrial batches and com. personal care products. The sample color and opacity do not disturb the SLES quantification. When the SLES content lies in the range from 5% to 9%, the optimal sample weight is from 6 g to 3 g.

Molecules published new progress about Almond. 3811-73-2 belongs to class pyridine-derivatives, and the molecular formula is C5H4NNaOS, Quality Control of 3811-73-2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Sardaru, Monica-Cornelia; Craciun, Anda Mihaela; Al Matarneh, Cristina-Maria; Sandu, Isabela Andreea; Amarandi, Roxana Maria; Popovici, Lacramioara; Ciobanu, Catalina Ionica; Peptanariu, Dragos; Pinteala, Mariana; Mangalagiu, Ionel I.; Danac, Ramona published the artcile< Cytotoxic substituted indolizines as new colchicine site tubulin polymerisation inhibitors>, Product Details of C10H8N2, the main research area is indolizine derivative preparation colchicine tubulin polymerization inhibitor cancer; Indolizine; Phenstatin; anticancer; pyridyl; tubulin polymerisation inhibitors.

A potential microtubule destabilizing series of new indolizine derivatives was synthesized and tested for their anticancer activity against a panel of 60 human cancer cell lines. the compounds showed a broad spectrum of growth inhibitory activity against cancer cell lines representing leukemia, melanoma and cancer of lung, colon, central nervous system, ovary, kidney, breast, and prostate. Among them, compound was distinguishable by its excellent cytostatic activity, showing GI50 values in the range of 10-100 nM on 43 cell lines. The less potent compounds and in terms of GI50 values showed a high cytotoxic effect against tested colon cancer, CNS cancer, renal cancer and melanoma cell lines and only on few cell lines from other types of cancer. In vitro assaying revealed tubulin polymerization inhibition by all active compounds Mol. docking showed good complementarity of active compounds with the colchicine binding site of tubulin.

Journal of Enzyme Inhibition and Medicinal Chemistry published new progress about Antitumor agents. 581-47-5 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2, Product Details of C10H8N2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

He, Yu-Ping; Cao, Jian; Wu, Hua; Wang, Qian; Zhu, Jieping published the artcile< Catalytic Enantioselective Aminopalladation-Heck Cascade>, Application In Synthesis of 1416819-91-4, the main research area is alkynylaniline cyclopentene diastereoselective enantioselective palladium pyrox aminopalladation Heck cascade; indole cyclopentene stereoselective preparation; asymmetric synthesis; domino reactions; homogeneous catalysis; nucleopalladation; oxidative Heck reactions.

Domino processes initiated by intramol. nucleopalladation of alkynes have been developed into powerful synthetic tools for the synthesis of functionalized heterocycles. However, a catalytic enantioselective version of this class of reactions remains scarce. We report herein that reaction of 2-alkynylanilines with prochiral cyclopentenes in the presence of a catalytic amount of Pd(OAc)2, a chiral bidentate pyrox ligand and O2 as terminal oxidant affords the structurally diverse indole-cyclopentene conjugates, e.g., I, bearing two stereocenters in a highly diastereo- and enantio-selective manner. One of the products is converted to a heavily functionalized tetracyclic indolinone derivative

Angewandte Chemie, International Edition published new progress about Addition reaction, aminopalladation. 1416819-91-4 belongs to class pyridine-derivatives, and the molecular formula is C13H15F3N2O, Application In Synthesis of 1416819-91-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Ciriano, Miguel A.; Perez-Torrente, Jesus J.; Oro, Luis A. published the artcile< Synthesis and reactivity of binuclear 7-azaindolate complexes of iridium. II. Oxidative-addition reactions of halogens and halocarbons to [{Ir(μ-aza)(CO)2}2]>, COA of Formula: C7H5BrN2, the main research area is azaindolate iridium complex oxidative addition; halogen oxidative addition azaindolate iridium complex; halocarbon oxidative addition azaindolate iridium complex; pyrrolopyridinate iridium complex oxidative addition.

The compound [{Ir(μ-aza)(CO)2}2] (1, aza = 7-azaindolate) is oxidized by AgBF4 in a donor solvent to [{Ir(μ-aza)(CO)2(S)}2]2+ (S = Me2CO, MeCN) and to the neutral complex [{Ir(μ-aza)(CO)2(O2CMe)}2] (2) by silver acetate. The head-to-tail (HT) and the head-to-head (HH) isomers of 1 undergo trans-annular oxidative-addition reactions with a variety of substrates. Halogens (X2) add to 1 giving the diiridium(II) complexes [{Ir(μ-aza)X(CO)2}2] (X = Cl (3), Br, iodo). In addition, bromine selectively attacks position 3 of the five-membered ring in the aza bridges, affording [{Ir(μ-azaBr)Br(CO)2}2] as a single isomer. MeI and polyiodomethanes react with both isomers of 1 to give the iodomethyl complexes [{Ir(μ-aza)(CO)2}2(I)(R)] (R = Me, CH2I, CHI2, or (CH2)3I) as a mixture of isomers. The relative disposition, HH and HT, of the bridging ligands is maintained in these reactions. Complex 1 is a powerful photoreductor that reacts with CHCl3 and CCl4 giving [{Ir(μ-aza)(CO)2}2(Cl)(R)] (R = CHCl2 or CCl3), resp., whereas compound 3 results from reaction with 1,2-dichloroethane. Reactions of complex 1 with di-Et acetylenedicarboxylate and di-Me acetylenedicarboxylate (A) afford the tetranuclear complexes of the type [{Ir(μ-aza)(CO)2}4(A)2].

Journal of Organometallic Chemistry published new progress about Oxidative addition reaction. 23612-36-4 belongs to class pyridine-derivatives, and the molecular formula is C7H5BrN2, COA of Formula: C7H5BrN2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Matesanz, Encarna; Alcazar, Jesus; Andres, J. Ignacio; Bartolome, Jose M.; De Bruyn, Marcel; Fernandez, Javier; Van Emelen, Kristof published the artcile< Synthesis of novel aza analogues of 2-substituted-2,3-dihydro-1,4-benzodioxins as potential new scaffolds for drug discovery>, Application of C5H4ClNO, the main research area is benzodioxin aza analog preparation.

New synthesis approaches that have led to a series of novel aza analogs of the 2-substituted-2,3-dihydro-1,4-benzodioxin core, bearing versatile bromomethyl group on the non aromatic oxygenated ring, are described. According to their structures these novel scaffolds can be useful intermediates for the preparation of potential new therapeutic agents.

Tetrahedron Letters published new progress about Cyclization, regioselective. 96630-88-5 belongs to class pyridine-derivatives, and the molecular formula is C5H4ClNO, Application of C5H4ClNO.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Lepeltier, Marc; Dumur, Frederic; Marrot, Jerome; Contal, Emmanuel; Bertin, Denis; Gigmes, Didier; Mayer, Cedric R. published the artcile< Unprecedented combination of regioselective hydrodefluorination and ligand exchange reaction during the syntheses of tris-cyclometalated iridium(III) complexes>, Computed Properties of 370878-69-6, the main research area is fluoropyridine cyclometalated iridium complex preparation unprecedented regioselective hydrodefluorination ligand; crystal mol structure tris fluoropyridine cyclometalated iridium complex.

The first reported combination of regioselective hydro-defluorination and a ligand exchange reaction during the syntheses of neutral iridium(III) complexes is presented. Surprisingly, loss of one fluorine atom per ligand combined with a complete ligand exchange reaction on the transition metal were jointly observed during a bridge-splitting and substitution reaction of two different dimeric iridium(III) precursor complexes with two different ancillary ligands. The regioselectivity of defluorination was evidenced in both cases. The reaction time was identified as a factor strongly impacting the kinetics of the thermally induced reaction.

Dalton Transactions published new progress about Coordinative substitution reaction. 370878-69-6 belongs to class pyridine-derivatives, and the molecular formula is C33H21F3IrN3, Computed Properties of 370878-69-6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

An, Yunfei; Dong, Yue; Liu, Min; Han, Jun; Zhao, Liyu; Sun, Bin published the artcile< Novel naphthylamide derivatives as dual-target antifungal inhibitors: Design, synthesis and biological evaluation>, Application In Synthesis of 3731-53-1, the main research area is naphthylamide imidazole preparation antifungal activity mol docking SAR; squalene epoxidase cytochrome P450 enzyme inhibitor; Antifungal activity; Dual-target; Fungal infections; Inhibitors; Organic synthesis.

In the study, a series of active fragments were screened through the method of De Novo Link, and these active fragments with the higher Ludi_Scores were selected, which can show the obvious binding ability with the dual targets (SE, CYP51). Subsequently, three series of target compounds with naphthyl amide scaffolds were constructed by connecting these core fragments, and their structures were synthesized. Most of compounds showed the antifungal activity in the treatment of pathogenic fungi. It was worth noting that compoundsI [R = pyridin-4-ylmethyl] and II [R = methyl] with the excellent broad-spectrum antifungal properties also exhibited the obvious antifungal effects against drug-resistant fungi. Preliminary mechanism study has proved these target compounds can block the biosynthesis of ergosterol by inhibiting the activity of dual targets (SE, CYP51). Furthermore, target compounds I [R = pyridin-4-ylmethyl] and II [R = methyl] with low toxicity side effects also demonstrated the excellent pharmacol. effects in vivo. The mol. docking and ADMET prediction were performed, which can guide the optimization of subsequent lead compounds

European Journal of Medicinal Chemistry published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 3731-53-1 belongs to class pyridine-derivatives, and the molecular formula is C6H8N2, Application In Synthesis of 3731-53-1.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Eremina, Julia A.; Lider, Elizaveta V.; Samsonenko, Denis G.; Sheludyakova, Liliya A.; Berezin, Alexey S.; Klyushova, Lyubov S.; Ostrovskii, Vladimir A.; Trifonov, Rostislav E. published the artcile< Mixed-ligand copper(II) complexes with tetrazole derivatives and 2,2'-bipyridine, 1,10-phenanthroline: Synthesis, structure and cytotoxic activity>, Category: pyridine-derivatives, the main research area is crystal structure copper phenanthroline bipyridine tetrazole; copper phenanthroline bipyridine phenyltetrazole tetrazole preparation cytotoxicity human.

The [Cu2(2,2′-bipy)2(L1)4] (1), [Cu2(1,10-phen)2(L1)4] (2), [Cu(2,2′-bipy)(L2)2]n (3) and [Cu2(1,10-phen)2(L2)4] (4) complexes, where HL1 – 5-phenyltetrazole, and HL2 – 1H-tetrazole, were synthesized. All complexes were characterized by elemental anal., IR, EPR spectroscopy and x-ray diffraction. The complexes possess distorted tetragonal-pyramidal coordination geometry. Compounds 1, 2, and 4 show μ-5-phenyl-tetrazole/tetrazole bridged dinuclear structures, while compound 3 reveals polymeric structure. The effect of the compounds on viability of the MCF-7 and Hep-2 cell lines was studied in vitro. Tetrazole ligands HL1 and HL2 are nontoxic at tested concentrations (1-50 μM), while 1,10-phen and 2,2′-bipy possess cytotoxicity. All of the complexes exhibit significant dose-dependent cytotoxic effect and have the potential to act as efficient cytotoxic drugs. [Cu(1,10-phen)Cl2] (5) and [Cu(2,2′-bipy)Cl2] (6) also were obtained to establish the influence of insertion of tetrazole ligands in compounds on their cytotoxic properties.

Inorganica Chimica Acta published new progress about Antitumor agents. 366-18-7 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Shirazi, Seyed Mohammad Hossein; Mokhtari, Javad; Mirjafary, Zohreh published the artcile< A new method for the synthesis of abiraterone drug catalyzed by Pd-NPs@Zn-MOF as efficient reusable catalyst>, Related Products of 329214-79-1, the main research area is abiraterone palladium nanoparticle heterogeneous catalyst Suzuki Miyaura.

The present work provides a novel process for the preparation of abiraterone drug in a Suzuki-Miyaura coupling approach by a new heterogeneous palladium catalyst, Pd-NPs@Zn-MOF, which has been synthesized by one-step encapsulation in nanoporous metal-organic framework Zn-MOF under a temperature control program for the first time. Pd-NPs@Zn-MOF were characterized by transmission electron microscopy (TEM), X-Ray powder diffraction (XRD), BET surface area anal., inductively coupled plasma (ICP)-optical emission spectrometry (OES), and XPS.

Applied Organometallic Chemistry published new progress about Emission spectroscopy. 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