Month: April 2022

Zhang, Tinghu; Kwiatkowski, Nicholas; Olson, Calla M.; Dixon-Clarke, Sarah E.; Abraham, Brian J.; Greifenberg, Ann K.; Ficarro, Scott B.; Elkins, Jonathan M.; Liang, Yanke; Hannett, Nancy M.; Manz, Theresa; Hao, Mingfeng; Bartkowiak, Bartlomiej; Greenleaf, Arno L.; Marto, Jarrod A.; Geyer, Matthias; Bullock, Alex N.; Young, Richard A.; Gray, Nathanael S. published an article about the compound: 3-(2,5-Dichloropyrimidin-4-yl)-1-(phenylsulfonyl)-1H-indole( cas:882562-40-5,SMILESS:ClC1=NC(C2=CN(C3=C2C=CC=C3)S(=O)(=O)C2=CC=CC=C2)=C(Cl)C=N1 ).SDS of cas: 882562-40-5. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:882562-40-5) through the article.

Cyclin-dependent kinases 12 and 13 (CDK12 and CDK13) play critical roles in the regulation of gene transcription. However, the absence of CDK12 and CDK13 inhibitors has hindered the ability to investigate the consequences of their inhibition in healthy cells and cancer cells. Here we describe the rational design of a first-in-class CDK12 and CDK13 covalent inhibitor, THZ531. Co-crystallization of THZ531 with CDK12-cyclin K indicates that THZ531 irreversibly targets a cysteine located outside the kinase domain. THZ531 causes a loss of gene expression with concurrent loss of elongating and hyperphosphorylated RNA polymerase II. In particular, THZ531 substantially decreases the expression of DNA damage response genes and key super-enhancer-associated transcription factor genes. Coincident with transcriptional perturbation, THZ531 dramatically induced apoptotic cell death. Small mols. capable of specifically targeting CDK12 and CDK13 may thus help identify cancer subtypes that are particularly dependent on their kinase activities.

When you point to this article, it is believed that you are also very interested in this compound(882562-40-5)SDS of cas: 882562-40-5 and due to space limitations, I can only present the most important information.

Reference:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

Kukushkin, V. Yu.; Tkachuk, V. M. published an article about the compound: cis-Dichlorobis(pyridine)platinum(II)( cas:15227-42-6,SMILESS:[Cl-][Pt+2]([N]1=CC=CC=C1)([Cl-])[N]2=CC=CC=C2 ).Formula: C10H10Cl2N2Pt. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:15227-42-6) through the article.

[Ph3PCH2Ph]2[PtXCl3] (X = Cl, NO2) are oxidized by Sb(BzCl)Cl5 (I) or Et3NCH2Ph[SbCl6] (II) in MeNO2, MeCN or DMF to give (Ph3PCH2Ph)2[PtXCl5]. SbCl5 oxidizes cis- and trans-Pt(py)2Cl2 to give cis- and trans-[Pt(py)2Cl4], resp. I oxidizes trans-[Pt(NH2CH2CO2H)2Cl2] to give trans-[Pt(NH2CH2CO2H)2Cl4] which on reaction with PCl5 in MeCN gives trans-[Pt(NH2CH2COCl)2Cl4]. [Pt(py)4]Cl2 reacted with I to give trans-[Pt(py)2Cl4]. cis- And trans-[PtL2Cl2] (L = PPh3, SMe2) are not oxidized by I or II.

When you point to this article, it is believed that you are also very interested in this compound(15227-42-6)Formula: C10H10Cl2N2Pt and due to space limitations, I can only present the most important information.

Reference:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

Lucier, Bryan E. G.; Reidel, Alex R.; Schurko, Robert W. published an article about the compound: cis-Dichlorobis(pyridine)platinum(II)( cas:15227-42-6,SMILESS:[Cl-][Pt+2]([N]1=CC=CC=C1)([Cl-])[N]2=CC=CC=C2 ).Category: tetrahydroisoquinoline. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:15227-42-6) through the article.

Multinuclear solid-state NMR (SSNMR) experiments were performed on cisplatin and four related square-planar compounds The wideband uniform rate smooth truncation-Carr-Purcell-Meiboom-Gill (WURST-CPMG) pulse sequence was used in NMR experiments to acquire 195Pt, 14N, and 35Cl ultra-wideline NMR spectra of high quality. Standard Hahn-echo and magic-angle spinning 195Pt NMR experiments are also performed to refine extracted chem. shielding (CS) tensor parameters. Platinum magnetic shielding (MS) tensor orientations are calculated using both plane-wave d. functional theory (DFT) and standard DFT methods. The tensor orientations are highly constrained by mol. symmetry elements, but also influenced to some degree by intermol. interactions. 14N WURST-CPMG experiments were performed on three compounds and elec. field gradient (EFG) parameters (the quadrupolar coupling constant, Cq, and the asymmetry parameter, ηq) are reported. First principles calculations of the 14N EFG tensor parameters and orientations and affirm their dependence on the local hydrogen bonding environment. 35Cl WURST-CPMG experiments on cisplatin and transplatin are reported, using two different static magnetic fields to extract EFG and CS tensor parameters, and 35Cl EFG tensor magnitudes and orientations are predicted using 1st principles calculations Transverse (T2) relaxation data for all nuclei were used to study heteronuclear dipolar relaxation mechanisms, as well as the nature of the local hydrogen bonding environments.

When you point to this article, it is believed that you are also very interested in this compound(15227-42-6)Category: tetrahydroisoquinoline and due to space limitations, I can only present the most important information.

Reference:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 1-Bromoundecane( cas:693-67-4 ) is researched.Recommanded Product: 1-Bromoundecane.Congdon, Molly; Fritzemeier, Russell G.; Kharel, Yugesh; Brown, Anne M.; Serbulea, Vlad; Bevan, David R.; Lynch, Kevin R.; Santos, Webster L. published the article 《Probing the substitution pattern of indole-based scaffold reveals potent and selective sphingosine kinase 2 inhibitors》 about this compound( cas:693-67-4 ) in European Journal of Medicinal Chemistry. Keywords: alkylindolyl oxadiazolylpyrrolidine preparation sphingosine kinase inhibition SAR mol docking; Molecular docking; SAR; SphK2; Sphingosine; Sphingosine 1-phosphate; Sphingosine kinase. Let’s learn more about this compound (cas:693-67-4).

Elevated levels of sphingosine 1-phosphate (S1P) and increased expression of sphingosine kinase isoforms (SphK1 and SphK2) have been implicated in a variety of disease states including cancer, inflammation, and autoimmunity. Selective inhibition of either SphK1 or SphK2 has been demonstrated to be effective in modulating S1P levels in animal models. Previously, authors reported a SphK2 naphthalene-based selective inhibitor, (R)-2-(3-(7-(pentyloxy)naphthalen-2-yl)-1,2,4-oxadiazol-5-yl)pyrrolidine-1-carboximidamide hydrochloride, which displays approx. 7-fold selectivity for hSphK2 over hSphK1 and has a SphK2 Ki value of 1.0μM. To improve SphK2 potency and selectivity, author’s designed, synthesized, and evaluated a series of indole-based compounds derived from (R)-2-(3-(7-(pentyloxy)naphthalen-2-yl)-1,2,4-oxadiazol-5-yl)pyrrolidine-1-carboximidamide hydrochloride. After investigating substitution patterns around the indole ring, author’s discovered that 1,5-disubstitution promoted optimal binding in the SphK2 substrate binding site and subsequent inhibition of enzymic activity. Author’s studies led to the identification of I (SphK2 Ki = 90 nM, >110 fold selective for SphK2 over SphK1). Mol. modeling studies revealed key nonpolar interactions with Val308, Phe548, His556, and Cys533 and hydrogen bonds with both Asp211 and Asp308 as responsible for the high SphK2 inhibition and selectivity.

When you point to this article, it is believed that you are also very interested in this compound(693-67-4)Recommanded Product: 1-Bromoundecane and due to space limitations, I can only present the most important information.

Reference:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: cis-Dichlorobis(pyridine)platinum(II)(SMILESS: [Cl-][Pt+2]([N]1=CC=CC=C1)([Cl-])[N]2=CC=CC=C2,cas:15227-42-6) is researched.Quality Control of cis-Dichlorobis(pyridine)platinum(II). The article 《The separation of nonelectrolytic geometric isomers of platinum(II) by thin-layer chromatography》 in relation to this compound, is published in Inorganic Chemistry. Let’s take a look at the latest research on this compound (cas:15227-42-6).

Microscope slides (75 × 25 mm.) were cleaned with detergent, rinsed in H2O, and coated with a slurry containing 1 part Silica Gel G in 3 parts of a 1:1 volume mixture of MeOH and redistilled CH2Cl2. The plates were air dried for 10-20 min. and activated for 1 hr. at 110°. Saturated solutions of the cis isomers, trans isomers, and a 1:1 by weight mixture of both Pt isomers in CH2Cl2 were applied to the plate. The plate was air dried for 2-3 min. and then developed with an ascending technique until the solvent had attained ∼6 cm. The plate was then air dried and the intense yellow-spots detected in a screw-cap jar containing I. The difference of the cis and trans migrations. ΔRf, indicated the effectiveness of separation For [Pt(Et2S)2Cl2] developed in C6H6, CH2Cl2, and 19:1 mixture of C6H6:Me2CO, ΔRf was 0.45, 0.45, and 0.45, resp. For [Pt(Bu3P)2Cl2] developed in C6H6, CH2Cl2, and a 1:1 mixture of C6H6:CH2Cl2 ΔRf was 0.95, 0.55 and 0.80, resp. For [Pt(pyridine)2Cl2] developed in CH2Cl2, 5:1 of C6H6:Me2CO Me2CO, and 5:1 of CH2Cl2:Me2CO ΔRf was 0.20, 0.45, and 0.35 resp. For [(Pr3P)2Pt2(PhS)2Cl2] developed in C6H6 and CH2Cl2 ΔRf was 0.40 and 0.45, resp. For [(Pr3P)2Pt(EtS)2Cl2] developed in CH2Cl2, 1:2 of C6H6:CH2Cl2, and C6H6 ΔRf was 0.40, 0.40, and 0.30, resp. For [Pr3P)2Pt2(p-O2NC6H4S)2Cl2] developed in CH2Cl2 and 2:1 of C6H6:Me2CO ΔRf was 0.30, 0.20, and 0.10, resp. Two (200 × 100 mm.) silica gel plates were prepared A mixture of 100 mg. cis and 100 mg. trans [Cl2Pt(PBu3)2] in CH2Cl2 were applied to the plates and developed with C6H6. The bands at Rf 0.0-0.1 and 0.85-0.10 were removed and eluted with Me2CO and CH2Cl2, resp. Evaporation yielded 91% cis isomer and 93% trans isomer. Thus, complete separation had been achieved with solvent induced isomerization.

When you point to this article, it is believed that you are also very interested in this compound(15227-42-6)Name: cis-Dichlorobis(pyridine)platinum(II) and due to space limitations, I can only present the most important information.

Reference:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

Quality Control of cis-Dichlorobis(pyridine)platinum(II). The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: cis-Dichlorobis(pyridine)platinum(II), is researched, Molecular C10H10Cl2N2Pt, CAS is 15227-42-6, about Interaction of cis platinum(II) compounds with poly(L-glutamate). A doubly anchored spin-label and a doubly anchored chromophore-label. Author is Chao, Yen Yau H.; Holtzer, Alfred; Mastin, Stephen H..

The free-radical 4-amino-2,2,6,6-tetramethylpiperidinyl-1-oxy [14691-88-4] yields cis-Pt(ATMPO)2(NO3)2 [64716-94-5], which is used to label poly(L-glutamate) (I), poly(L-aspartate) (II), and poly(L-lysine) (III). Labeling occurs by displacement of nitrate by polymer side chains. EPR spectra of oriented films of labeled I are strongly anisotropic; several arguments suggest that the major cause is g anisotropy. Spectra of solutions, in several solvents, of labeled I are also anisotropic and monitor the helix-coil transition and polymer aggregation. Since monofunctional, side-chain labels show only isotropic motions, Pt must be bifunctionally anchored to adjacent carboxylates, requiring the label to follow backbone segmental motions. With shorter side chains (II) adjacent double anchoring is impossible; with longer side chains (III), flexibility reduces coupling to backbone motion; in each, therefore, spectra are isotropic. Chromophoric compounds, particularly cis-Pt(bipy)(H2O)2][NO3]2 [64800-95-9], are similarly used. Bifunctional attachment is evidenced by the absence of base-induced UV spectral shifts (characteristic of attachment of OH- to Pt) shown by label alone, and by similarity of the spectra of labeled polymer and labeled oxalate. Induced CD appears for α helix in the region of the chromophore π-π* bands; transition to random coil drastically reduces this CD. With extensively labeled polymer differences in the course of the helix-coil transition as monitored by CD in the backbone region with that monitored in the chromophore region show that the label stabilizes its attached helical residue. A study of Corey-Pauling-Koltun models and extant theories suggests that the induced CD arises by coupling of the carboxylate π-π* and the bound chromophore 1B1 elec. transition moments.

When you point to this article, it is believed that you are also very interested in this compound(15227-42-6)Quality Control of cis-Dichlorobis(pyridine)platinum(II) and due to space limitations, I can only present the most important information.

Reference:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

Reference of Picolinamide. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: Picolinamide, is researched, Molecular C6H6N2O, CAS is 1452-77-3, about Ethene-1,1,2,2-tetracarbonitrile and Methanol in the Methylating Reaction of Tertiary Amines to the Quaternary Ammonium Compounds of 1,1-Dicyano-2-methoxy-2-oxoethane-1-ide. Author is Sheverdov, Vladimir P.; Davydova, Vera V.; Nasakin, Oleg E.; Mar’yasov, Maksim A.; Lodochnikova, Olga A..

We discovered a new method to methylate tertiary amines such as urotropine, triethylamine, pyridine, 2-methylpyridine, 4-acetylpyridine, and isonicotinamide, to quaternary ammonium compounds, with 1,1-dicyano-2-methoxy-2-oxoethane-1-ide being the counterion. Methyl-1,3,5,7-tetraazaadamantan-1-ium 1,1-dicyano-2-methoxy-2-oxoethane-1-ide, N,N-diethyl-N-methylethanaminium 1,1-dicyano-2-methoxy-2-oxoethane-1-ide, and substituted-methylpyridinium 1,1-dicyano-2-methoxy-2-oxoethane-1-ides were synthesized. Quaternary ammonium compounds of 1,1-dicyano-2-methoxy-2-oxothane-1-ide were synthesized within a single stage by stirring methanol solutions of tertiary amines with ethene-1,1,2,2-tetracarbonitrile (ETCN) at room temperature In the reaction of ETCN with tertiary amines in methanol, processes occur that form the 1,1-dicyano-2-methoxy-2-oxoethane-1-ide fragment with simultaneous N-methylation. Crystal structures based on X-ray diffraction anal. of the obtained compounds were studied.

When you point to this article, it is believed that you are also very interested in this compound(1452-77-3)Reference of Picolinamide and due to space limitations, I can only present the most important information.

Reference:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

Recommanded Product: 4-Chloro-4′-ethynyl-1,1′-biphenyl. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: 4-Chloro-4′-ethynyl-1,1′-biphenyl, is researched, Molecular C14H9Cl, CAS is 57399-11-8, about Discovery of a novel series of N-hydroxypyridone derivatives protecting astrocytes against hydrogen peroxide-induced toxicity via improved mitochondrial functionality. Author is Singh, Sarbjit; Goo, Ja-Il; Noh, Hyojin; Lee, Sung Jae; Kim, Myoung Woo; Park, Hyejun; Jalani, Hitesh B.; Lee, Kyeong; Kim, Chunsook; Kim, Won-Ki; Ju, Chung; Choi, Yongseok.

Astrocytes play a key role in brain homeostasis, protecting neurons against neurotoxic stimuli such as oxidative stress. Therefore, the neuroprotective therapeutics that enhance astrocytic functionality has been regarded as a promising strategy to reduce brain damage. We previously reported that ciclopirox, a well-known antifungal N-hydroxypyridone compound, protects astrocytes from oxidative stress by enhancing mitochondrial function. Using the N-hydroxypyridone scaffold, we have synthesized a series of cytoprotective derivatives Mitochondrial activity assay showed that N-hydroxypyridone derivatives with biphenyl group have comparable to better protective effects than ciclopirox in astrocytes exposed to H2O2. N-hydroxypyridone derivatives, especially 11g, inhibited H2O2-induced deterioration of mitochondrial membrane potential and oxygen consumption rate, and significantly improved cell viability of astrocytes. The results indicate that the N-hydroxypyridone motif can provide a novel cytoprotective scaffold for astrocytes via enhancing mitochondrial functionality.

When you point to this article, it is believed that you are also very interested in this compound(57399-11-8)Recommanded Product: 4-Chloro-4′-ethynyl-1,1′-biphenyl and due to space limitations, I can only present the most important information.

Reference:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. Compound: 4-Chloro-4′-ethynyl-1,1′-biphenyl, is researched, Molecular C14H9Cl, CAS is 57399-11-8, about Chemodivergent Synthesis of One-Carbon-Extended Alcohols via Copper-Catalyzed Hydroxymethylation of Alkynes with Formic Acid.Formula: C14H9Cl.

Here an intriguing strategy for the chemodivergent copper-catalyzed hydroxymethylation of alkynes RCCR1 (R = Ph, cyclopropyl, thiophen-2-yl, etc.; R1 = Ph, H, 3-fluorophenyl, 2-fluorophenyl, etc.) and R2CCH [R2 = 4-(4-methylphenyl)phenyl, 4-(4-fluorophenyl)phenyl, 4-(thiophen-2-yl)phenyl, etc.] and 9-ethynylphenanthrene with formic acid and hydrosilane has been developed. By simply tuning the amount of formic acid and reaction temperature, distinct one-carbon-extended primary alcs., i.e., allylic alcs. (E)/(Z)-RCH=C(R1)CH2OH and β-branched alkyl alcs., (S)-R2CH(CH3)CH2OH and (S)-2-(phenanthren-9-yl)propan-1-ol were produced with high levels of Z/E-, regio-, and enantioselectivity.

When you point to this article, it is believed that you are also very interested in this compound(57399-11-8)Formula: C14H9Cl and due to space limitations, I can only present the most important information.

Reference:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

Product Details of 15227-42-6. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: cis-Dichlorobis(pyridine)platinum(II), is researched, Molecular C10H10Cl2N2Pt, CAS is 15227-42-6, about Nucleophilic displacement of the chelating bis(sulfoxide) from cis-[meso-1,2-bis(phenylsulfinyl)ethane]dichloroplatinum(II) and cis-[rac-1,2-bis(phenylsulfinyl)ethane]dichloroplatinum(II). Author is Cattalini, Lucio; Marangoni, Giampaolo; Michelon, Gianni; Paolucci, Gino; Tobe, Martin L..

The kinetics were measured for ring opening of the title Pt complex isomers by amines in 1,2-dimethoxyethane solutions The results are used in a discussion of the differences between the 2 isomers in comparison with other Pt(II) complexes in terms of absolute reactivity, nucleophilic discrimination, and steric retardation effects.

When you point to this article, it is believed that you are also very interested in this compound(15227-42-6)Product Details of 15227-42-6 and due to space limitations, I can only present the most important information.

Reference:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem