Month: April 2022

The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: Picolinamide(SMILESS: O=C(N)C1=NC=CC=C1,cas:1452-77-3) is researched.Category: tetrahydroisoquinoline. The article 《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》 in relation to this compound, is published in Synlett. Let’s take a look at the latest research on this compound (cas:1452-77-3).

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.

In addition to the literature in the link below, there is a lot of literature about this compound(Picolinamide)Application In Synthesis of Picolinamide, illustrating the importance and wide applicability of this compound(1452-77-3).

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: Picolinamide( cas:1452-77-3 ) is researched.Category: tetrahydroisoquinoline.Chen, Chao-Cheng; Chen, Yang-Yi; Lo, Yi-Hsuan; Lin, Ming-Hsien; Chang, Chih-Hsien; Chen, Chuan-Lin; Wang, Hsin-Ell; Wu, Chun-Yi published the article 《Evaluation of radioiodinated fluoronicotinamide/fluoropicolinamide-benzamide derivatives as theranostic agents for melanoma》 about this compound( cas:1452-77-3 ) in International Journal of Molecular Sciences. Keywords: melanoma theranostic agent radioiodinated fluoronicotinamide fluoropicolinamide benzamide; 131I-iodofluoronicotiamide benzamide (131I-IFNABZA); 131I-iodofluoropicolinamide benzamide (131I-IFPABZA); melanoma; theranostic agent. Let’s learn more about this compound (cas:1452-77-3).

Malignant melanoma is the most harmful type of skin cancer and its incidence has increased in this past decade. Early diagnosis and treatment are urgently desired. In this study, we conjugated picolinamide/nicotinamide with the pharmacophore of 131I-MIP-1145 to develop 131I-iodofluoropicolinamide benzamide (131I-IFPABZA) and 131I-iodofluoronicotiamide benzamide (131I-IFNABZA) with acceptable radiochem. yield (40 ± 5%) and high radiochem. purity (>98%). We also presented their biol. characteristics in melanoma-bearing mouse models. 131I-IFPABZA (Log P = 2.01) was more lipophilic than 131I-IFNABZA (Log P = 1.49). B16F10-bearing mice injected with 131I-IFNABZA exhibited higher tumor-to-muscle ratio (T/M) than those administered with 131I-IFPABZA in planar γ-imaging and biodistribution studies. However, the imaging of 131I-IFNABZA- and 131I-IFPABZA-injected mice only showed marginal tumor uptake in A375 amelanotic melanoma-bearing mice throughout the experiment period, indicating the high binding affinity of these two radiotracers to melanin. Comparing the radiation-absorbed dose of 131I-IFNABZA with the melanin-targeted agents reported in the literature, 131I-IFNABZA exerts lower doses to normal tissues on the basis of similar tumor dose. Based on the in vitro and in vivo studies, we clearly demonstrated the potential of using 131I-IFNABZA as a theranostic agent against melanoma.

In addition to the literature in the link below, there is a lot of literature about this compound(Picolinamide)Category: tetrahydroisoquinoline, illustrating the importance and wide applicability of this compound(1452-77-3).

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

Diver, Catherine; Lawrance, Geoffrey A. published the article 《Trifluoromethanesulfonato-O complexes of platinum(II) and palladium(II)》. Keywords: trifluoromethanesulfonato palladium platinum complex; hydrolysis kinetics trifluoromethanesulfonato platinum.They researched the compound: cis-Dichlorobis(pyridine)platinum(II)( cas:15227-42-6 ).Formula: C10H10Cl2N2Pt. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:15227-42-6) here.

Reaction of chloroplatinum(II) and chloropalladium(II) complexes containing amine, pyridine, or phosphine ligands at or above room temperature with anhydrous CF3SO3H gave F3CSO3–O complexes, characterized spectroscopically. The complexes cis-[Pt(NH3)2(OSO2CF3)2], trans-[Pt(NH3)2Cl(OSO2CF3)], Pt(en)Cl(OSO2CF3)], [Pt(dppe)(OSO2CF3)2], [Pt(py)2Cl(OSO2CF3)], [Pt(terpy)(OSO2CF3)][CF3SO3], (terpy = 2,2′:6′,2′-terpyridine), trans-[Pd(NH3)2Cl(OSO2CF3)], [Pd(en)(OSO2CF3)2], [Pd(bpy)(OSO2CF3)2] (bpy = 2,2′-bipyridine), and [Pd(PPh3)2(OSO2CF3)2] were isolated. Aquation reactions of selected complexes showed that F3CSO3- hydrolysis is rapid for complexes of both PtII and PdII. Pt(O3SCF3)2 complexes exhibit 2 consecutive rate processes, with k1/k2 ca. 5, consistent with sequential hydrolysis of both anions. Coordinated CF3SO3- in these complexes may be substituted even by neutral coordinating O-donor solvents.

In addition to the literature in the link below, there is a lot of literature about this compound(cis-Dichlorobis(pyridine)platinum(II))Formula: C10H10Cl2N2Pt, illustrating the importance and wide applicability of this compound(15227-42-6).

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

The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: cis-Dichlorobis(pyridine)platinum(II), is researched, Molecular C10H10Cl2N2Pt, CAS is 15227-42-6, about Conformational properties of purine and pyrimidine complexes of cis-platinum. Implications for platinum(II)-DNA crosslinking modes, the main research direction is platinum complex conformation DNA binding; structure activity platinum complex; neoplasm inhibitor platinum complex; stereochem DNA platinum complex.Safety of cis-Dichlorobis(pyridine)platinum(II).

The stereochem. properties of a variety of cis complexes of Pt(II) containing purine or pyrimidine ligands are examined The critical intramol. conformational parameters [the interbase dihedral angle and the base/coordination plane dihedral angles] are systematically studied and trends sought. Where intramol. interactions are determinative of the adopted mol. conformation, the nature of the steric demands imposed by increasing numbers of exocyclic functional groups contiguous to the Pt binding site are clearly of major importance for the antitumor activity.

In addition to the literature in the link below, there is a lot of literature about this compound(cis-Dichlorobis(pyridine)platinum(II))Safety of cis-Dichlorobis(pyridine)platinum(II), illustrating the importance and wide applicability of this compound(15227-42-6).

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: cis-Dichlorobis(pyridine)platinum(II), is researched, Molecular C10H10Cl2N2Pt, CAS is 15227-42-6, about Ligand effects in platinum binding to DNA. A comparison of DNA binding properties for cis- and trans-[PtCl2(amine)2] (amine = NH3, pyridine).Reference of cis-Dichlorobis(pyridine)platinum(II).

The DNA binding properties of cis- and trans-[PtCl2(pyridine)2] have been examined and compared with their NH3 analogs, cis- and trans-DDP. The presence of a planar ligand reduces the rates of DNA binding but does not greatly affect the overall conformation of CT DNA, as measured by CD spectroscopy. The sequence specificity of trans-[PtCl2(py)2] includes alternating purine-pyrimidine sequences. The sequence specificity is further different between the two pyridine isomers, and the steric effects of two cis-pyridine groups are demonstrated by the appearance of relatively few binding sites in the 49-bp duplex. The effects of the pyridine ligand are further manifested by a greatly enhanced DNA-DNA interstrand crosslinking efficiency for the trans isomer, with a cross-link per adduct frequency of between 0.14 and 0.23, depending on the rb of the sample. The unwinding of closed circular pUC19 DNA by trans-[PtCl2(pyridine)2] is also more efficient than that by either DDP isomer. In contrast, little unwinding is induced by cis-[PtCl2(pyridine)2]. These results invert the standard cis/trans structure-activity relationships observed previously for [PtCl2(NH3)2]. The results are discussed with respect to the previously demonstrated effect of activation of the trans-platinum geometry using sterically hindered ligands.

In addition to the literature in the link below, there is a lot of literature about this compound(cis-Dichlorobis(pyridine)platinum(II))Reference of cis-Dichlorobis(pyridine)platinum(II), illustrating the importance and wide applicability of this compound(15227-42-6).

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: 1-Bromoundecane(SMILESS: CCCCCCCCCCCBr,cas:693-67-4) is researched.Recommanded Product: Picolinamide. The article 《A simple and efficient approach for the synthesis of a novel class aliphatic 1,3,4-thiadiazol-2(3H)-one derivatives via intramolecular nucleophilic substitution reaction》 in relation to this compound, is published in Synthetic Communications. Let’s take a look at the latest research on this compound (cas:693-67-4).

In this study, a new series of substituted 1,3,4-thiadiazol-2(3H)-one derivatives I [R = Et, CH2CH=CH2, cyclohexylmethyl, etc.] was synthesized in yields ranging from 42 to 70% via reaction of alkyl bromides with 1-(4-chlorophenyl)-2-((5-methyl-1,3,4-thiadiazol-2-yl)thio)ethanol with an interesting mechanism that involved internal nucleophilic substitution followed by an SN2-type nucleophilic substitution. First, 1-(4-chlorophenyl)-2-((5-methyl-1,3,4-thiadiazol-2-yl)thio)ethanone was synthesized from the reaction of 5-methyl-1,3,4-thiadiazole-2-thiol with 2-bromo-1-(4-chlorophenyl)ethanone which underwent reduction to afford 1-(4-chlorophenyl)-2-((5-methyl-1,3,4-thiadiazol-2-yl)thio)ethanol. The advantages of this protocol were synthesis of target compounds under mild conditions using simple synthetic methods and obtaining them without phosgene.

In addition to the literature in the link below, there is a lot of literature about this compound(1-Bromoundecane)COA of Formula: C11H23Br, illustrating the importance and wide applicability of this compound(693-67-4).

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

Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 1452-77-3, is researched, Molecular C6H6N2O, about Improving Compliance and Decreasing Drug Accumulation of Diethylstilbestrol through Cocrystallization, the main research direction is diethylstilbestrol cocrystal cocrystn.Recommanded Product: 1452-77-3.

Diethylstilbestrol (DES), a synthetic nonsteroidal estrogen, has been prescribed for advanced breast cancer and prostate cancer. However, its poor compliance, reactive metabolite toxicity and hydrophobicity-induced drug accumulation has limited its applications. In this study, we aimed to modulate its dissolution rate and reduce reactive metabolites and drug accumulation through cocrystn. Cocrystals of DES with isonicotinamide (INA), picolinamide (PIN), nicotinamide (NIA), urea (UREA), sarcosine (SAR), and flavone (FLA) were obtained. Different crystallization strategies result in cocrystal polymorphs for DES with INA and FLA. Intrinsic dissolution rate (IDR) characterizations in pH 2.0 buffer solution were conducted. Two assumptions (enhancing Cmax or prolonging Tmax) with the aim of improving compliance were put forward. On the basis of the IDR results (DES-NIA with a 1.5-fold increase in IDR and DES-2FLA-B with a 5.5-fold decrease in IDR) and the pharmacol. activities of coformers (NIA and FLA with CYPs inhibition and UGTs stimulation effects), the pharmacokinetic behaviors of these two cocrystals were further researched. The 2-fold prolongation of Tmax in the PK profile DES-2FLA-B facilitated an improvement in compliance. In addition, the higher clearance rates and the potential to reduce oxidative metabolites in DES-2FLA-B help to decrease the drug accumulation and reduce the adverse effects of DES.

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

Quality Control of 1-Bromoundecane. The protonation of heteroatoms in aromatic heterocycles can be divided into two categories: lone pairs of electrons are in the aromatic ring conjugated system; and lone pairs of electrons do not participate. Compound: 1-Bromoundecane, is researched, Molecular C11H23Br, CAS is 693-67-4, about Probing the substitution pattern of indole-based scaffold reveals potent and selective sphingosine kinase 2 inhibitors. Author is Congdon, Molly; Fritzemeier, Russell G.; Kharel, Yugesh; Brown, Anne M.; Serbulea, Vlad; Bevan, David R.; Lynch, Kevin R.; Santos, Webster L..

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.

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

Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 15227-42-6, is researched, SMILESS is [Cl-][Pt+2]([N]1=CC=CC=C1)([Cl-])[N]2=CC=CC=C2, Molecular C10H10Cl2N2PtJournal, Article, Research Support, Non-U.S. Gov’t, Journal of Inorganic Biochemistry called Might telomerase enzyme be a possible target for trans-Pt(II) complexes?, Author is Colangelo, Donato; Ghiglia, AnnaLisa; Viano, Ilario; Mahboobi, Homa; Ghezzi, AnnaRita; Cassino, Claudio; Osella, Domenico, the main research direction is trans platinum antitumor complex telomerase target.Product Details of 15227-42-6.

Telomerase is a ribonucleoprotein polymerase that synthesizes telomeric DNA (TTAGGG) repeats. Previously, we have studied the effect on telomerase enzyme of several cis-platinum(II) complexes bearing aromatic amines as bulky carrier groups. All these complexes possess cis-geometry, according to the Cleare and Hoschele’s rule. Since recent reports have dealt with the anti-cancer activity of trans-platinum compounds, in this study we have investigated the Farrell’s prototypical trans-[Pt(Cl)2(pyridine)2], hereafter called trans-PtPy, to understand whether it may possess any anti-telomerase activity. The trans-PtPy has low water solubility and requires DMSO as co-solvent, thus making the biol. tests problematic. The effect of trans-PtPy on MCF-7 cell line concerning log-term telomerase inhibition, telomerase-related gene expression, viability, and apoptosis was evaluated. In a cell-free biochem. assay, trans-PtPy showed significant and dose-dependent inhibition of semi-purified telomerase. The bulk of data indicate that trans-PtPy acts as a non-properly selective anti-proliferative agent, although it shows an initial telomerase inhibitory effect. Telomere length reduction seems not to be the main mechanism causing the observed cell apoptosis. For comparison purpose, results on cis-[Pt(Cl)2(pyridine)2] are reported.

In addition to the literature in the link below, there is a lot of literature about this compound(cis-Dichlorobis(pyridine)platinum(II))Product Details of 15227-42-6, illustrating the importance and wide applicability of this compound(15227-42-6).

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.Category: tetrahydroisoquinoline. The article 《Cytostatic trans-platinum(II) complexes》 in relation to this compound, is published in Journal of Medicinal Chemistry. Let’s take a look at the latest research on this compound (cas:15227-42-6).

The unusual cytostatic properties of trans-Pt(II) complexes of pyridine, trans-[PtCl2L2] (L = pyridine, 4-methylpyridine), are reported. The complexes demonstrate increased cytostatic activity to L1210 leukemia cells over the cis-pyridine analogs and had activity equivalent to that of cisplatin. The results have implications for the design of structurally novel Pt antitumor agents.

In addition to the literature in the link below, there is a lot of literature about this compound(cis-Dichlorobis(pyridine)platinum(II))Name: cis-Dichlorobis(pyridine)platinum(II), illustrating the importance and wide applicability of this compound(15227-42-6).

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