Month: April 2022

Recommanded Product: 1452-77-3. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: Picolinamide, is researched, Molecular C6H6N2O, CAS is 1452-77-3, about Bis(N-picolinamido)cobalt(II) Complexes Display Antifungal Activity toward Candida albicans and Aspergillus fumigatus. Author is Ghandhi, Laura H. D.; Bidula, Stefan; Pask, Christopher M.; Lord, Rianne M.; McGowan, Patrick C..

This report highlights the synthesis and characterization of ten new bis(N-picolinamido)cobalt(II) complexes of the type [(L)2CoX2]0/2+, whereby L=N-picolinamide ligand and X=diisothiocyanato (-NCS), dichlorido (-Cl) or diaqua (-OH2) ligands. Single crystal X-ray (SC-XRD) anal. for nine of the structures are reported and confirm the picolinamide ligand is bound to the Co(II) center through a neutral N,O binding mode. With the addition of powder X-ray diffraction (PXRD), we have confirmed the cis and trans ligand arrangements of each complex. All complexes were screened against several fungal species and show increased antifungal activity. Notably, these complexes had significant activity against strains of Candida albicans and Aspergillus fumigatus, with several compounds exhibiting growth inhibition of >80 %, and onecompound inhibiting Aspergillus fumigatus hyphal growth by >90 %. Conversely, no antifungal activity was exhibited toward Cryptococcus neoformans and no cytotoxicity towards mammalian cell lines.

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

Most of the compounds have physiologically active properties, and their biological properties are often attributed to the heteroatoms contained in their molecules, and most of these heteroatoms also appear in cyclic structures. A Journal, Article, Research Support, Non-U.S. Gov’t, Journal of Organic Chemistry called δ-Valerolactamic quaternary amino acid derivatives: Enantiodivergent synthesis and evidence for stereodifferentiated β-turn-inducing properties, Author is Zhang, Xiaofei; Ligny, Romain; Chewchanwuttiwong, Sopa; Hadade, Rawan; Laurent, Mathieu Y.; Martel, Arnaud; Jacquemmoz, Corentin; Lhoste, Jerome; Bricaud, Sullivan; Py, Sandrine; Dujardin, Gilles, which mentions a compound: 61302-99-6, SMILESS is N[C@H](C)C(NC)=O.[H]Cl, Molecular C4H11ClN2O, Name: D-Alanine methylamide hydrochloride.

Enantiopure (R) and (S) cyclic α,α-disubstituted amino acid derivatives displaying a δ-valerolactam side chain were prepared from a common isoxazolidine precursor. The (R)-configured δ-valerolactam (I) was converted into diastereoisomeric pseudopeptides to investigate its ability to induce secondary structures in peptidomimetics. Conformational studies of these pseudopeptides were carried out in the solid state (X-ray diffraction), in solution (NMR analyses), and in silico (computer-aided conformational anal.), which demonstrated that such quaternary amino acids induce β-turn conformations stable enough to be retained in polar media (DMSO). Incorporation of this new type of α,α-disubstituted amino acid into a representative pseudopeptidic sequence by N- then C-elongation and N-debenzylation is also described herein and could serve for the synthesis of various structured peptidomimetics.

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

Most of the compounds have physiologically active properties, and their biological properties are often attributed to the heteroatoms contained in their molecules, and most of these heteroatoms also appear in cyclic structures. A Journal, Article, Research Support, Non-U.S. Gov’t, Validation Study, Journal of Inorganic Biochemistry called The RP-HPLC measurement and QSPR analysis of log Po/w values of several Pt(II) complexes, Author is Platts, James A.; Oldfield, Steven P.; Reif, Maria M.; Palmucci, Alessandra; Gabano, Elisabetta; Osella, Domenico, which mentions a compound: 15227-42-6, SMILESS is [Cl-][Pt+2]([N]1=CC=CC=C1)([Cl-])[N]2=CC=CC=C2, Molecular C10H10Cl2N2Pt, Synthetic Route of C10H10Cl2N2Pt.

The n-octanol/water partition coefficient, log Po/w, for a set of 24 Pt(II)-complexes was estimated by means of reversed-phase high performance liquid chromatog. (RP-HPLC) technique using a C18 (ODS, octadecyl silane) column as a stationary phase and water/methanol mixtures as mobile phases. Based on the known log P o/w of several Pt(II)-complexes, the authors set a method to correlate the partition coefficient of this kind of complexes with the corresponding retention parameters. The best result was obtained from extrapolation to 0% of the organic modifier (MeOH) of the aqueous eluant. A quant. structure-property relationship (QSPR) was constructed using mol. descriptors derived from d. functional theory (DFT) calculations, which was found to correlate and predict these values with good accuracy. The use of DFT calculations is required because group-additive methods fail due to lack of values for appropriate fragments for many Pt(II)-complexes.

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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: 1-Bromoundecane, is researched, Molecular C11H23Br, CAS is 693-67-4, about Ionic liquid crystals: Synthesis and characterization via NMR, DSC, POM, X-ray diffraction and ionic conductivity of asymmetric viologen bistriflimide salts.Reference of 1-Bromoundecane.

A series of asym. viologen bistriflimide salts I (R = n-pentyl, dodecyl, octadecyl, etc.) of both short and long alkyl chains were synthesized by the metathesis reaction of lithium triflimide salt with the resp. asym. viologen dibromide salts II in methanol. Their thermotropic liquid crystalline properties were determined by differential scanning calorimetry, polarizing optical microscopy and variable temperature X-ray diffraction techniques. These salts melt into highly-ordered smectic T phases i.e., crystal-to SmT transitions (Tms) at relatively low temperatures (lowest Tm at -12°C) and maintain liquid crystallinity in a wide range of temperatures (8-132°C), with excellent thermal stabilities up to 320°C as determined by thermogravimetric anal. These results differ with respect to the sym. viologen bistriflimide salts I. Ionic conductivity of these salts was also measured by dielec. impedance spectroscopy and found to be in the 10-2.5 S cm-1 range, highlighting their potential as electrolytes at room temperature

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

So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Li, Yangfeng; Zhao, Jiong; Gutgesell, Lauren M.; Shen, Zhengnan; Ratia, Kiira; Dye, Katherine; Dubrovskyi, Oleksii; Zhao, Huiping; Huang, Fei; Tonetti, Debra A.; Thatcher, Gregory R. J.; Xiong, Rui researched the compound: 7-Bromo-5-nitro-1H-indole( cas:87240-07-1 ).Related Products of 87240-07-1.They published the article 《Novel Pyrrolopyridone Bromodomain and Extra-Terminal Motif (BET) Inhibitors Effective in Endocrine-Resistant ER+ Breast Cancer with Acquired Resistance to Fulvestrant and Palbociclib》 about this compound( cas:87240-07-1 ) in Journal of Medicinal Chemistry. Keywords: pyrrolopyridone bromodomain BET inhibitor preparation resistant breast cancer thrombocytopenia. We’ll tell you more about this compound (cas:87240-07-1).

Acquired resistance to fulvestrant and palbociclib is a new challenge to treatment of estrogen receptor pos. (ER+) breast cancer. ER is expressed in most resistance settings; thus, bromodomain and extra-terminal protein inhibitors (BETi) that target BET-amplified ER-mediated transcription have therapeutic potential. Novel pyrrolopyridone BETi leveraged novel interactions with L92/L94 confirmed by a cocrystal structure of 27 with BRD4. Optimization of BETi using growth inhibition in fulvestrant-resistant (MCF-7:CFR) cells was confirmed in endocrine-resistant, palbociclib-resistant, and ESR1 mutant cell lines. 27 was more potent in MCF-7:CFR cells than six BET inhibitors in clin. trials. Transcriptomic anal. differentiated 27 from the benchmark BETi, JQ-1, showing downregulation of oncogenes and upregulation of tumor suppressors and apoptosis. The therapeutic approach was validated by oral administration of 27 in orthotopic xenografts of endocrine-resistant breast cancer in monotherapy and in combination with fulvestrant. Importantly, at an equivalent dose in rats, thrombocytopenia was mitigated.

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

Recommanded Product: 6-Bromo-4-methoxypicolinamide. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: 6-Bromo-4-methoxypicolinamide, is researched, Molecular C7H7BrN2O2, CAS is 2241400-93-9, about Scaffold-Hopping Approach To Discover Potent, Selective, and Efficacious Inhibitors of NF-κB Inducing Kinase.

NF-κB-inducing kinase (NIK) is a protein kinase central to the noncanonical NF-κB pathway downstream from multiple TNF receptor family members, including BAFF, which has been associated with B cell survival and maturation, dendritic cell activation, secondary lymphoid organ development, and bone metabolism We report herein the discovery of lead chem. series of NIK inhibitors that were identified through a scaffold-hopping strategy using structure-based design. Electronic and steric properties of lead compounds were modified to address glutathione conjugation and amide hydrolysis. These highly potent compounds exhibited selective inhibition of LTβR-dependent p52 translocation and transcription of NF-κB2 related genes. Compound 4f is shown to have a favorable pharmacokinetic profile across species and to inhibit BAFF-induced B cell survival in vitro and reduce splenic marginal zone B cells in vivo.

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

Application of 882562-40-5. 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: 3-(2,5-Dichloropyrimidin-4-yl)-1-(phenylsulfonyl)-1H-indole, is researched, Molecular C18H11Cl2N3O2S, CAS is 882562-40-5, about Discovery and resistance mechanism of a selective CDK12 degrader. Author is Jiang, Baishan; Gao, Yang; Che, Jianwei; Lu, Wenchao; Kaltheuner, Ines H.; Dries, Ruben; Kalocsay, Marian; Berberich, Matthew J.; Jiang, Jie; You, Inchul; Kwiatkowski, Nicholas; Riching, Kristin M.; Daniels, Danette L.; Sorger, Peter K.; Geyer, Matthias; Zhang, Tinghu; Gray, Nathanael S..

Cyclin-dependent kinase 12 (CDK12) is an emerging therapeutic target due to its role in regulating transcription of DNA-damage response (DDR) genes. However, development of selective small mols. targeting CDK12 has been challenging due to the high degree of homol. between kinase domains of CDK12 and other transcriptional CDKs, most notably CDK13. In the present study, the rational design and characterization of a CDK12-specific degrader, BSJ-4-116 (I), is reported. BSJ-4-116 selectively degraded CDK12 as assessed through quant. proteomics. Selective degradation of CDK12 resulted in premature cleavage and poly(adenylation) of DDR genes. Moreover, BSJ-4-116 exhibited potent antiproliferative effects, alone and in combination with the poly(ADP-ribose) polymerase inhibitor olaparib, as well as when used as a single agent against cell lines resistant to covalent CDK12 inhibitors. Two point mutations in CDK12 were identified that confer resistance to BSJ-4-116, demonstrating a potential mechanism that tumor cells can use to evade bivalent degrader mols.

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

COA of Formula: C10H10Cl2N2Pt. 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: cis-Dichlorobis(pyridine)platinum(II), is researched, Molecular C10H10Cl2N2Pt, CAS is 15227-42-6, about Reactions of potassium tetrachloroplatinate(II) with pyridine derivatives in dimethylformamide and synthesis of potassium trichloro(pyridine)platinum(II). Author is Kong, Pi-Chang; Rochon, F. D..

The reactions of K2PtCl4 with pyridine derivatives L (L = py = pyridine, pic = picoline, and lut = lutidine) were studied in DMF. K[PtLCl3] (I) were isolated and the yield decreased with the order, 2,4-lut = 2-pic > 2,6-lut > 4-pic = py, which can be correlated to the steric hindrance of the ortho Me groups. Cis-[PtL2Cl2] (II) is the final product of the reactions. Trans-[PtL2Cl2] (III) can also be obtained from a DMF solution of [Pt(L)4]Cl2 (L = py) at room temperature A comparison of the above reactions in H2O and in DMF was also made.

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

Berezin, V. I.; Ganin, V. V.; Kovrikov, A. B.; Lipnitskii, I. V.; Rogalevich, N. L. 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 ).Application of 15227-42-6. 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.

An IR and Raman spectroscopic investigation of crystalline PdPy2Cl2 was made. The vibrational frequencies were measured in the region from 3500 to 30 cm-1. The assignments of the observed bands were made on the basis of the frequency calculation for trans- and cis-PdPy2Cl2 plane and nonplanar configurations, using force constants, modelled from constants of [Pd(NH3)4]2+ and [PdCl4]2-. The calculation results were used to specify the metal-ligands stretching constants and their interactions.

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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: 1452-77-3, is researched, SMILESS is O=C(N)C1=NC=CC=C1, Molecular C6H6N2OJournal, Polyhedron called Structural and electrochemical properties of two novel CdX2 (X = Br, I) picolinamide complexes, Author is Jadresko, Dijana; Markovic, Berislav; Medvidovic-Kosanovic, Martina; Matkovic-Calogovic, Dubravka; Szechenyi, Aleksandar; Pockaj, Marta; Balic, Tomislav; Popovic, Zora, the main research direction is cadmium bromine iodine picolinamide complex preparation thermal stability electrochem; crystal structure cadmium bromine iodine picolinamide complex.Safety of Picolinamide.

Two novel discrete cadmium(II) complexes, namely [CdBr2(pia)2] (1) and [CdI2(pia)2] (2) were prepared by reactions of aqueous solutions of CdX2 (X = Br, I) salts with picolinamide (pia) in the 2:1 ligand to metal stoichiometric ratio. Both compounds were characterized by elemental anal., IR-spectroscopy, TG/DSC analyses and electrochem. methods. The electrochem. characteristics of both ligand (pia) and prepared complexes were studied by cyclic and (cyclic) square-wave voltammetry, on a static mercury drop electrode (SMDE), in aqueous media over a wide pH range. The mol. and crystal structure of the compounds was determined by the single crystal X-ray diffraction method. X-ray structure anal. of 1 and 2 have shown that the compounds are isostructural with minor differences in the bond angles of the coordination sphere. In both compounds the Cd(II) ion is coordinated by two halide atoms and two mutually orthogonal picolinamide ligands that act as N,O-chelators in a distorted octahedral arrangement. In the crystal structure, the mols. of 1 and 2 are primarily linked via strong head-to-head amide hydrogen bond interactions forming dimers. In 1 the adjacent dimers are connected via N-H···Br hydrogen bonds and offset face to face π···π interactions that involve pyridine rings, while in the structure of 2, the dimers are connected via C-H···O, C-H···N and N-H···I hydrogen bonds into the final 3D structure. The intermol. interactions in both crystal structures were further studied by Hirshfeld surface anal. Electrochem. anal. of 2-picolinamide indicates the irreversible nature of its electro-reduction reaction on SMDE at pH 2. To provide better insight into the redox mechanism and electrokinetic properties of 2-picolinamide, the study of the effect of signal frequency on CSWV response was carried out, too. The electrochem. reduction of complex 2 involves two electron transfer reactions at -0.55 V and -0.83 V, indicating two redox active centers in the mol., while complex 1 appears to be apparently electro-inactive in the studied potential range.

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