Tag: M.W:100-200

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: 23794-15-2, is researched, SMILESS is CC(=O)C1=CC(Cl)=NC=C1, Molecular C7H6ClNOPreprint, bioRxiv called Generation of strong casein kinase 1 inhibitor of Arabidopsis thaliana, Author is Saito, Ami N.; Matsuo, Hiromi; Kuwata, Keiko; Ono, Azusa; Kinoshita, Toshinori; Yamaguchi, Junichiro; Nakamichi, Norihito, the main research direction is Arabidopsis casein kinase inhibitor eukaryote.Computed Properties of C7H6ClNO.

Casein kinase 1 (CK1) is an evolutionarily conserved protein kinase among eukaryotes. Studies on yeast, fungi, and animals have revealed that CK1 plays roles in divergent biol. processes. By contrast, the collective knowledge regarding the biol. roles of plant CK1 lags was behind those of animal CK1. One of reasons for this is that plants have more multiple genes encoding CK1 than animals. To accelerate the research for plant CK1, a strong CK1 inhibitor that efficiently inhibits multiple members of CK1 proteins in vivo (in planta) is required. Here, we report a novel strong CK1 inhibitor of Arabidopsis (AMI-331). Using a circadian period-lengthening activity as estimation of the CK1 inhibitor effect in vivo, we performed a structure-activity relationship (SAR) study of PHA767491 (1,5,6,7-tetrahydro-2-(4-pyridinyl)-4H-pyrrolo[3,2-c]pyridin-4-one hydrochloride), a potent CK1 inhibitor of Arabidopsis, and found that PHA767491 analogs bearing a propargyl group at the pyrrole nitrogen atom (AMI-212) or a bromine atom at the pyrrole C3 position (AMI-23) enhance the period-lengthening activity. The period lengthening activity of a hybrid mol. of AMI-212 and AMI-23 (AMI-331) is about 100-fold stronger than that of PHA767491. An in vitro assay indicated a strong inhibitory activity of CK1 kinase by AMI-331. Also, affinity proteomics using an AMI-331 probe showed that targets of AMI-331 are mostly CK1 proteins. As such, AMI-331 is a strong potent CK1 inhibitor that shows promise in the research of CK1 in plants.

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Piperidine – Wikipedia,
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Product Details of 144230-52-4. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 4,4-Difluoropiperidine hydrochloride, is researched, Molecular C5H10ClF2N, CAS is 144230-52-4, about Discovery of CRBN E3 Ligase Modulator CC-92480 for the Treatment of Relapsed and Refractory Multiple Myeloma. Author is Hansen, Joshua D.; Correa, Matthew; Nagy, Mark A.; Alexander, Matt; Plantevin, Veronique; Grant, Virginia; Whitefield, Brandon; Huang, Dehua; Kercher, Timothy; Harris, Roy; Narla, Rama Krishna; Leisten, Jim; Tang, Yang; Moghaddam, Mehran; Ebinger, Katalin; Piccotti, Joseph; Havens, Courtney G.; Cathers, Brian; Carmichael, James; Daniel, Thomas; Vessey, Rupert; Hamann, Lawrence G.; Leftheris, Katerina; Mendy, Derek; Baculi, Frans; LeBrun, Laurie A.; Khambatta, Gody; Lopez-Girona, Antonia.

Many patients with multiple myeloma (MM) initially respond to treatment with modern combination regimens including immunomodulatory agents (lenalidomide and pomalidomide) and proteasome inhibitors. However, some patients lack an initial response to therapy (i.e., are refractory), and although the mean survival of MM patients has more than doubled in recent years, most patients will eventually relapse. To address this need, we explored the potential of novel cereblon E3 ligase modulators (CELMoDs) for the treatment of patients with relapsed or refractory multiple myeloma (RRMM). We found that optimization beyond potency of degradation, including degradation efficiency and kinetics, could provide efficacy in a lenalidomide-resistant setting. Guided by both phenotypic and protein degradation data, we describe a series of CELMoDs for the treatment of RRMM, culminating in the discovery of CC-92480, a novel protein degrader and the first CELMoD to enter clin. development that was specifically designed for efficient and rapid protein degradation kinetics.

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Piperidine – Wikipedia,
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Quality Control of 1-(2-chloropyridine-4-yl)ethanone. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: 1-(2-chloropyridine-4-yl)ethanone, is researched, Molecular C7H6ClNO, CAS is 23794-15-2, about Synthesis of some new 4-(2-chloropyridin-4-yl)-N-aryl-1,3-thiazol-2-amine derivatives as possible antifungal and antibacterial agents. Author is Narayana, B.; Raj, K. K. Vijaya; Ashalatha, B. V.; Kumari, N. Suchetha.

Novel 4-(2-chloropyridin-4-yl)-N-aryl-1,3-thiazol-2-amines were prepared by reacting (4-bromoacetyl)-2-chloropyridine with thiourea and substituted thioureas. The newly synthesized compounds were characterized by anal. and spectral data. All the compounds were screened for their antifungal and antibacterial activities. Almost all the compounds possess excellent antifungal and antibacterial activities.

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Reference:
Piperidine – Wikipedia,
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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-(2-chloropyridine-4-yl)ethanone, is researched, Molecular C7H6ClNO, CAS is 23794-15-2, about Pyrrolopyridine Inhibitors of Mitogen-Activated Protein Kinase-Activated Protein Kinase 2 (MK-2).Formula: C7H6ClNO.

A new class of potent kinase inhibitors selective for mitogen-activated protein kinase-activated protein kinase 2 (MAPKAP-K2 or MK-2) for the treatment of rheumatoid arthritis has been prepared and evaluated. These inhibitors have IC50 values as low as 10 nM against the target and have good selectivity profiles against a number of kinases including CDK2, ERK, JNK, and p38. These MK-2 inhibitors have been shown to suppress TNFα production in U937 cells and to be efficacious in an acute inflammation model. The structure-activity relationships of this series, the selectivity for MK-2 and their activity in both in vitro and in vivo models are discussed. The observed selectivity is discussed with the aid of an MK-2/inhibitor crystal structure.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Alvey, Luke; Prado, Soizic; Huteau, Valerie; Saint-Joanis, Brigitte; Michel, Sylvie; Koch, Michel; Cole, Stewart T.; Tillequin, Francois; Janin, Yves L. published an article about the compound: 1-(2-chloropyridine-4-yl)ethanone( cas:23794-15-2,SMILESS:CC(=O)C1=CC(Cl)=NC=C1 ).Reference of 1-(2-chloropyridine-4-yl)ethanone. 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:23794-15-2) through the article.

From the structure of 3,3-dimethyl-3H-benzofuro[3,2-f][1]-benzopyran, a selective in vitro inhibitor of mycobacterial growth, a structure-activity relationship investigation has been undertaken. Reported here are the results on the use of [2+3] cycloadditions between 2-formylbenzoquinone and various enol derivatives to give various 4-formyl-5-hydroxy benzofurans. In the next step, an ytterbium triflate-catalyzed reaction with 2-methylpropene allowed the preparation of various original furo[3,2-f]chromenes derivatives Their biol. evaluation on the growth of Mycobacterium smegmatis as well as Mycobacterium tuberculosis pointed out that some analogs were four times more active than the initial hit.

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Piperidine – Wikipedia,
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Shu, Xiaomin; Jin, Ronghua; Zhao, Zhongrui; Cheng, Tanyu; Liu, Guohua published an article about the compound: 1-(2-chloropyridine-4-yl)ethanone( cas:23794-15-2,SMILESS:CC(=O)C1=CC(Cl)=NC=C1 ).Safety of 1-(2-chloropyridine-4-yl)ethanone. 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:23794-15-2) through the article.

Herein, by utilized hollow-shell-structured silica, hydrogen-bonding immobilization via a ship-in-a-bottle synthesis locks a Pd(carbene) center in a nanocage and covalent-bonding immobilization tethers chiral Ru(diamine) centers within the nanochannels, constructed a hetero-bifunctional catalyst. The benefit of this dual center manipulation enabled a challenging Suzuki coupling-asym. transfer hydrogenation tandem reaction and the advantage of this process provided various chiral biarylols I [Ar = Ph, 3-MeC6H4, 3-thienyl, etc.] with enhanced reactivity and enantioselectivity.

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Piperidine – Wikipedia,
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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: 23794-15-2, is researched, Molecular C7H6ClNO, about Synthesis of some biologically active 2,4′-bipyridine-5-carbonitriles carrying the 4-hydroxyphenylthio moiety, the main research direction is bipyridine carbonitrile hydroxyphenylthio preparation antibacterial fungicide structure activity relationship.Reference of 1-(2-chloropyridine-4-yl)ethanone.

The reaction of 4-hydroxythiophenol with 4-acetyl-2-chloropyridine yielded a key intermediate, 1-{2-[(4-hydroxyphenyl)thio]pyridin-4-yl}ethanone. Further treatment of the key intermediate with Et cyanoacetate and various aromatic aldehydes in the presence of ammonium acetate furnished 4-aryl-2′-[(4-hydroxyphenyl)thio]-6-oxo-1,6-dihydro-2,4′-bipyridine-5-carbonitriles, e.g., I (R = H, MeO, Ph, Cl, Me2N). On the other hand, condensation of the key intermediate with aromatic aldehydes and malononitrile in the presence ammonium acetate of in alc. gave 6-amino-4-aryl-2′-[(4-hydroxyphenyl)thio]-2,4′-bipyridine-5-carbonitriles. All the title compounds were subjected to in vitro antibacterial testing against two strains and antifungal screening against two fungi. Some of the compounds showed promising activity.

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LaMattina, John L. published an article about the compound: 1-(2-chloropyridine-4-yl)ethanone( cas:23794-15-2,SMILESS:CC(=O)C1=CC(Cl)=NC=C1 ).Recommanded Product: 1-(2-chloropyridine-4-yl)ethanone. 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:23794-15-2) through the article.

A general synthetic scheme for the preparation of 2-amino-4-(4-imidazolyl)pyridines I (R = NH2, NHEt, NMe2; R1 = H, Me; R2 = H, NH2, Me), potential histamine H2 antagonists, is based on the Neber rearrangement of 1-(4-pyridyl)-1-alkanone oxime O-tosylates to α-amino ketones or α-amino ketals, which are then converted to the imidazoles. The reaction of Grignard reagents with 2-chloroisonicotinonitrile, as well as nucleophilic displacement of Cl by amines on 2-chloroisonicotinonitrile and derivatives, are discussed in relation to the preparation of the ketone intermediates.

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Recommanded Product: 4,4-Difluoropiperidine hydrochloride. 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: 4,4-Difluoropiperidine hydrochloride, is researched, Molecular C5H10ClF2N, CAS is 144230-52-4, about Discovery of M-808 as a Highly Potent, Covalent, Small-Molecule Inhibitor of the Menin-MLL Interaction with Strong In Vivo Antitumor Activity.

Targeting the menin-MLL protein-protein interaction is a new therapeutic strategy for the treatment of acute leukemia carrying MLL fusion (MLL leukemia). We describe herein the structure-based optimization of a class of covalent menin inhibitors, which led to the discovery of M-808 (16)(I) as a highly potent and efficacious covalent menin inhibitor. M-808 effectively inhibits leukemia cell growth at low nanomolar concentrations and is capable of achieving partial tumor regression in an MV4;11 xenograft tumor model in mice at a well-tolerated dose schedule. Determination of the co-crystal structure of M-808 in complex with menin provides a structural basis for their high-affinity, covalent interactions. M-808 represents a promising, covalent menin inhibitor for further optimization and evaluation toward developing a new therapy for the treatment of MLL leukemia.

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The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: Potassium trifluoro(1-methyl-1H-pyrazol-5-yl)borate, is researched, Molecular C4H5BF3KN2, CAS is 1258323-45-3, about Nickel-Catalyzed Cross-Coupling of Potassium Aryl- and Heteroaryltrifluoroborates with Unactivated Alkyl Halides, the main research direction is arene preparation; potassium aryltrifluoroborate alkyl halide cross coupling nickel catalyst.Quality Control of Potassium trifluoro(1-methyl-1H-pyrazol-5-yl)borate.

A method for the cross-coupling of alkyl electrophiles with various potassium aryl- and heteroaryltrifluoroborates has been developed. Nearly stoichiometric amounts of organoboron species could be employed to cross-couple a large variety of challenging heteroaryl nucleophiles. Several functional groups were tolerated on both the electrophilic and the nucleophilic partners. Chemoselective reactivity of C(sp3)-Br bonds in the presence of C(sp2)-Br bonds was achieved.

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Piperidine – Wikipedia,
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