Month: October 2022

On November 1, 2015, Dong, Yan; Li, Kehuang; Xu, Zhixiang; Ma, Haikuo; Zheng, Jiyue; Hu, Zhilin; He, Sudan; Wu, Yiyuan; Sun, Zhijian; Luo, Lusong; Li, Jiajun; Zhang, Hongjian; Zhang, Xiaohu published an article.Category: piperazines The title of the article was Exploration of the linkage elements of porcupine antagonists led to potent Wnt signaling pathway inhibitors. And the article contained the following:

The Wnt signaling pathway is a pivotal developmental pathway. It operates through control of cellular functions such as proliferation, differentiation, migration and polarity. Aberrant Wnt signaling has been implicated in the formation and metastasis of tumors. Porcupine is a component of the Wnt signaling pathway. It is a member of the membrane-bound O-acyltransferase family of proteins. Porcupine catalyzes the palmitoylation of Wnt proteins, a process which is essential to their secretion and activity. Here we report a novel series of compounds obtained by a scaffold hybridization strategy from two known porcupine inhibitor classes. The leading compound 62 demonstrated subnanomolar (IC50 0.11 nM) inhibition of Wnt signaling in a paracrine cellular reporter gene assay. Compound 62 also potently inhibited Wnt secretion into culture medium, an indication of direct inhibition of the porcupine protein. Furthermore, compound 62 showed excellent chem., plasma and liver microsomal stabilities. Collectively, these results strongly support further optimization of this novel scaffold to develop better Wnt pathway inhibitors. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Category: piperazines

The Article related to protein palmitoyltransferase porcupine antagonist synthesis inhibitor wnt signaling secretion, antagonist, cancer therapy, porcupine, scaffold hybridization, wnt signaling pathway and other aspects.Category: piperazines

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On October 31, 1980, Carissimi, M.; Picciola, G.; Ravenna, F.; Carenini, G.; Gentili, P. published an article.Computed Properties of 59695-29-3 The title of the article was 2-(2-Thienyl)morpholines active on the central nervous system. And the article contained the following:

Morpholinones I [R = H, PhCH2, CHMe2, substituted 3-(1-piperazinyl)propionyl, substituted 3-(1-piperazinyl)propyl; Z = O] underwent LiAlH4 reduction to yield I (Z = H2), which showed antidepressant activity. Cyclocondensation of 2-benzylamin-1-(2-thienyl)ethanol with ClCH2COCl gave I (R = PhCH2, Z = 0). The experimental process involved the reaction of 3-(4-Methylpiperazin-1-yl)propanoic acid dihydrochloride(cas: 59695-29-3).Computed Properties of 59695-29-3

The Article related to morpholine thienyl preparation antidepressant, thienylmorpholine preparation antidepressant, analgesic thienylmorpholine preparation, antiinflammatory thienylmorpholine preparation and other aspects.Computed Properties of 59695-29-3

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On September 27, 2017, Beyzavi, Hudson; Mandal, Debashis; Strebl, Martin G.; Neumann, Constanze N.; D’Amato, Erica M.; Chen, Junting; Hooker, Jacob M.; Ritter, Tobias published an article.Formula: C12H16N2O2 The title of the article was 18F-Deoxyfluorination of Phenols via Ru π-Complexes. And the article contained the following:

The deficiency of robust and practical methods for 18F-radiofluorination is a bottleneck for positron emission tomog. (PET) tracer development. Here, we report the first transition-metal-assisted 18F-deoxyfluorination of phenols. The transformation benefits from readily available phenols as starting materials, tolerance of moisture and ambient atm., large substrate scope, and translatability to generate doses appropriate for PET imaging. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Formula: C12H16N2O2

The Article related to transition metal assisted deoxyfluorination phenol ruthenium complex, crystal mol structure fluorophenyl ruthenium cyclopentenyl complex, radiofluorination phenol ruthenium complex and other aspects.Formula: C12H16N2O2

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On March 31, 2020, Omsland, Maria; Andresen, Vibeke; Gullaksen, Stein-Erik; Ayuda-Duran, Pilar; Popa, Mihaela; Hovland, Randi; Brendehaug, Atle; Enserink, Jorrit; McCormack, Emmet; Gjertsen, Bjorn Tore published an article.Product Details of 380843-75-4 The title of the article was Tyrosine kinase inhibitors and interferon-a increase tunneling nanotube (TNT) formation and cell adhesion in chronic myeloid leukemia (CML) cell lines. And the article contained the following:

Chronic myeloid leukemia (CML) is a stem cell disease of the bone marrow where mechanisms of inter-leukemic communication and cell-to-cell interactions are proposed to be important for optimal therapy response. Tunneling nanotubes (TNTs) are novel intercellular communication structures transporting different cargos with potential implications in therapy resistance. Here, we have investigated TNTs in CML cells and following treatment with the highly effective CML therapeutics tyrosine kinase inhibitors (TKIs) and interferon-a (IFNa). CML cells from chronic phase CML patients as well as the blast crisis phase cell lines, Kcl-22 and K562, formed few or no TNTs. Treatment with imatinib increased TNT formation in both Kcl-22 and K562 cells, while nilotinib or IFNa increased TNTs in Kcl-22 cells only where the TNT increase was associated with adherence to fibronectin-coated surfaces, altered morphol., and reduced movement involving beta1integrin. Ex vivo treated cells from chronic phase CML patients showed limited changes in TNT formation similarly to bone marrow cells from healthy individuals. Interestingly, in vivo nilotinib treatment in a Kcl-22 s.c. mouse model resulted in morphol. changes and TNT-like structures in the tumor-derived Kcl-22 cells. Our results demonstrate that CML cells express low levels of TNTs, but CML therapeutics increase TNT formation in designated cell models indicating TNT functionality in bone marrow derived malignancies and their microenvironment. The experimental process involved the reaction of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile(cas: 380843-75-4).Product Details of 380843-75-4

The Article related to imatinib nilotinib antineoplastic agent chronic myeloid leukemia tnt ifnalpha, cell adhesion, chronic myeloid leukemia, interferon-α, tunneling nanotubes, tyrosine kinase inhibitors and other aspects.Product Details of 380843-75-4

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On May 31, 2020, Botros, Liza; Pronk, Manon C. A.; Juschten, Jenny; Liddle, John; Morsing, Sofia K. H.; van Buul, Jaap D.; Bates, Robert H.; Tuinman, Pieter R.; van Bezu, Jan S. M.; Huveneers, Stephan; Bogaard, Harm Jan; van Hinsbergh, Victor W. M.; Hordijk, Peter L.; Aman, Jurjan published an article.COA of Formula: C26H29Cl2N5O3 The title of the article was Bosutinib prevents vascular leakage by reducing focal adhesion turnover and reinforcing junctional integrity. And the article contained the following:

Endothelial barrier dysfunction leads to edema and vascular leak, causing high morbidity and mortality. Previously, Abl kinase inhibition has been shown to protect against vascular leak. Using the distinct inhibitory profiles of clin. available Abl kinase inhibitors, we aimed to provide a mechanistic basis for novel treatment strategies against vascular leakage syndromes. We found that the inhibitor bosutinib most potently protected against inflammation-induced endothelial barrier disruption. In vivo, bosutinib prevented lipopolysaccharide (LPS)-induced alveolar protein extravasation in an acute lung injury mice model. Mechanistically, mitogen-activated protein 4 kinase 4 (MAP4K4) was identified as important novel mediator of endothelial permeability, which signaled via ezrin, radixin and moesin proteins to increase turnover of integrin-based focal adhesions. The combined inhibition of MAP4K4 and Abl-related gene (Arg, also known as ABL2) by bosutinib preserved adherens junction integrity and reduced turnover of focal adhesions, which synergistically act to stabilize the endothelial barrier during inflammation. We conclude that MAP4K4 is an important regulator of endothelial barrier integrity, increasing focal adhesion turnover and disruption of cell-cell junctions during inflammation. Because it inhibits both Arg and MAP4K4, use of the clin. available drug bosutinib might form a viable strategy against vascular leakage syndromes. The experimental process involved the reaction of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile(cas: 380843-75-4).COA of Formula: C26H29Cl2N5O3

The Article related to bosutinib antiinflammatory agent focal adhesion acute lung injury, bosutinib, endothelial barrier function, focal adhesion, map4k4, tyrosine kinase inhibitors, vascular permeability and other aspects.COA of Formula: C26H29Cl2N5O3

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On May 10, 2018, Yu, Le-Mao; Hu, Zhu; Chen, Yu; Ravji, Azhar; Lopez, Sophia; Plescia, Caroline B.; Yu, Qian; Yang, Hui; Abdelmalak, Monica; Saha, Sourav; Agama, Keli; Kiselev, Evgeny; Marchand, Christophe; Pommier, Yves; An, Lin-Kun published an article.COA of Formula: C12H16N2O2 The title of the article was Synthesis and structure-activity relationship of furoquinolinediones as inhibitors of Tyrosyl-DNA phosphodiesterase 2 (TDP2). And the article contained the following:

Tyrosyl-DNA phosphodiesterase 2 (TDP2) is a recently discovered enzyme specifically repairing topoisomerase II (TOP2)-mediated DNA damage. It has been shown that inhibition of TDP2 synergize with TOP2 inhibitors. Herein, we report the discovery of the furoquinolinedione chemotype as a suitable skeleton for the development of selective TDP2 inhibitors. Compound 1 was identified as a TDP2 inhibitor as a result of screening our inhouse compound library for compounds selective for TDP2 vs. TDP1. Further SAR studies provide several selective TDP2 inhibitors at low-micromolar range. The most potent compound 74 shows inhibitory activity with IC50 of 1.9 and 2.1 μM against recombinant TDP2 and TDP2 in whole cell extracts (WCE), resp. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).COA of Formula: C12H16N2O2

The Article related to furoquinoline dione derivative preparation structure tyrosyl dna phosphodiesterase inhibitor, dna repair, furoquinolinedione, inhibitor, topoisomerase, tyrosyl-dna phosphodiesterase and other aspects.COA of Formula: C12H16N2O2

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On February 5, 2022, Degirmencioglu, Ismail; Iren, Kubra; Yalcin, Izzet; Gol, Cem; Durmus, Mahmut published an article.Name: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone The title of the article was Synthesis of axially disubstituted silicon(IV) phthalocyanines and investigation of their photophysical and photochemical properties. And the article contained the following:

In this study, the axially 1-(4-(3-(6-hydroxyhexyl)-3,4-dihydro-2H-benzo[e][1,3]oxazin-6-yl)piperazin-1-yl)ethanone and 1-(4-(3-(2-(2-hydroxyethoxy)ethyl)-3,4-dihydro-2H-benzo[e][1,3]oxazin-6-yl)piperazin-1-yl)ethanone disubstituted silicon(IV) phthalocyanines and their corresponding quaternized derivatives were synthesized for the first time as candidate photosensitizers for photodynamic therapy (PDT) in cancer treatment. The structures of these novel compounds were confirmed by some spectroscopic techniques such as FT-IR, 1H NMR, 13C NMR, UV-Vis, and mass. The axially substitution increased the solubility of the silicon(IV) phthalocyanines. The prepared silicon(IV) phthalocyanines showed great results achieved from photochem. and photophys. investigations in DMSO solution Especially, high singlet oxygen and the fluorescence quantum yield values of the quaternized silicon (IV) phthalocyanines indicates that these compounds have major potential as photosensitizers in PDT. Furthermore, studied silicon(IV) phthalocyanine complexes could be classified as the stable photosensitizer in accordance with photodegradation study results. The fluorescence quenching behavior of these phthalocyanine complexes was also examined using fluorescence quenching method by 1,4-benzoquinone (BQ). The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Name: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

The Article related to silicon phthalocyanine disubstituted axial preparation photophys photochem property, fluorescence quenching solubility absorbance photolysis silicon phthalocyanine disubstituted axial and other aspects.Name: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On October 31, 2013, Bhattacharya, Anindya; Wang, Qi; Ao, Hong; Shoblock, James R.; Lord, Brian; Aluisio, Leah; Fraser, Ian; Nepomuceno, Diane; Neff, Robert A.; Welty, Natalie; Lovenberg, Timothy W.; Bonaventure, Pascal; Wickenden, Alan D.; Letavic, Michael A. published an article.COA of Formula: C28H32N4O2S The title of the article was Pharmacological characterization of a novel centrally permeable P2X7 receptor antagonist: JNJ-47965567. And the article contained the following:

Background and Purpose : An increasing body of evidence suggests that the purinergic receptor P2X, ligand-gated ion channel, 7 (P2X7) in the CNS may play a key role in neuropsychiatry, neurodegeneration and chronic pain. In this study, we characterized JNJ-47965567, a centrally permeable, high-affinity, selective P2X7 antagonist. Exptl. Approach : We have used a combination of in vitro assays (calcium flux, radioligand binding, electrophysiol., IL-1β release) in both recombinant and native systems. Target engagement of JNJ-47965567 was demonstrated by ex vivo receptor binding autoradiog. and in vivo blockade of Bz-ATP induced IL-1β release in the rat brain. Finally, the efficacy of JNJ-47965567 was tested in standard models of depression, mania and neuropathic pain. Key Results : JNJ-47965567 is potent high affinity (pKi 7.9 ± 0.07), selective human P2X7 antagonist, with no significant observed speciation. In native systems, the potency of the compound to attenuate IL-1β release was 6.7 ± 0.07 (human blood), 7.5 ± 0.07 (human monocytes) and 7.1 ± 0.1 (rat microglia). JNJ-47965567 exhibited target engagement in rat brain, with a brain EC50 of 78 ± 19 ng·mL-1 (P2X7 receptor autoradiog.) and functional block of Bz-ATP induced IL-1β release. JNJ-47965567 (30 mg·kg-1) attenuated amphetamine-induced hyperactivity and exhibited modest, yet significant efficacy in the rat model of neuropathic pain. No efficacy was observed in forced swim test. Conclusion and Implications : JNJ-47965567 is centrally permeable, high affinity P2X7 antagonist that can be used to probe the role of central P2X7 in rodent models of CNS pathophysiol. The experimental process involved the reaction of N-((4-(4-Phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide(cas: 1428327-31-4).COA of Formula: C28H32N4O2S

The Article related to neuroprotectant jnj47965567 p2x7 receptor antagonist central nervous system, p2x7, autoradiography, depression, interleukin 1β (il-1β), mania, microdialysis, neuropathic pain, purinergic and other aspects.COA of Formula: C28H32N4O2S

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On June 30, 2013, Shou, Kai-jun; Li, Jie; Jin, Yi; Lv, Yan-wen published an article.Recommanded Product: 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate The title of the article was Design, synthesis, biological evaluation, and molecular docking studies of quinolone derivatives as potential antitumor topoisomerase I inhibitors. And the article contained the following:

A novel series of quinolone derivatives were designed and synthesized, and their biol. activities were evaluated as potential antitumor topoisomerase I (Top I) inhibitors. Among these compounds, one compound exhibited the most potent antitumor activities against multiple cancer cell lines. Docking simulation was performed to insert compound this compound into the crystal structure of DNA-Top I to determine the probable binding model. The experimental process involved the reaction of 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate(cas: 86393-32-0).Recommanded Product: 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate

The Article related to phenylsulfonyl carbamidoyl quinolone preparation topoisomerase inhibitor structure activity relationship, topoisomerase phenylsulfonyl carbamidoyl quinolone docking antitumor drug design and other aspects.Recommanded Product: 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On March 31, 2021, Liu, Juan; Zhang, Yuan; Huang, Honglin; Lei, Xiaoyong; Tang, Guotao; Cao, Xuan; Peng, Junmei published an article.COA of Formula: C26H29Cl2N5O3 The title of the article was Recent advances in Bcr-Abl tyrosine kinase inhibitors for overriding T315I mutation. And the article contained the following:

A review. BCR-ABL is a gene produced by the fusion of the bcr gene and the c-abl proto-oncogene and is considered to be the main cause of chronic myelogenous leukemia (CML) production Therefore, the development of selective Bcr-Abl kinase inhibitors is an attractive strategy for the treatment of CML. However, in the treatment of CML with a Bcr-Abl kinase inhibitor, the T315I gatekeeper mutant disrupts the important contact interaction between the inhibitor and the enzyme, resistant to the first- and second-generation drugs currently approved, such as imatinib, bosutinib, nilotinib, and dasatinib. In order to overcome this special resistance, several different strategies have been explored, and many mols. have been studied to effectively inhibit Bcr-Abl T315I. Some of these mols. are still under development, and some are being studied preclinically, and still others are in clin. research. Herein, this review reports some of the major examples of third-generation Bcr-Abl inhibitors against the T315I mutation. The experimental process involved the reaction of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile(cas: 380843-75-4).COA of Formula: C26H29Cl2N5O3

The Article related to review imatinib bosutinib anticancer bcr abl chronic myelogenous leukemia, atp-competitive inhibitors, bcr-abl, t315i mutation, chronic myelogenous leukemia, non-atp-competitive inhibitors and other aspects.COA of Formula: C26H29Cl2N5O3

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics