Category: piperazines

Toxicological screening of drugs by microbore high-performance liquid chromatography with photodiode-array detection and ultraviolet spectral library searches was written by Turcant, A.;Premel-Cabic, A.;Cailleux, A.;Allain, P.. And the article was included in Clinical Chemistry (Washington, DC, United States) in 1991.Computed Properties of C22H30N4O2S2 This article mentions the following:

UV data, acquired with a photodiode-array detector coupled to a reversed-phase liquid-chromatog. system, was used to identify unknown drugs in plasma samples of acutely poisoned patients. Both retention time and spectra of the peaks obtained with a microbore Hypersil ODS column under gradient elution are compared with a library of 鈭?50 compounds The authors three-year experience with this system, which identifies drugs in <1 h, with a high degree of confidence is presented. In the experiment, the researchers used many compounds, for example, N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide (cas: 316-81-4Computed Properties of C22H30N4O2S2).

N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide (cas: 316-81-4) belongs to piperazine derivatives. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.Computed Properties of C22H30N4O2S2

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

Design, synthesis and nootropic activity of new analogues of sunifiram and sapunifiram, two potent cognition-enhancers was written by Martini, Elisabetta;Salvicchi, Alberto;Ghelardini, Carla;Manetti, Dina;Dei, Silvia;Guandalini, Luca;Martelli, Cecilia;Melchiorre, Michele;Cellai, Cristina;Scapecchi, Serena;Teodori, Elisabetta;Romanelli, Maria Novella. And the article was included in Bioorganic & Medicinal Chemistry in 2009.Electric Literature of C7H14N2O This article mentions the following:

A series of amides and sulfonamides, structurally related to DM235 (sunifiram) and MN19 (sapunifiram), derived by ring expansion or contraction, or by inversion of the exocyclic amide function, have been synthesized and tested for cognition-enhancing activity in the mouse passive-avoidance test. Some of the compounds display good antiamnesic and procognitive activity, with higher potency than piracetam, and with a potency similar to the parent compounds In the experiment, the researchers used many compounds, for example, 1-(1,4-Diazepan-1-yl)ethanone (cas: 61903-11-5Electric Literature of C7H14N2O).

1-(1,4-Diazepan-1-yl)ethanone (cas: 61903-11-5) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. Electric Literature of C7H14N2O

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

Overall Survival with palbociclib and fulvestrant in Women with HR+/HER2- ABC: updated exploratory analyses of PALOMA-3, a double-blind, phase iii randomized study was written by Cristofanilli, Massimo;Rugo, Hope S.;Im, Seock-Ah;Slamon, Dennis J.;Harbeck, Nadia;Bondarenko, Igor;Masuda, Norikazu;Colleoni, Marco;Demichele, Angela;Loi, Sherene;Iwata, Hiroji;O’leary, Ben;Andre, Fabrice;Loibl, Sibylle;Bananis, Eustratios;Liu, Yuan;Huang, Xin;Kim, Sindy;Frean, Maria Jose Lechuga;Turner, Nicholas C.. And the article was included in Clinical Cancer Research in 2022.Product Details of 571190-30-2 This article mentions the following:

Purpose: To conduct an updated exploratory anal. of overall survival (OS) with a longer median follow-up of 73.3 mo and evaluate the prognostic value of mol. anal. by circulating tumor DNA (ctDNA). Patients and methods: Patients with hormone receptor-pos./human epidermal growth factor receptor 2-neg. (HR+/HER2-) advanced breast cancer (ABC) were randomized 2:1 to receive palbociclib (125 mg orally/day; 3/1 wk schedule) and fulvestrant (500 mg i.m.) or placebo and fulvestrant. This OS anal. was performed when 75% of enrolled patients died (393 events in 521 randomized patients). ctDNA anal. was performed among patients who provided consent. Results: At the data cutoff (August 17, 2020), 258 and 135 deaths occurred in the palbociclib and placebo groups, resp. The median OS [95% confidence interval (CI)] was 34.8 mo (28.8-39.9) in the palbociclib group and 28.0 mo (23.5-33.8) in the placebo group (stratified hazard ratio, 0.81; 95% CI, 0.65-0.99). The 6-yr OS rate (95% CI) was 19.1% (14.9-23.7) and 12.9% (8.0-19.1) in the palbociclib and placebo groups, resp. Favorable OS with palbociclib plus fulvestrant compared with placebo plus fulvestrant was observed in most subgroups, particularly in patients with endocrine-sensitive disease, no prior chemotherapy for ABC and low circulating tumor fraction and regardless of ESR1, PIK3CA, or TP53 mutation status. No new safety signals were identified. Conclusions: The clin. meaningful improvement in OS associated with palbociclib plus fulvestrant was maintained with >6 years of follow-up in patients with HR+/HER2- ABC, supporting palbociclib plus fulvestrant as a standard of care in these patients. In the experiment, the researchers used many compounds, for example, 6-Acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one (cas: 571190-30-2Product Details of 571190-30-2).

6-Acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one (cas: 571190-30-2) belongs to piperazine derivatives. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. Two common salts in the form of which piperazine is usually prepared for pharmaceutical or veterinary purposes are the citrate, 3C4H10N2.2C6H8O7 (i.e. containing 3 molecules of piperazine to 2 molecules of citric acid), and the adipate, C4H10N2.C6H10O4 (containing 1 molecule each of piperazine and adipic acid).Product Details of 571190-30-2

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

Effects of Itraconazole and Tandospirone on the Pharmacokinetics of Perospirone was written by Masui, Takuya;Kusumi, Ichiro;Takahashi, Yoshito;Koyama, Tsukasa. And the article was included in Therapeutic Drug Monitoring in 2005.Safety of rel-(3aR,4S,7R,7aS)-2-(4-(4-(Pyrimidin-2-yl)piperazin-1-yl)butyl)hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione 2-hydroxypropane-1,2,3-tricarboxylate This article mentions the following:

Perospirone is an atypical antipsychotic agent originated and clin. used in Japan. Based on an in vitro study, it is reported that perospirone is mainly metabolized to ID-15036 by cytochrome P 450 (CYP) 3A4. In this study, the authors investigated the effects of itraconazole, which is a specific inhibitor of CYP3A4, or tandospirone, which is mainly metabolized by CYP3A4 and is expected to competitively inhibit the activity of this enzyme, on single oral dose pharmacokinetics of perospirone. After pretreatment with 200 mg daily of itraconazole or 10 mg daily of tandospirone for 5 days, 9 healthy male subjects received 8 mg of perospirone. Plasma concentrations of perospirone and ID-15036 up to 10 h after perospirone dosing were measured by high-performance liquid chromatog. (HPLC). The metabolism of perospirone was significantly inhibited by treatment with itraconazole but not by tandospirone. The present study suggests that CYP3A4 is significantly involved in metabolism of perospirone in humans. In the experiment, the researchers used many compounds, for example, rel-(3aR,4S,7R,7aS)-2-(4-(4-(Pyrimidin-2-yl)piperazin-1-yl)butyl)hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione 2-hydroxypropane-1,2,3-tricarboxylate (cas: 112457-95-1Safety of rel-(3aR,4S,7R,7aS)-2-(4-(4-(Pyrimidin-2-yl)piperazin-1-yl)butyl)hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione 2-hydroxypropane-1,2,3-tricarboxylate).

rel-(3aR,4S,7R,7aS)-2-(4-(4-(Pyrimidin-2-yl)piperazin-1-yl)butyl)hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione 2-hydroxypropane-1,2,3-tricarboxylate (cas: 112457-95-1) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.Safety of rel-(3aR,4S,7R,7aS)-2-(4-(4-(Pyrimidin-2-yl)piperazin-1-yl)butyl)hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione 2-hydroxypropane-1,2,3-tricarboxylate

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

Infigratinib (BGJ398) in previously treated patients with advanced or metastatic cholangiocarcinoma with FGFR2 fusions or rearrangements: mature results from a multicentre, open-label, single-arm, phase 2 study. was written by Javle, Milind;Roychowdhury, Sameek;Kelley, Robin Kate;Sadeghi, Saeed;Macarulla, Teresa;Weiss, Karl Heinz;Waldschmidt, Dirk-Thomas;Goyal, Lipika;Borbath, Ivan;El-Khoueiry, Anthony;Borad, Mitesh J;Yong, Wei Peng;Philip, Philip A;Bitzer, Michael;Tanasanvimon, Surbpong;Li, Ai;Pande, Amit;Soifer, Harris S;Shepherd, Stacie Peacock;Moran, Susan;Zhu, Andrew X;Bekaii-Saab, Tanios S;Abou-Alfa, Ghassan K. And the article was included in The lancet. Gastroenterology & hepatology in 2021.Recommanded Product: 3-(2,6-Dichloro-3,5-dimethoxyphenyl)-1-(6-((4-(4-ethylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)-1-methylurea This article mentions the following:

BACKGROUND: Treatment options are sparse for patients with advanced cholangiocarcinoma after progression on first-line gemcitabine-based therapy. FGFR2 fusions or rearrangements occur in 10-16% of patients with intrahepatic cholangiocarcinoma. Infigratinib is a selective, ATP-competitive inhibitor of fibroblast growth factor receptors. We aimed to evaluate the antitumour activity of infigratinib in patients with locally advanced or metastatic cholangiocarcinoma, FGFR2 alterations, and previous gemcitabine-based treatment. METHODS: This multicentre, open-label, single-arm, phase 2 study recruited patients from 18 academic centres and hospitals in the USA, Belgium, Spain, Germany, Singapore, Taiwan, and Thailand. Eligible participants were aged 18 years or older, had histologically or cytologically confirmed, locally advanced or metastatic cholangiocarcinoma and FGFR2 fusions or rearrangements, and were previously treated with at least one gemcitabine-containing regimen. Patients received 125 mg of oral infigratinib once daily for 21 days of 28-day cycles until disease progression, intolerance, withdrawal of consent, or death. Radiological tumour evaluation was done at baseline and every 8 weeks until disease progression via CT or MRI of the chest, abdomen, and pelvis. The primary endpoint was objective response rate, defined as the proportion of patients with a best overall response of a confirmed complete or partial response, as assessed by blinded independent central review (BICR) according to Response Evaluation Criteria in Solid Tumors, version 1.1. The primary outcome and safety were analysed in the full analysis set, which comprised all patients who received at least one dose of infigratinib. This trial is registered with ClinicalTrials.gov, NCT02150967, and is ongoing. FINDINGS: Between June 23, 2014, and March 31, 2020, 122 patients were enrolled into our study, of whom 108 with FGFR2 fusions or rearrangements received at least one dose of infigratinib and comprised the full analysis set. After a median follow-up of 10路6 months (IQR 6路2-15路6), the BICR-assessed objective response rate was 23路1% (95% CI 15路6-32路2; 25 of 108 patients), with one confirmed complete response in a patient who only had non-target lesions identified at baseline and 24 partial responses. The most common treatment-emergent adverse events of any grade were hyperphosphataemia (n=83), stomatitis (n=59), fatigue (n=43), and alopecia (n=41). The most common ocular toxicity was dry eyes (n=37). Central serous retinopathy-like and retinal pigment epithelial detachment-like events occurred in 18 (17%) patients, of which ten (9%) were grade 1, seven (6%) were grade 2, and one (1%) was grade 3. There were no treatment-related deaths. INTERPRETATION: Infigratinib has promising clinical activity and a manageable adverse event profile in previously treated patients with locally advanced or metastatic cholangiocarcinoma harbouring FGFR2 gene fusions or rearrangements, and so represents a potential new therapeutic option in this setting. FUNDING: QED Therapeutics and Novartis. In the experiment, the researchers used many compounds, for example, 3-(2,6-Dichloro-3,5-dimethoxyphenyl)-1-(6-((4-(4-ethylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)-1-methylurea (cas: 872511-34-7Recommanded Product: 3-(2,6-Dichloro-3,5-dimethoxyphenyl)-1-(6-((4-(4-ethylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)-1-methylurea).

3-(2,6-Dichloro-3,5-dimethoxyphenyl)-1-(6-((4-(4-ethylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)-1-methylurea (cas: 872511-34-7) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.Recommanded Product: 3-(2,6-Dichloro-3,5-dimethoxyphenyl)-1-(6-((4-(4-ethylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)-1-methylurea

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

Effects of a new diphenylpiperazine calcium antagonist, KB-2796, on cerebral ischemic neuronal damage in rats was written by Yamashita, Akira;Ozaki, Akio;Ikegami, Akira;Hayashi, Akemi;Hara, Hideaki;Sukamoto, Takayuki;Ito, Keizo. And the article was included in General Pharmacology in 1993.Application In Synthesis of 1-(Bis(4-fluorophenyl)methyl)-4-(2,3,4-trimethoxybenzyl)piperazine dihydrochloride This article mentions the following:

The effects of KB-2796, a new diphenylpiperazine calcium antagonist, on the mitochondrial dysfunction and energy metabolism deficits were examined in the ischemic rat brain. KB-2796 (30 mg/kg, p.o.), administered 60 min prior to decapitation, improved the reduced respiratory activity of mitochondria obtained from rat brain 5 min after decapitative ischemia. KB-2796 (30 mg/kg, p.o.), administered 60 min prior to ischemic insult, improved both the reductions in pyruvate and ATP and prevented increases in the lactate/pyruvate ratio induced by 30-min forebrain ischemia in rats with 4-vessel occlusion (4-VO). The effect of KB-2796 on local glucose utilization (LCGU) was examined by a quant. autoradiog. 2-[¹⁴C]deoxyglucose method in normal and 4-VO rats. Postischemic LCGU measured 24 h after reperfusion in the forebrain, in particular in the cortex, thalamus, geniculate body, hippocampus, caudate-putamen, nucleus accumbens, colliculus, and corpus callosum, was below the normal control value. KB-2796 (1 mg/kg, i.v.), administered 1 min prior to the injection of 2-[¹⁴C]deoxyglucose, improved the reductions in LCGU that were produced by cerebral ischemia in the cortex, thalamus, geniculate body, caudate-putamen, nucleus accumbens and substantia nigra, but did not affect LCGU in normal rats. These findings suggest that KB-2796 minimized the deficits in brain energy metabolism produced by ischemia; this agent may therefore be a valuable therapeutic drug in cerebrovascular-related disorders. In the experiment, the researchers used many compounds, for example, 1-(Bis(4-fluorophenyl)methyl)-4-(2,3,4-trimethoxybenzyl)piperazine dihydrochloride (cas: 101477-54-7Application In Synthesis of 1-(Bis(4-fluorophenyl)methyl)-4-(2,3,4-trimethoxybenzyl)piperazine dihydrochloride).

1-(Bis(4-fluorophenyl)methyl)-4-(2,3,4-trimethoxybenzyl)piperazine dihydrochloride (cas: 101477-54-7) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 掳C and boils at 125鈥?30 掳C. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.Application In Synthesis of 1-(Bis(4-fluorophenyl)methyl)-4-(2,3,4-trimethoxybenzyl)piperazine dihydrochloride

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

Effective anti-mycobacterial treatment for BCG disease in patients with Mendelian Susceptibility to Mycobacterial Disease (MSMD): a case series was written by Mahdaviani, Seyed Alireza;Fallahi, Mazdak;Jamee, Mahnaz;Marjani, Majid;Tabarsi, Payam;Moniri, Afshin;Farnia, Parisa;Daneshmandi, Zahra;Parvaneh, Nima;Casanova, Jean-Laurent;Bustamante, Jacinta;Mansouri, Davood;Velayati, Ali Akbar. And the article was included in Annals of Clinical Microbiology and Antimicrobials in 2022.SDS of cas: 13292-46-1 This article mentions the following:

Post-vaccination BCG disease typically attests to underlying inborn errors of immunity (IEIs), with the highest rates of complications in patients with Mendelian susceptibility to mycobacterial disease (MSMD). However, therapeutic protocols for the management of BCG-osis (disseminated) and persistent BCG-itis (localized) are still controversial. Twenty-four Iranian patients with MSMD (BCG-osis or BCG-itis), followed from 2009 to 2020 in Tehran, were included in the study. Their medical records were retrospectively reviewed for demographics, clin. features, laboratory findings, and mol. diagnosis. The therapeutic protocol sheets were prepared to contain the types and duration of anti-mycobacterial agents. BCG disease either as BCG-itis (33.3%) or BCG-osis (66.7%) was confirmed in all patients by pos. gastric washing test (54.2%), microbial smear and culture (58.3%), or purified protein derivative (PPD) test (4.2%). The duration between BCG-osis onset and MSMD diagnosis was 21.6 mo. All except three patients were initiated on second-line anti-mycobacterial agents with either a fluoroquinolone (levofloxacin: 15 mg/kg/day, ciprofloxacin: 20 mg/kg/day, ofloxacin: 15 mg/kg/day), aminoglycoside (amikacin: 10-15 mg/kg/day, streptomycin: 15 mg/kg/day), and/or macrolide (clarithromycin: 15 mg/kg/day) along with oral rifampin (10 mg/kg/day), isoniazid (15 mg/kg/day), and ethambutol (20 mg/kg/day). Three patients showed a clin. response to rifampin, despite in vitro resistance. Fourteen (58.3%) patients received also adjuvant s.c. IFN-纬 therapy, 50渭/m2 every other day. At the end of survey, most patients (n = 22, 91.7%) were alive and two patients died following BCG-osis and respiratory failure. We recommend the early instigation of second-line anti-mycobacterial agents in MSMD patients with BCG disease. In the experiment, the researchers used many compounds, for example, 8-(n-(4-methyl-1-piperazinyl)formidoyl)-rifomycins (cas: 13292-46-1SDS of cas: 13292-46-1).

8-(n-(4-methyl-1-piperazinyl)formidoyl)-rifomycins (cas: 13292-46-1) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.SDS of cas: 13292-46-1

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

Identification and characterization of teratogenic chemicals using embryonic stem cells isolated from a wnt/尾-catenin-reporter transgenic mouse line was written by Kugler, Josephine;Kemler, Rolf;Luch, Andreas;Oelgeschlaeger, Michael. And the article was included in Toxicological Sciences in 2016.Recommanded Product: 4-(6-(4-(Piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline This article mentions the following:

Embryonic stem cells (ESCs) are commonly used for the anal. of gene function in embryonic development and provide valuable models for human diseases. In recent years, ESCs have also become an attractive tool for toxicol. testing, in particular for the identification of teratogenic compounds The authors have recently described a Bmp-reporter ESC line as a new tool to identify teratogenic compounds and to characterize the mol. mechanisms mediating embryonic toxicity. Here the authors describe the use of a Wnt/尾-Catenin-reporter ESC line isolated from a previously described mouse line that carries the LacZ reporter gene under the control of a 尾-Catenin responsive promoter. The reporter ESC line stably differentiates into cardiomyocytes within 12 days. The reporter was endogenously induced between day 3-5 of differentiation reminiscent of its expression in vivo, in which strong LacZ activity is detected around gastrulation. Subsequently its expression becomes restricted to mesodermal cells and cells undergoing an epithelial to mesenchymal transition. The Wnt/尾-Catenin-dependent expression of the reporter protein allowed quantification of dose- and time-dependent effects of teratogenic chems. In particular, valproic acid reduced reporter activity on day 7, whereas retinoic acid induced reporter activity on day 5 at concentrations comparable to the ones inhibiting the formation of functional cardiomyocytes, the classical read-out of the embryonic stem cell test (EST). In addition, the authors were also able to show distinct effects of teratogenic chems. on the Wnt/尾-Catenin-reporter compared with the previously described Bmp-reporter ESCs. Thus, different reporter cell lines provide complementary tools for the identification and anal. of potentially teratogenic compounds In the experiment, the researchers used many compounds, for example, 4-(6-(4-(Piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline (cas: 1062368-24-4Recommanded Product: 4-(6-(4-(Piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline).

4-(6-(4-(Piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline (cas: 1062368-24-4) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Piperazine is an anthelminthic especially useful in the treatment of partial intestinal obstruction caused by Ascaris worms, which is a condition primarily seen in children. Piperazine hydrate and piperazine citrate are the main anthelminthic piperazines.Recommanded Product: 4-(6-(4-(Piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline

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

Synthesis, Crystal Structure, and Activity of Pyrazole-Based Inhibitors of p38 Kinase was written by Graneto, Matthew J.;Kurumbail, Ravi G.;Vazquez, Michael L.;Shieh, Huey-Sheng;Pawlitz, Jennifer L.;Williams, Jennifer M.;Stallings, William C.;Geng, Lifeng;Naraian, Ashok S.;Koszyk, Francis J.;Stealey, Michael A.;Xu, Xiangdong D.;Weier, Richard M.;Hanson, Gunnar J.;Mourey, Robert J.;Compton, Robert P.;Mnich, Stephen J.;Anderson, Gary D.;Monahan, Joseph B.;Devraj, Rajesh. And the article was included in Journal of Medicinal Chemistry in 2007.Synthetic Route of C7H14N2 This article mentions the following:

A series of pyrazole inhibitors of p38 mitogen-activated protein (MAP) kinase were designed using a binding model based on the crystal structure of SC-102 derivative bound to p38 enzyme. New chem. using dithietanes was developed to assemble nitrogen-linked substituents at the 5-position of pyrazoles. Calculated log D was used in tandem with structure-based design to guide medicinal chem. strategy and improve the in vivo activity of a series of mols. The crystal structure of an optimized inhibitor, I (SC-806), in complex with p38 enzyme was obtained to confirm the hypothesis that the addition of a basic nitrogen to the mol. induces an interaction with Asp112 of p38伪. A compound identified from this series was efficacious in an animal model of rheumatic disease. In the experiment, the researchers used many compounds, for example, (S)-1,4-Diazabicyclo[4.3.0]nonane (cas: 93643-24-4Synthetic Route of C7H14N2).

(S)-1,4-Diazabicyclo[4.3.0]nonane (cas: 93643-24-4) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Synthetic Route of C7H14N2

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

CDK4/6 inhibitors downregulate the ubiquitin-conjugating enzymes UBE2C/S/T involved in the ubiquitin-proteasome pathway in ER + breast cancer was written by Lin, Chih-Yi;Yu, Chung-Jen;Liu, Chun-Yu;Chao, Ta-Chung;Huang, Chi-Cheng;Tseng, Ling-Ming;Lai, Jiun-I.. And the article was included in Clinical and Translational Oncology in 2022.Related Products of 1211441-98-3 This article mentions the following:

Abstract: Despite significant improvement in therapeutic development in the past decades, breast cancer remains a formidable cause of death for women worldwide. The hormone pos. subtype (HR( +)) (also known as luminal type) is the most prevalent category of breast cancer, comprising 鈭?70% of patients. The clin. success of the three CDK4/6 inhibitors palbociclib, ribociclib, and abemaciclib has revolutionized the treatment of choice for metastatic HR( +) breast cancer. Accumulating evidence demonstrate that the properties of CDK4/6 inhibitors extend beyond inhibition of the cell cycle, including modulation of immune function, sensitizing PI3K inhibitors, metabolism reprogramming, kinome rewiring, modulation of the proteasome, and many others. The ubiquitin-proteasome pathway (UPP) is a crucial cellular proteolytic system that maintains the homeostasis and turnover of proteins. By transcriptional profiling of the HR( +) breast cancer cell lines MCF7 and T47D treated with Palbociclib, we have uncovered a novel mechanism that demonstrates that the CDK4/6 inhibitors suppress the expression of three ubiquitin-conjugating enzymes UBE2C, UBE2S, UBE2T. Further validation in the HR( +) cell lines show that Palbociclib and ribociclib decrease UBE2C at both the mRNA and protein level, but this phenomenon was not shared with abemaciclib. These three E2 enzymes modulate several E3 ubiquitin ligases, including the APC/C complex which plays a role in G1/S progression. We further demonstrate that the UBE2C/UBE2T expression levels are associated with breast cancer survival, and HR( +) breast cancer cells demonstrate dependence on the UBE2C. Our study suggests a novel link between CDK4/6 inhibitor and UPP pathway, adding to the potential mechanisms of their clin. efficacy in cancer. In the experiment, the researchers used many compounds, for example, 7-Cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide (cas: 1211441-98-3Related Products of 1211441-98-3).

7-Cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide (cas: 1211441-98-3) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 掳C and boils at 125鈥?30 掳C. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.Related Products of 1211441-98-3

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