Month: February 2023

FGFR1 Cooperates with EGFR in Lung Cancer Oncogenesis, and Their Combined Inhibition Shows Improved Efficacy was written by Quintanal-Villalonga, Alvaro;Molina-Pinelo, Sonia;Cirauqui, Cristina;Ojeda-Marquez, Laura;Marrugal, Angela;Suarez, Rocio;Conde, Esther;Ponce-Aix, Santiago;Enguita, Ana Belen;Carnero, Amancio;Ferrer, Irene;Paz-Ares, Luis. And the article was included in Journal of Thoracic Oncology in 2019.Recommanded Product: 872511-34-7 This article mentions the following:

There is substantial evidence for the oncogenic effects of fibroblast growth factor receptor 1 (FGFR1) in many types of cancer, including lung cancer, but the role of this receptor has not been addressed specifically in lung adenocarcinoma. We performed FGFR1 and EGFR overexpression and co-overexpression assays in adenocarcinoma and in inmortalized lung cell lines, and we also carried out surrogate and interaction assays. We performed monotherapy and combination EGFR/FGFR inhibitor sensitivity assays in vitro and in vivo in cell line- and patient-derived xenografts. We determined FGFR1 mRNA expression in a cohort of patients with anti-EGFR therapy-treated adenocarcinoma. We have reported a cooperative interaction between FGFR1 and EGFR in this context, resulting in increased EGFR activation and oncogenic signaling. We have provided in vitro and in vivo evidence indicating that FGFR1 expression increases tumorigenicity in cells with high EGFR activation in EGFR-mutated and EGFR wild-type models. At the clin. level, we have shown that high FGFR1 expression levels predict higher resistance to erlotinib or gefitinib in a cohort of patients with tyrosine kinase inhibitor-treated EGFR-mutated and EGFR wild-type lung adenocarcinoma. Dual EGFR and FGFR inhibition in FGFR1-overexpressing, EGFR-activated models shows synergistic effects on tumor growth in vitro and in cell line- and patient-derived xenografts, suggesting that patients with tumors bearing these characteristics may benefit from combined EGFR/FGFR inhibition. These results support the extended the use of EGFR inhibitors beyond monotherapy in the EGFR-mutated adenocarcinoma setting in combination with FGFR inhibitors for selected patients with increased FGFR1 overexpression and EGFR activation. 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: 872511-34-7).

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 belongs to the family of medicines called anthelmintics. 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: 872511-34-7

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

Inhibition of CDK4/6 kinases causes production of aneuploid oocytes by inactivating the spindle assembly checkpoint and accelerating first meiotic progression was written by Dong, Feng;Meng, Tie-Gang;Li, Jian;Wang, Feng;Li, Yuan-yuan;Ouyang, Ying-Chun;Hou, Yi;Wang, Zhen-Bo;Schatten, Heide;Sun, Qing-Yuan. And the article was included in Biochimica et Biophysica Acta, Molecular Cell Research in 2021.COA of Formula: C23H30N8O This article mentions the following:

Cyclin D-CDK4/6 complex mediates the transition from the G1 to S phase in mammalian somatic cells. Meiotic oocytes pass through the G2/M transition and complete the first meiosis to reach maturation at the metaphase of meiosis II without intervening S phase, while Cyclin D-CDK4/6 complex is found to express during meiotic progression. Whether Cyclin D-CDK4/6 complex regulates meiotic cell cycle progression is not known. Here, we found its different role in oocyte meiosis: Cyclin D-CDK4/6 complex served as a regulator of spindle assembly checkpoint (SAC) to prevent aneuploidy in meiosis I. Inhibition of CDK4/6 kinases disrupted spindle assembly, chromosome alignment and kinetochore-microtubule attachments, but unexpectedly accelerated meiotic progression by inactivating SAC, consequently resulting in production of aneuploid oocytes. Further studies showed that the MPF activity decrease before first polar body extrusion was accelerated probably by inactivation of the SAC to promote ubiquitin-mediated cyclin B1 degradation Taken together, these data reveal a novel role of Cyclin D-CDK4/6 complex in mediating control of the SAC in female meiosis I. 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: 1211441-98-3COA of Formula: C23H30N8O).

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. Piperazine belongs to the family of medicines called anthelmintics. 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).COA of Formula: C23H30N8O

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

Palladium-Catalyzed Regio- and Stereoselective γ-Arylation of Tertiary Allylic Amines: Identification of Potent Adenylyl Cyclase Inhibitors was written by Ye, Zhishi;Brust, Tarsis F.;Watts, Val J.;Dai, Mingji. And the article was included in Organic Letters in 2015.COA of Formula: C17H18F2N2 This article mentions the following:

Substituted allylic amines and their derivatives are key structural motifs of many drug mols. and natural products. A general, mild, and practical palladium-catalyzed γ-arylation of tertiary allylic amines, one of the most challenging Heck arylation substrates, has been developed. The γ-arylation products, e.g. I, were obtained in excellent regio- and stereoselectivity. Moreover, novel and potent adenylyl cyclase inhibitors with the potential for treating neuropathic and inflammatory pain have been identified from the γ-arylation products. In the experiment, the researchers used many compounds, for example, 4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9COA of Formula: C17H18F2N2).

4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. 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.COA of Formula: C17H18F2N2

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

N-Alkyl-4-piperidinyl-2,3-diarylpyrrole derivatives with heterocyclic substitutions as potent and broad spectrum anticoccidial agents was written by Liang, Gui-Bai;Qian, Xiaoxia;Feng, Dennis;Fisher, Michael;Crumley, Tami;Darkin-Rattray, Sandra J.;Dulski, Paula M.;Gurnett, Anne;Leavitt, Penny Sue;Liberator, Paul A.;Misura, Andrew S.;Samaras, Samantha;Tamas, Tamas;Schmatz, Dennis M.;Wyvratt, Matthew;Biftu, Tesfaye. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2008.Application In Synthesis of 1,4-Dimethylpiperazine-2-carboxylic acid This article mentions the following:

Diaryl-(4-piperidinyl)pyrrole derivatives bearing cyclic amine substituents, e. g. I and II, have been synthesized and evaluated as anticoccidial agents. Improvements in potency of Et-PKG inhibition, such as azetidine derivative 3a, and broad spectrum anticoccidial activities in feed, such as morpholine derivative 8c, have been achieved. In the experiment, the researchers used many compounds, for example, 1,4-Dimethylpiperazine-2-carboxylic acid (cas: 58895-88-8Application In Synthesis of 1,4-Dimethylpiperazine-2-carboxylic acid).

1,4-Dimethylpiperazine-2-carboxylic acid (cas: 58895-88-8) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. 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.Application In Synthesis of 1,4-Dimethylpiperazine-2-carboxylic acid

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

Visible fluorescence and chemical structure. III. Double-bond nitrogen compounds and amine hydrochlorides was written by Bertrand, Didier. And the article was included in Bull. soc. chim. in 1945.Electric Literature of C4H12Cl2N2 This article mentions the following:

The double-bond N gives a fluorescence spectrum radically different from those of the amines and anilines studied. The effect of HCl is frequently to alter the intensity but not the shape of the spectral curve of the base. Fluorescence spectra are given for pyridine, quinoline, isoquinoline, acridine, N-benzylidenebenzylamine, N-heptylidenebenzylamine, and the hydrochlorides of pyridine, quinoline, isoquinoline, acridine, N-benzylideneaniline, N-benzylidenebenzylamine, N-benzylidene-β-naphthylamine, β-naphthylamine, carbazole, piperazine, PhNHEt, PhNEt₂, 2-phenylethylamine, tetrahydroquinoline, and tetrahydroisoquinoline. In the experiment, the researchers used many compounds, for example, Piperazine Dihydrochloride (cas: 142-64-3Electric Literature of C4H12Cl2N2).

Piperazine Dihydrochloride (cas: 142-64-3) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. 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.Electric Literature of C4H12Cl2N2

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

Combined serotonin (5-HT)_1A agonism, 5-HT_2A and dopamine D₂ receptor antagonism reproduces atypical antipsychotic drug effects on phencyclidine-impaired novel object recognition in rats was written by Oyamada, Yoshihiro;Horiguchi, Masakuni;Rajagopal, Lakshmi;Miyauchi, Masanori;Meltzer, Herbert Y.. And the article was included in Behavioural Brain Research in 2015.Electric Literature of C27H37N5O9 This article mentions the following:

Subchronic administration of an N-methyl-D-aspartate receptor (NMDAR) antagonist, e.g. phencyclidine (PCP), produces prolonged impairment of novel object recognition (NOR), suggesting they constitute a hypoglutamate-based model of cognitive impairment in schizophrenia (CIS). Acute administration of atypical, e.g. lurasidone, but not typical antipsychotic drugs (APDs), e.g. haloperidol, are able to restore NOR following PCP (acute reversal model). Furthermore, atypical APDs, when co-administered with PCP, have been shown to prevent development of NOR deficits (prevention model). Most atypical, but not typical APDs, are more potent 5-HT_2A receptor inverse agonists than dopamine (DA) D₂ antagonists, and have been shown to enhance cortical and hippocampal efflux and to be direct or indirect 5-HT_1A agonists in vivo. To further clarify the importance of these actions to the restoration of NOR by atypical APDs, sub-effective or non-EDs of combinations of the 5-HT_1A partial agonist (tandospirone), the 5-HT_2A inverse agonist (pimavanserin), or the D₂ antagonist (haloperidol), as well as the combination of all three agents, were studied in the acute reversal and prevention PCP models of CIS. Only the combination of all three agents restored NOR and prevented the development of PCP-induced deficit. Thus, this triple combination of 5-HT_1A agonism, 5-HT_2A antagonism/inverse agonism, and D₂ antagonism is able to mimic the ability of atypical APDs to prevent or ameliorate the PCP-induced NOR deficit, possibly by stimulating signaling cascades from D₁ and 5-HT_1A receptor stimulation, modulated by D₂ and 5-HT_2A receptor antagonism. 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: 112457-95-1Electric Literature of C27H37N5O9).

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. Simple N-substituted piperazines have been found in many drug molecules. 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.Electric Literature of C27H37N5O9

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

Effects of KB-2796, a new diphenylpiperazine calcium antagonist, on renal hemodynamics and urine formation in anesthetized dogs was written by Iwamoto, Takahiro;Morita, Tominori;Sukamoto, Takayuki;Ito, Keizo. And the article was included in Japanese Journal of Pharmacology in 1992.Computed Properties of C27H32Cl2F2N2O3 This article mentions the following:

The effects of KB-2796, a new calcium antagonist with a diphenylpiperazine moiety, on renal hemodynamics and urine formation were investigated in anesthetized dogs. I.v. infusion of KB-2796 (10, 30, and 100 μg/kg/min) decreased mean blood pressure (MBP) and renal vascular resistance (RVR) in a dose-dependent manner, but did not change renal blood flow (RBF). At the highest dose, glomerular filtration rate (GFR) and urine flow (UF) tended to decrease. Nicardipine (0.1, 0.3, and 1 μg/kg/min) also dose-dependently decreased MBP, RVR, GFR, and UF. When KB-2796 was infused into the renal artery at lower doses of 3 and 10 μg/kg/min, UF and urinary excretion of electrolytes increased without a significant change in RBF and GFR. Intrarenal infusion of KB-2796 at 30 μg/kg/min and nicardipine at 0.3 μg/kg/min produced a significant increase in GFR, RBF, UF, urinary excretion of electrolytes, and renin secretion rate. These results suggest that KB-2796 administered intrarenally exerts a diuretic action via tubular effects and the alteration of renal hemodynamics. However, its diuretic action might be masked by diminished urine formation via a reflex activation of the sympathetic nerves and/or via a reduction of renal perfusion pressure when it is administered systemically. In the experiment, the researchers used many compounds, for example, 1-(Bis(4-fluorophenyl)methyl)-4-(2,3,4-trimethoxybenzyl)piperazine dihydrochloride (cas: 101477-54-7Computed Properties of C27H32Cl2F2N2O3).

1-(Bis(4-fluorophenyl)methyl)-4-(2,3,4-trimethoxybenzyl)piperazine dihydrochloride (cas: 101477-54-7) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. 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.Computed Properties of C27H32Cl2F2N2O3

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

Structure-Activity Relationship Studies of Sulfonylpiperazine Analogues as Novel Negative Allosteric Modulators of Human Neuronal Nicotinic Receptors was written by Henderson, Brandon J.;Carper, Daniel J.;Gonzalez-Cestari, Tatiana F.;Yi, Bitna;Mahasenan, Kiran;Pavlovicz, Ryan E.;Dalefield, Martin L.;Coleman, Robert S.;Li, Chenglong;McKay, Dennis B.. And the article was included in Journal of Medicinal Chemistry in 2011.Formula: C10H14N2O2S This article mentions the following:

Neuronal nicotinic receptors have been implicated in several diseases and disorders such as autism, Alzheimer’s disease, Parkinson’s disease, epilepsy, and various forms of addiction. To understand the role of nicotinic receptors in these conditions, it would be beneficial to have selective mols. that target specific nicotinic receptors in vitro and in vivo. Our laboratory has previously identified novel neg. allosteric modulators of human α4β2 (Hα4β2) and human α3β4 (Hα3β4) nicotinic receptors. The effects of novel sulfonylpiperazine analogs that act as neg. allosteric modulators in both Hα4β2 nAChRs and Hα3β4 nAChRs were investigated. This work, through structure-activity relationship (SAR) studies, describes the chem. features of these mols. that are important for both potency and selectivity on Hα4β2 nAChRs. In the experiment, the researchers used many compounds, for example, 1-(Phenylsulfonyl)piperazine (cas: 14172-55-5Formula: C10H14N2O2S).

1-(Phenylsulfonyl)piperazine (cas: 14172-55-5) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. 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.Formula: C10H14N2O2S

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

Re: Overall survival with palbociclib plus endocrine therapy versus capecitabine in postmenopausal patients with hormone receptor-positive, HER2-negative metastatic breast cancer in the PEARL study was written by Altundag, Kadri. And the article was included in European Journal of Cancer in 2022.SDS of cas: 571190-30-2 This article mentions the following:

A polemic in response to Martin et al. (Eur J Cancer 2022;168:12e24) is given. In a recent publication by Martin et al. concluded that Overall survival with palbociclib plus endocrine therapy vs. capecitabine in postmenopausal patients with hormone receptor-pos., HER2-neg. metastatic breast cancer. Specifically, the visceral metastatic burden was not described. It would be expected that tumors with a higher visceral tumor burden are less likely to be responsive to treatment. Second, weak estrogen receptor status (close similarity to triple-neg. breast cancer) has not been reported. The author concluded that these tumors seem to be more likely to be responsive to capecitabine than the palbociclib combination. 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: 571190-30-2SDS of cas: 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 belongs to the family of medicines called anthelmintics. 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.SDS of cas: 571190-30-2

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

Design and synthesis of C-12 dithiocarbamate andrographolide analogues as an anticancer agent was written by Arsakhant, Patcharee;Sirion, Uthaiwan;Chairoungdua, Arthit;Suksen, Kanoknetr;Piyachaturawat, Pawinee;Suksamrarn, Apichart;Saeeng, Rungnapha. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2020.Application of 27469-60-9 This article mentions the following:

A series of 21 new analogs of C-12 dithiocarbamate andrographolide, I (R = morpholino, 4-phenylpiperazino, dibenzylamino, etc.), was designed and synthesized from natural andrographolide isolated from a common Thai plant, Andrographis paniculata. The reaction used to manipulate the andrographolide scaffold was conducted in one pot under mild reaction conditions. This avoided toxic catalysts and gave nearly quant. yields of the new analogs, generally without byproducts and can be easily scaled up for industrial processing. All new analogs were evaluated against nine cancer cell lines; some analogs exhibited greater selective cytotoxic activity to MCF-7 cancer cell than that of the parent andrographolide and cancer drugs. In the experiment, the researchers used many compounds, for example, 4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9Application of 27469-60-9).

4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9) 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.Application of 27469-60-9

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