Category: piperazines

Characterization of DDR2 Inhibitors for the Treatment of DDR2 Mutated Nonsmall Cell Lung Cancer was written by Terai, Hideki;Tan, Li;Beauchamp, Ellen M.;Hatcher, John M.;Liu, Qingsong;Meyerson, Matthew;Gray, Nathanael S.;Hammerman, Peter S.. And the article was included in ACS Chemical Biology in 2015.Recommanded Product: 630125-91-6 This article mentions the following:

Despite advances in precision medicine approaches over the past decade, the majority of nonsmall cell lung cancers (NSCLCs) are refractory to treatment with targeted small mol. inhibitors. Previous work has identified mutations in the Discoidin Domain Receptor 2 (DDR2) kinase as potential therapeutic targets in NSCLCs. While DDR2 is potently targeted by several multitargeted kinase inhibitors, most notably dasatinib, toxicity has limited the clin. application of anti-DDR2 therapy. Here, the authors have characterized compound I and other tool compounds demonstrating selectivity for DDR2 and show that while these compounds inhibit DDR2 in lung cancer model systems, they display limited antiproliferative activity in DDR2 mutated cell lines as compared to dual DDR2/SRC inhibitors. The authors show that DDR2 and SRC are binding partners, that SRC activity is tied to DDR2 activation, and that dual inhibition of both DDR2 and SRC leads to enhanced suppression of DDR2 mutated lung cancer cell lines. These results support the further evaluation of dual SRC/DDR2 targeting in NSCLC, and the authors report a tool compound II which potently inhibits both SRC and DDR2 with a distinct selectivity profile as compared to dasatinib. In the experiment, the researchers used many compounds, for example, 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (cas: 630125-91-6Recommanded Product: 630125-91-6).

4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (cas: 630125-91-6) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 鎺矯 and boils at 125閳?30 鎺矯. 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.Recommanded Product: 630125-91-6

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

On-DNA Palladium-Catalyzed Hydrogenation-like Reaction Suitable for DNA-Encoded Library Synthesis was written by Priego, Julian;de Pedro Beato, Eduardo;Benavides, Jesus;Gironda-Martinez, Adrian;Gonzalez, Fernando;Blas, Jesus;Martin-Ortega, Maria Dolores;Rama-Garda, Ramon;Ezquerra, Jesus;Toledo, Miguel A.;Torrado, Alicia. And the article was included in Bioconjugate Chemistry in 2021.Safety of 4-((Benzyloxy)carbonyl)-1-(tert-butoxycarbonyl)piperazine-2-carboxylic acid This article mentions the following:

Herein we describe a method to orthogonally remove on-DNA N-Cbz, N-Alloc, N-Allyl, O-Bn, and O-Allyl protecting groups in the presence of other common protecting groups to afford free amines and carboxylic acids, resp. The developed method uses NaBH₄ as the source of hydrogen in the presence of Pd(OAc)₂ under DNA aqueous conditions. In addition, under the developed conditions we were able to successfully hydrogenate triple and double bonds to totally saturated compounds Furthermore, we introduce a new alternative procedure to reduce azides and aromatic nitro compounds to primary amines. In the experiment, the researchers used many compounds, for example, 4-((Benzyloxy)carbonyl)-1-(tert-butoxycarbonyl)piperazine-2-carboxylic acid (cas: 149057-19-2Safety of 4-((Benzyloxy)carbonyl)-1-(tert-butoxycarbonyl)piperazine-2-carboxylic acid).

4-((Benzyloxy)carbonyl)-1-(tert-butoxycarbonyl)piperazine-2-carboxylic acid (cas: 149057-19-2) belongs to piperazine derivatives. The piperazine scaffold is often found in biologically active compounds in different therapeutic areas. These therapeutic areas include antifungals, antidepressants, antivirals, and serotonin receptor (5-HT) antagonists/agonists. 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.Safety of 4-((Benzyloxy)carbonyl)-1-(tert-butoxycarbonyl)piperazine-2-carboxylic acid

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

Broad spectrum alkynyl inhibitors of T315I Bcr-Abl was written by Deng, Xianming;Lim, Sang Min;Zhang, Jianming;Gray, Nathanael S.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2010.Electric Literature of C14H20F3N3 This article mentions the following:

A series of alkyne-containing type II inhibitors with potent inhibitory activity of T315I Bcr-Abl has been identified. The most active compound 4 exhibits an EC₅₀ of less than 1 nM against wild-type Bcr-Abl and an EC₅₀ of 10 nM against T315I mutant but is broadly active against a number of other kinases. In the experiment, the researchers used many compounds, for example, 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (cas: 630125-91-6Electric Literature of C14H20F3N3).

4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (cas: 630125-91-6) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. 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.Electric Literature of C14H20F3N3

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

The preparation and reaction of enolates within micro reactors was written by Wiles, Charlotte;Watts, Paul;Haswell, Stephen J.;Pombo-Villar, Esteban. And the article was included in Tetrahedron in 2005.Computed Properties of C7H16N2 This article mentions the following:

Over the past 5 years, interest in the miniaturization of chem. synthesis has grown rapidly, however in order to facilitate transfer of the technol. from its current position as a research tool to industrial applications, a core understanding of the challenges associated with transferring reactions from the macro to the micro domain is required. This paper therefore aims to broach this problem by investigating the application of micro reactors to a range of commonly employed synthetic reactions including acylation, aldol, alkylation, 1,4-conjugate addition (Michael addition) and the Knoevenagel condensation. Comparison of the results obtained with traditional batch techniques aimed to highlight some of the advantages associated with micro reaction technol. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Computed Properties of C7H16N2).

1-Propylpiperazine (cas: 21867-64-1) 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.Computed Properties of C7H16N2

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

An amino-indazole scaffold with spectrum selective kinase inhibition of FLT3, PDGFR浼?and kit was written by Deng, Xianming;Zhou, Wenjun;Weisberg, Ellen;Wang, Jinhua;Zhang, Jianming;Sasaki, Takaaki;Nelson, Erik;Griffin, James D.;Janne, Pasi A.;Gray, Nathanael S.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2012.Product Details of 630125-91-6 This article mentions the following:

The synthesis and characterization of a number of 3-amino-1H-indazol-6-yl-benzamides that were designed to target the ‘DFG-out’ conformation of the kinase activation loop were reported. Several compounds such as I [R = H, Me] exhibit single-digit nanomolar EC₅₀s against FLT3, c-Kit and the gatekeeper T674M mutant of PDGFR浼? In the experiment, the researchers used many compounds, for example, 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (cas: 630125-91-6Product Details of 630125-91-6).

4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (cas: 630125-91-6) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Product Details of 630125-91-6

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

Nitroaldol reactions catalyzed by amine-MCM-41 hybrids was written by Wang, Qingqing;Shantz, Daniel F.. And the article was included in Journal of Catalysis in 2010.Product Details of 21867-64-1 This article mentions the following:

The catalytic properties of several amine-functionalized MCM-41 materials in a nitroaldol (Henry) reaction are reported. The work investigated the effects of organoamine type (primary, secondary, tertiary), amine d., and the presence of silanol groups on the catalytic activity and product selectivity. High selectivity to the nitro alc. product was achieved by introducing secondary and tertiary amine groups on the MCM-41 surface, while the nitroalkene is the dominant product for primary amines. Steric effects appear to be significant in determining the overall reactivity as the least sterically hindered amines are the most active. The capping of silanols with trimethylsilyl groups resulted in a reduction in catalytic activity for nearly all samples, indicating the importance of surface silanols and/or the surface polarity in the reaction. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Product Details of 21867-64-1).

1-Propylpiperazine (cas: 21867-64-1) 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. Although many piperazine derivatives occur naturally, piperazine itself can be synthesized by reacting alcoholic ammonia with 1,2-dichloroethane, by the action of sodium and ethylene glycol on ethylene diamine hydrochloride, or by reduction of pyrazine with sodium in ethanol.Product Details of 21867-64-1

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

New Heterocyclic Hepatitis C Virus (HCV) Inhibitors Containing A 2-Aminomethyl-1H-Indole Fragment was written by Ivachtchenko, A. V.;Yamanushkin, P. M.;Mit’kin, O. D.;Ezhova, E. V.;Korzinov, O. M.;Bulanova, E. A.;Bichko, V. V.;Ivashchenko, A. A.. And the article was included in Pharmaceutical Chemistry Journal in 2015.SDS of cas: 21867-64-1 This article mentions the following:

A focused library of heterocyclic compounds including a 2-aminomethyl-1H-benzimidazole, 2-aminomethylindole, benzofuran-2-ylmethylamine, or 2-piperazin-1-ylmethylbenzoxazole fragment was screened for the ability to inhibit in vitro hepatitis C virus (HCV). The synthetic methods were described. The antiviral activity and cytotoxicity data were presented. Most of the compounds carrying a benzoxazol-2-ylmethylamine fragment inhibited Huh7.3 human hepatoma cells infected in vitro with HCV with nanomolar potency but were inactive against the HCV RNA-replicon. The only exception was 9-methyl-N(6)-(3-nitrophenyl)-2,3,4,9-tetrahydro-1H-carbazole-1,6-diamine, which demonstrated nanomolar potency against HCV in both models. The most active and selective compounds were (piperazin-1-yl)-[(1H-indol-2-ylmethyl)piperidin-4-yl]-ketones (EC₅₀ 0.31-2.2 婵炴挾鎷? CC₅₀ 10.2-110 婵炴挾鎷? and 2-(1,2,3a,4,5,6-hexahydropyrazino[3,2,1-jk]carbazol-3-yl)acetamide (EC₅₀ 1.69闁?.5 婵炴挾鎷? CC₅₀ 114闁?2 婵炴挾鎷?. The two most selective inhibitors I (TI₅₀ = 52) and II (TI₅₀ = 68) were selected for further preclin. trials. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1SDS of cas: 21867-64-1).

1-Propylpiperazine (cas: 21867-64-1) 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: 21867-64-1

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

Synthesis and hypoglycemic activity of 7,8-dihydro-6H-thiopyrano[3,2-d]pyrimidine derivatives and related compounds was written by Ohno, Sachio;Mizukoshi, Kiyoshi;Komatsu, Osamu;Kuno, Yasuo;Nakamura, Yoshiki;Kato, Eiichi;Nagasaka, Mitsuaki. And the article was included in Chemical & Pharmaceutical Bulletin in 1986.Related Products of 21867-64-1 This article mentions the following:

Apparatus 80 amino piperazino derivatives of the title system were prepared and tested for hypoglycemic activity for potential use as antidiabetics. The most promising were I and II. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Related Products of 21867-64-1).

1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 闁硅櫣鐓?and boils at 125闂?30 闁硅櫣鐓? 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.Related Products of 21867-64-1

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

Discovery of 3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-[4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl]benzamide (AP24534), a Potent, Orally Active Pan-Inhibitor of Breakpoint Cluster Region-Abelson (BCR-ABL) Kinase Including the T315I Gatekeeper Mutant was written by Huang, Wei-Sheng;Metcalf, Chester A.;Sundaramoorthi, Raji;Wang, Yihan;Zou, Dong;Thomas, R. Mathew;Zhu, Xiaotian;Cai, Lisi;Wen, David;Liu, Shuangying;Romero, Jan;Qi, Jiwei;Chen, Ingrid;Banda, Geetha;Lentini, Scott P.;Das, Sasmita;Xu, Qihong;Keats, Jeff;Wang, Frank;Wardwell, Scott;Ning, Yaoyu;Snodgrass, Joseph T.;Broudy, Marc I.;Russian, Karin;Zhou, Tianjun;Commodore, Lois;Narasimhan, Narayana I.;Mohemmad, Qurish K.;Iuliucci, John;Rivera, Victor M.;Dalgarno, David C.;Sawyer, Tomi K.;Clackson, Tim;Shakespeare, William C.. And the article was included in Journal of Medicinal Chemistry in 2010.Recommanded Product: 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline This article mentions the following:

In the treatment of chronic myeloid leukemia (CML) with BCR-ABL kinase inhibitors, the T315I gatekeeper mutant has emerged as resistant to all currently approved agents. This report describes the structure-guided design of a novel series of potent pan-inhibitors of BCR-ABL, including the T315I mutation. A key structural feature is the carbon-carbon triple bond linker which skirts the increased bulk of Ile315 side chain. Extensive SAR studies led to the discovery of development candidate benzamide I (AP24534), which inhibited the kinase activity of both native BCR-ABL and the T315I mutant with low nM IC₅₀s, and potently inhibited proliferation of corresponding Ba/F3-derived cell lines. Daily oral administration of I significantly prolonged survival of mice injected i.v. with BCR-ABL^T315I expressing Ba/F3 cells. These data, coupled with a favorable ADME profile, support the potential of I to be an effective treatment for CML, including patients refractory to all currently approved therapies. In the experiment, the researchers used many compounds, for example, 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (cas: 630125-91-6Recommanded Product: 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline).

4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (cas: 630125-91-6) 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. 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. Recommanded Product: 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline

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

Synthesis, and antitumor activity of some N1-(7-coumarinyl)amidrazones and related congeners was written by Mustafa, Mohammad S.;El-Abadelah, Mustafa M.;Zihlif, Malek A.;Naffa, Randa G.;Mubarak, Mohammad S.. And the article was included in Molecules in 2011.Category: piperazines This article mentions the following:

Piperazine coumarin amidrazone derivatives and related congeners were designed, the synthesis of the target compounds was achieved using 2-oxo-N-(2-oxo-4-methyl-2H-1-benzopyran-7-yl)propanehydrazonoyl chloride and piperazine derivatives, piperidine, morpholine, thiomorpholine, 1-[2-ethyl-4-nitro-1-(phenylmethyl)-1H-imidazol-5-yl]piperazine, etc., as reactants and the products thus obtained [i.e., 1-(1-piperazinyl)-1,2-propanedione 1-[2-(3-methyl-2-oxo-2H-1-benzopyran-7-yl)hydrazone] derivatives, amidrazones] were confirmed by elemental analyses, ¹H-NMR, ¹³C-NMR, and ESI-HRMS spectral data. The title compounds were evaluated against the cell line MCF-7 (human mammary adenocarcinoma cell line), cell line K562 (human chronic myelogenous leukemia cell line), cell line HL60 (human promyelocytic leukemia cell line) and cell line ZR-75-1 (human mammary tumor, breast carcinoma cell line) it was discovered that they displayed activity as antitumor agents. Among all the compounds tested, 7-[2-[1-[4-(1-benzyl-2-ethyl-4-nitro-1H-imidazol-5-yl)-1-piperazinyl]-2-(oxo)propylidene]hydrazinyl]-4-methyl-2-chromenone was the most potent against MCF-7 and K562 cells, with IC₅₀ values of 20.2 and 9.3 婵炴挾鎷? resp. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Category: piperazines).

1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 闁硅櫣鐓?and boils at 125闂?30 闁硅櫣鐓? 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.Category: piperazines

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