Month: February 2023

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

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

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

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

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

Discovery of new thieno[3,2-d]pyrimidine derivatives targeting EGFR^L858R/T790M NSCLCs by the conformation constrained strategy was written by Chen, Yang;Yang, Linlin;Qiao, Hui;Cheng, Zhongyu;Xie, Jiahao;Zhou, Wenjuan;Huang, Xin;Jiang, Yaoxuan;Yu, Bin;Zhao, Wen. And the article was included in European Journal of Medicinal Chemistry in 2020.Related Products of 611225-86-6 This article mentions the following:

Studies on the third-generation of epidermal growth factor receptor tyrosine kinase inhibitors (EGFRTKIs) targeting EGFR^L858R/T790M mutant remain hotspots, specifically for non-small cell lung cancer(NSCLC) were described. In the current study, a new series of EGFR-TKIs with thieno[3,2-d]pyrimidine derivatives bearing quinolin-2(1H)-ones I (R = 4-fluoro-phenylamino, 4-(4-methyl-piperazin-1-yl)-phenylamino, 4-morpholin-4-ylmethyl-phenylamino, etc.) was designed and synthesized, through conformational constrained strategy from the third generation of EGFR-TKI olmutinib. In vitro structure-activity relationship (SAR) studies indicated that compounds I (R = 4-(4-methyl-piperazin-1-yl)-phenylamino, 4-[1,4′]bipiperidinyl-1′-yl-3-fluoro-phenylamino, 4-(4-methyl-piperazin-1-ylmethyl)-phenylamino, 4-(4-ethyl-piperazin-1-ylmethyl)-phenylamino, 4-(2-(dimethylamino)ethylamino)-3-fluorophenylamino) exhibited good selective inhibition to EGFR^L858R/T790M (IC₅₀ 閳?250 nM) over wild type EGFR (IC₅₀ > 10000 nM). The observed selectivity of compounds I (R = 4-[1,4′]bipiperidinyl-1′-yl-3-fluoro-phenylamino, 4-(2-(dimethylamino)ethylamino)-3-fluorophenylamino) (A) was also proved by the computational mol. docking and the cellular thermal shift assay. These compounds I had good growth inhibitory effect on the four tested cancer cell lines. Specifically, I (R = 4-(2-(dimethylamino)ethylamino)-3-fluorophenylamino) could significantly inhibit the colony formation, wound healing and the expression of p-EGFR and its downstream p-ERK in EGFR^L858R/T790M H1975 lung cancer cells. The above finding results suggest that the thieno[3,2-d]pyrimidine compounds, especially compounds A, can selectively target the mutant EGFR^L858R/T790M in vitro and at cellular level and may serve as the lead compounds for generating new series of the third generation EGFR-TKIs. In the experiment, the researchers used many compounds, for example, 4-(4-Ethylpiperazin-1-ylmethyl)phenylamine (cas: 611225-86-6Related Products of 611225-86-6).

4-(4-Ethylpiperazin-1-ylmethyl)phenylamine (cas: 611225-86-6) 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.Related Products of 611225-86-6

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

Two birds with one stone: dendrimer surface engineering enables tunable periphery hydrophobicity and rapid endosomal escape was written by Wang, Zheng;Chen, Chao;Liu, Ruihong;Fan, Aiping;Kong, Deling;Zhao, Yanjun. And the article was included in Chemical Communications (Cambridge, United Kingdom) in 2014.Quality Control of 1-Propylpiperazine This article mentions the following:

Multifunctional thermosensitive dendrimeric nanocarriers were generated via tailored surface modification. Such design not only facilitated the rapid endosomal escape of dendrimers, but also achieved tunable surface hydrophobicity, which could be employed to achieve on-demand cargo release. These smart dendrimers are promising for enhancing intracellular drug delivery. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Quality Control of 1-Propylpiperazine).

1-Propylpiperazine (cas: 21867-64-1) 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.Quality Control of 1-Propylpiperazine

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

New 1-aryl-3-substituted propanol derivatives as antimalarial agents was written by Perez-Silanes, Silvia;Berrade, Luis;Garcia-Sanchez, Rory N.;Mendoza, Adela;Galiano, Silvia;Perez-Solorzano, Berta Martin;Nogal-Ruiz, Juan J.;Martinez-Fernandez, Antonio R.;Aldana, Ignacio;Monge, Antonio. And the article was included in Molecules in 2009.Application In Synthesis of 1-Boc-4-(4-Nitrophenyl)piperazine This article mentions the following:

This paper describes the synthesis and in vitro antimalarial activity against a P. falciparum 3D7 strain of some new 1-aryl-3-substituted propanol derivatives Twelve of the tested compounds showed an IC₅₀ lower than 1 娓璏. These compounds were also tested for cytotoxicity in murine J774 macrophages. The most active compounds were evaluated for in vivo activity against P. berghei in a 4-day suppressive test. Compound 12 inhibited more than 50% of parasite growth at a dose of 50 mg/kg/day. In addition, an FBIT test was performed to measure the ability to inhibit ferriprotoporphyrin biocrystn. This data indicates that 1-aryl-3-substituted propanol derivatives hold promise as a new therapeutic option for the treatment of malaria. In the experiment, the researchers used many compounds, for example, 1-Boc-4-(4-Nitrophenyl)piperazine (cas: 182618-86-6Application In Synthesis of 1-Boc-4-(4-Nitrophenyl)piperazine).

1-Boc-4-(4-Nitrophenyl)piperazine (cas: 182618-86-6) 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. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Application In Synthesis of 1-Boc-4-(4-Nitrophenyl)piperazine

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

Conversion of 4-cyanomethyl-pyrazole-3-carboxamides into CB1 antagonists with lowered propensity to pass the blood-brain-barrier was written by Receveur, Jean-Marie;Murray, Anthony;Linget, Jean-Michel;Norregaard, Pia K.;Cooper, Martin;Bjurling, Emelie;Nielsen, Peter Aadal;Hoegberg, Thomas. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2010.Recommanded Product: 6-(Piperazin-1-yl)nicotinonitrile This article mentions the following:

A series of amides, amidines and amidoximes have been made from the corresponding nitrile compounds, to provide potent antagonists and inverse agonists for the CB1 receptor with considerably lower lipophilicity, higher polar surface area and improved plasma/brain ratios compared to the centrally acting rimonabant. Extensive investigations of ADME and in vivo pharmacol. properties led to selection of the amide series and specifically the 4-(4-fluorophenyl)piperidin-4-ol derivative D4. A clear improvement in the peripheral profile over rimonabant was seen, although some contribution of central effect on the pronounced weight reduction in obese mice cannot be ruled out. In the experiment, the researchers used many compounds, for example, 6-(Piperazin-1-yl)nicotinonitrile (cas: 149554-29-0Recommanded Product: 6-(Piperazin-1-yl)nicotinonitrile).

6-(Piperazin-1-yl)nicotinonitrile (cas: 149554-29-0) 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. 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.Recommanded Product: 6-(Piperazin-1-yl)nicotinonitrile

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

Synthesis of substituted 5-amino-3-aryl-4-(methoxycarbonyl)isoxazoles was written by Alyab’ev, S. B.;Kosul’nikova, T. S.;Dmitriev, D. E.;Il’in, A. P.;Kravchenko, D. V.;Filimonov, S. I.;Ivashchenko, A. V.. And the article was included in Izvestiya Vysshikh Uchebnykh Zavedenii, Khimiya i Khimicheskaya Tekhnologiya in 2007.Category: piperazines This article mentions the following:

A combinatorial library of substituted 5-amino-3-aryl-4-(methoxycarbonyl)isoxazoles was obtained by reaction of 3-aryl-4-methoxycarbonyl-5-chloroisoxazoles with primary and secondary amines in 1,4-dioxane in the presence of NEt₃ under parallel synthesis conditions. Products were obtained in yields of 21-95%. This reaction proceeds less uniformly in DMF in the presence of K₂CO₃, and, in the case of primary amines, bis(4-methoxycarbonyl-3-aryl-isoxazol-5-yl)arylamines are also formed in 20-69% yields. In the experiment, the researchers used many compounds, for example, 4-(4-Ethylpiperazin-1-ylmethyl)phenylamine (cas: 611225-86-6Category: piperazines).

4-(4-Ethylpiperazin-1-ylmethyl)phenylamine (cas: 611225-86-6) 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. 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.Category: piperazines

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