Category: 41838-46-4

Combining structure- and property-based optimization to identify selective FLT3-ITD inhibitors with good antitumor efficacy in AML cell inoculated mouse xenograft model was written by Heng, Hao;Wang, Zhijie;Li, Hongmei;Huang, Yatian;Lan, Qingyuan;Guo, Xiaoxing;Zhang, Liang;Zhi, Yanle;Cai, Jiongheng;Qin, Tianren;Xiang, Li;Wang, Shuxian;Chen, Yadong;Lu, Tao;Lu, Shuai. And the article was included in European Journal of Medicinal Chemistry in 2019.Synthetic Route of C6H14N2 This article mentions the following:

FLT3 mutation is among the most common genetic mutations in acute myeloid leukemia (AML), which is also related with poor overall survival and refractory in AML patients. Recently, FLT3 inhibitors have been approved for AML therapy. Herein, a series of new compounds with pyrazole amine scaffold was discovered, which showed potent inhibitory activity against FLT3-ITD and significant selectivity against both FLT3-ITD and AML cells expressing FLT3-ITD. Compound 46, possessing the most promising cellular activity, blocked the autophosphorylation of FLT3 pathway in MV4-11 cell line. Furthermore, the apoptosis and down regulation of P-STAT5 were also observed in tumor cells extracted from the MV4-11 cell xenografts model upon compound 46 treatment. Compound 46 was also metabolically stable in vitro and suppressed tumor growth significantly in MV4-11 xenografts model in vivo. Compound 46 showed no toxicity to the viscera of mice and caused no decrease in body weight of mice. In conclusion, the results of this study could provide valuable insights into discovery of new FLT3 inhibitors, and compound 46 was worthy of further development as potential drug candidate to treat AML. In the experiment, the researchers used many compounds, for example, 4-Amino-1-methylpiperidine (cas: 41838-46-4Synthetic Route of C6H14N2).

4-Amino-1-methylpiperidine (cas: 41838-46-4) belongs to piperidine derivatives.Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Several piperidine alkaloids isolated from natural herbs, were found to exhibit antiproliferation and antimetastatic effects on various types of cancers both in vitro and in vivo for example Piperine, Evodiamine, Matrine, Berberine and Tetrandine.Synthetic Route of C6H14N2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

CO₂ absorption performance in advanced water-lean diamine solvents was written by Xu, Yanjie;Wang, Tao;Yang, Qi;Yu, Hai;Fang, Mengxiang;Puxty, Graeme. And the article was included in Chemical Engineering Journal (Amsterdam, Netherlands) in 2021.SDS of cas: 41838-46-4 This article mentions the following:

In an effort to reduce energy penalties, a range of advanced water-lean solutions blended from one of 8 diamines, an organic solvent diluent and water, were screened. The diamines N,N-dimethyl-1,3-propanediamine and N,N-dimethyl-1,2-ethanediamine with one primary and one tertiary amino group remain homogenous during CO₂ uptake with the addition of cosolvents (1-methyl-2-pyrrolidinone or sulfolane) and are further investigated for absorption and desorption performance compared with their corresponding aqueous solutions Water-lean solutions with different water concentrations are tested to explain the impact of water content on the solution performance. Phys. properties such as d. and viscosity are also measured for a versatile evaluation. The results show that diamine water-lean solutions obtain low viscosity, preferable cyclic capacities and rapid absorption and desorption rates. ENH-5% H₂O (mass ratio DMEDA: NMP: H₂O = 3:6.5:0.5) shows the most competitive advantages with comparable viscosity (1.49 mPa鈥 at 313 K) to aqueous MEA-H₂O and a 140% improvement in cyclic capacity. Four-fold higher desorption rate is gained ESH-5%H₂O (mass ratio DMEDA: SFL: H₂O = 3:6.5:0.5) compared with MEA-H₂O. Considerable reduction in energy penalties is expected to be achieved in diamine water-lean solutions In addition, the equilibrium solubility of diamine water-lean solutions also shows potential for industrial application due to their sensitivity to CO₂ partial pressure in contrast with aqueous solutions In the experiment, the researchers used many compounds, for example, 4-Amino-1-methylpiperidine (cas: 41838-46-4SDS of cas: 41838-46-4).

4-Amino-1-methylpiperidine (cas: 41838-46-4) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.SDS of cas: 41838-46-4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Discovery of AS-0141, a Potent and Selective Inhibitor of CDC7 Kinase for the Treatment of Solid Cancers was written by Irie, Takayuki;Asami, Tokiko;Sawa, Ayako;Uno, Yuko;Taniyama, Chika;Funakoshi, Yoko;Masai, Hisao;Sawa, Masaaki. And the article was included in Journal of Medicinal Chemistry in 2021.Computed Properties of C6H14N2 This article mentions the following:

CDC7, a serine-threonine kinase, plays conserved and important roles in regulation of DNA replication and has been recognized as a potential anticancer target. We report here the optimization of a series of furanone analogs starting from compound 1 with a focus on ADME properties suitable for clin. development. By replacing the 2-chlorobenzene moiety in 1 with various aliphatic groups, we identified compound 24 as a potent CDC7 inhibitor with excellent kinase selectivity and favorable oral bioavailability in multiple species. Oral administration of 24 demonstrated robust in vivo antitumor efficacy in a colorectal cancer xenograft model. Compound 24 (AS-0141) is currently in phase I clin. trials for the treatment of solid cancers. In the experiment, the researchers used many compounds, for example, 4-Amino-1-methylpiperidine (cas: 41838-46-4Computed Properties of C6H14N2).

4-Amino-1-methylpiperidine (cas: 41838-46-4) belongs to piperidine derivatives. The piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.Computed Properties of C6H14N2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Focused library design and synthesis of 2-mercapto benzothiazole linked 1,2,4-oxadiazoles as COX-2/5-LOX inhibitors was written by Yatam, Satayanarayana;Gundla, Rambabu;Jadav, Surender Singh;Pedavenkatagari, Narayana reddy;Chimakurthy, Jithendra;Rani B, Namratha;Kedam, Thyagaraju. And the article was included in Journal of Molecular Structure in 2018.Application In Synthesis of 4-Amino-1-methylpiperidine This article mentions the following:

Mercapto benzothiazole linked 1,2,4-oxadiazole derivatives were designed as anti-inflammatory agents using bioisosteric approach and docking studies. The docking results clearly indicated that the compounds shown good docking interaction towards COX-2 enzyme. In silico drug-like properties were also calculated for the prepared compounds and exhibited significant H-bond acceptor ratio. All compounds were synthesized and biol. evaluated using in vitro COX-1, COX-2 and 5-LOX assays. Compound I and II (IC₅₀ = 6.8 渭M and IC₅₀ = 5.0 渭M) found to be potent, selective COX-2 inhibitors and display better anti-inflammatory activity than standard Ibuprofen. Compound III and IV found to be potent inhibitors against 5-LOX (IC₅₀ = 5.1 渭M and IC₅₀ = 5.5 渭M). The in vivo anti-inflammatory activity studies shown that the compounds II and I effectively reducing the paw edema volume at 3h and 5h than standard drug Ibuprofen. The DPPH radical scavenging activity provided anti-oxidant activity of compound IV (IC₅₀ = 25.6 渭M) than reference standard Ascorbic acid. In the experiment, the researchers used many compounds, for example, 4-Amino-1-methylpiperidine (cas: 41838-46-4Application In Synthesis of 4-Amino-1-methylpiperidine).

4-Amino-1-methylpiperidine (cas: 41838-46-4) belongs to piperidine derivatives.Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Fluorinated piperidines are also the subject of continued interest in medicinal chemistry, for example in the synthesis of selective dipeptidyl peptidase II (DPP II) inhibitors. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions.Application In Synthesis of 4-Amino-1-methylpiperidine

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Scaffold and Parasite Hopping: Discovery of New Protozoal Proliferation Inhibitors was written by Singh, Baljinder;Bernatchez, Jean A.;McCall, Laura-Isobel;Calvet, Claudia M.;Ackermann, Jasmin;Souza, Julia M.;Thomas, Diane;Silva, Everton M.;Bachovchin, Kelly A.;Klug, Dana M.;Jalani, Hitesh B.;Bag, Seema;Buskes, Melissa J.;Leed, Susan E.;Roncal, Norma E.;Penn, Erica C.;Erath, Jessey;Rodriguez, Ana;Sciotti, Richard J.;Campbell, Robert F.;McKerrow, James;Siqueira-Neto, Jair L.;Ferrins, Lori;Pollastri, Michael P.. And the article was included in ACS Medicinal Chemistry Letters in 2020.Application of 41838-46-4 This article mentions the following:

Utilizing a target repurposing and parasite-hopping approach, we tested a previously reported library of compounds that were active against Trypanosoma brucei, plus 31 new compounds, against a variety of protozoan parasites including Trypanosoma cruzi, Leishmania major, Leishmania donovani, and Plasmodium falciparum. This led to the discovery of several compounds with submicromolar activities and improved physicochem. properties that are early leads toward the development of chemotherapeutic agents against kinetoplastid diseases and malaria. In the experiment, the researchers used many compounds, for example, 4-Amino-1-methylpiperidine (cas: 41838-46-4Application of 41838-46-4).

4-Amino-1-methylpiperidine (cas: 41838-46-4) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. Several piperidine alkaloids isolated from natural herbs, were found to exhibit antiproliferation and antimetastatic effects on various types of cancers both in vitro and in vivo for example Piperine, Evodiamine, Matrine, Berberine and Tetrandine.Application of 41838-46-4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Trisubstituted thiazoles as potent and selective inhibitors of Plasmodium falciparum protein kinase G (PfPKG) was written by Tsagris, Denise J.;Birchall, Kristian;Bouloc, Nathalie;Large, Jonathan M.;Merritt, Andy;Smiljanic-Hurley, Ela;Wheldon, Mary;Ansell, Keith H.;Kettleborough, Catherine;Whalley, David;Stewart, Lindsay B.;Bowyer, Paul W.;Baker, David A.;Osborne, Simon A.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2018.COA of Formula: C6H14N2 This article mentions the following:

A series of trisubstituted thiazoles have been identified as potent inhibitors of Plasmodium falciparum (Pf) cGMP-dependent protein kinase (PfPKG) through template hopping from known Eimeria PKG (EtPKG) inhibitors. The thiazole series has yielded compounds with improved potency, kinase selectivity and good in vitro ADME properties. These compounds could be useful tools in the development of new anti-malarial drugs in the fight against drug resistant malaria. In the experiment, the researchers used many compounds, for example, 4-Amino-1-methylpiperidine (cas: 41838-46-4COA of Formula: C6H14N2).

4-Amino-1-methylpiperidine (cas: 41838-46-4) belongs to piperidine derivatives. Piperidine has a role as a reagent, a protic solvent, a base, a catalyst, a plant metabolite, a human metabolite and a non-polar solvent. Several piperidine alkaloids isolated from natural herbs, were found to exhibit antiproliferation and antimetastatic effects on various types of cancers both in vitro and in vivo for example Piperine, Evodiamine, Matrine, Berberine and Tetrandine.COA of Formula: C6H14N2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Scaffold and Parasite Hopping: Discovery of New Protozoal Proliferation Inhibitors was written by Singh, Baljinder;Bernatchez, Jean A.;McCall, Laura-Isobel;Calvet, Claudia M.;Ackermann, Jasmin;Souza, Julia M.;Thomas, Diane;Silva, Everton M.;Bachovchin, Kelly A.;Klug, Dana M.;Jalani, Hitesh B.;Bag, Seema;Buskes, Melissa J.;Leed, Susan E.;Roncal, Norma E.;Penn, Erica C.;Erath, Jessey;Rodriguez, Ana;Sciotti, Richard J.;Campbell, Robert F.;McKerrow, James;Siqueira-Neto, Jair L.;Ferrins, Lori;Pollastri, Michael P.. And the article was included in ACS Medicinal Chemistry Letters in 2020.Application of 41838-46-4 This article mentions the following:

Utilizing a target repurposing and parasite-hopping approach, we tested a previously reported library of compounds that were active against Trypanosoma brucei, plus 31 new compounds, against a variety of protozoan parasites including Trypanosoma cruzi, Leishmania major, Leishmania donovani, and Plasmodium falciparum. This led to the discovery of several compounds with submicromolar activities and improved physicochem. properties that are early leads toward the development of chemotherapeutic agents against kinetoplastid diseases and malaria. In the experiment, the researchers used many compounds, for example, 4-Amino-1-methylpiperidine (cas: 41838-46-4Application of 41838-46-4).

4-Amino-1-methylpiperidine (cas: 41838-46-4) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. Several piperidine alkaloids isolated from natural herbs, were found to exhibit antiproliferation and antimetastatic effects on various types of cancers both in vitro and in vivo for example Piperine, Evodiamine, Matrine, Berberine and Tetrandine.Application of 41838-46-4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Trisubstituted thiazoles as potent and selective inhibitors of Plasmodium falciparum protein kinase G (PfPKG) was written by Tsagris, Denise J.;Birchall, Kristian;Bouloc, Nathalie;Large, Jonathan M.;Merritt, Andy;Smiljanic-Hurley, Ela;Wheldon, Mary;Ansell, Keith H.;Kettleborough, Catherine;Whalley, David;Stewart, Lindsay B.;Bowyer, Paul W.;Baker, David A.;Osborne, Simon A.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2018.COA of Formula: C6H14N2 This article mentions the following:

A series of trisubstituted thiazoles have been identified as potent inhibitors of Plasmodium falciparum (Pf) cGMP-dependent protein kinase (PfPKG) through template hopping from known Eimeria PKG (EtPKG) inhibitors. The thiazole series has yielded compounds with improved potency, kinase selectivity and good in vitro ADME properties. These compounds could be useful tools in the development of new anti-malarial drugs in the fight against drug resistant malaria. In the experiment, the researchers used many compounds, for example, 4-Amino-1-methylpiperidine (cas: 41838-46-4COA of Formula: C6H14N2).

4-Amino-1-methylpiperidine (cas: 41838-46-4) belongs to piperidine derivatives. Piperidine has a role as a reagent, a protic solvent, a base, a catalyst, a plant metabolite, a human metabolite and a non-polar solvent. Several piperidine alkaloids isolated from natural herbs, were found to exhibit antiproliferation and antimetastatic effects on various types of cancers both in vitro and in vivo for example Piperine, Evodiamine, Matrine, Berberine and Tetrandine.COA of Formula: C6H14N2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Design and Synthesis of Potent Quinazolines as Selective β-Glucocerebrosidase Modulators was written by Zheng, Jianbin;Chen, Long;Schwake, Michael;Silverman, Richard B.;Krainc, Dimitri. And the article was included in Journal of Medicinal Chemistry in 2016.Quality Control of 4-Amino-1-methylpiperidine This article mentions the following:

Gaucher’s disease is a common genetic disease caused by mutations in the β-glucocerebrosidase (GBA1) gene that have been also linked to increased risk of Parkinson’s disease and Lewy body dementia. Stabilization of misfolded mutant β-glucocerebrosidase (GCase) represents an important therapeutic strategy in synucleinopathies. Here we report a novel class of GCase quinazoline inhibitors, obtained in a high throughput screening, with moderate potency against wild-type GCase. Rational design and a SAR study of this class of compounds led to a new series of quinazoline derivatives with single-digit nanomolar potency. These compounds were shown to selectively stabilize GCase when compared to other lysosomal enzymes and to increase N370S mutant GCase protein concentration and activity in cell assays. To the best of our knowledge, these mols. are the most potent noniminosugar GCase modulators to date that may prove useful for future mechanistic studies and therapeutic approaches in Gaucher’s and Parkinson’s diseases. In the experiment, the researchers used many compounds, for example, 4-Amino-1-methylpiperidine (cas: 41838-46-4Quality Control of 4-Amino-1-methylpiperidine).

4-Amino-1-methylpiperidine (cas: 41838-46-4) belongs to piperidine derivatives. Piperidine has a role as a reagent, a protic solvent, a base, a catalyst, a plant metabolite, a human metabolite and a non-polar solvent. Several piperidine alkaloids isolated from natural herbs, were found to exhibit antiproliferation and antimetastatic effects on various types of cancers both in vitro and in vivo for example Piperine, Evodiamine, Matrine, Berberine and Tetrandine.Quality Control of 4-Amino-1-methylpiperidine

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem