Category: 182618-86-6

Discovery of the selective and efficacious inhibitors of FLT3 mutations was written by Zhi, Yanle;Li, Baoquan;Yao, Chao;Li, Hongmei;Chen, Puzhou;Bao, Jiyin;Qin, Tianren;Wang, Yue;Lu, Tao;Lu, Shuai. And the article was included in European Journal of Medicinal Chemistry in 2018.Reference of 182618-86-6 This article mentions the following:

Fms-like tyrosine kinase 3 (FLT3) is among the most frequently mutated protein in acute myeloid leukemia (AML), which has been confirmed as an important drug target for AML chemotherapy. Starting from the lead compound LT-106-175, a series of 1-H-pyrazole-3-carboxamide derivatives were synthesized to improve the FLT3 inhibitory potency and selectivity. Among them, compound 50 (4-((2-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)amino)-N-(4-(piperazin-1-yl)phenyl)-1H-pyrazole-3-carboxamide) was identified as a highly potent and selective FLT3 inhibitor (IC₅₀ = 0.213 nM), which showed equal activities against various mutants of FLT3 including FLT3 (ITD)-D835V and FLT3 (ITD)-F691L that is resistant to quizartinib. Compound 50 also exhibited efficacy against the human AML cell line MV4-11 (IC₅₀ = 16.1 nM) harboring FLT3-ITD mutants. Inversely, compound 50 displayed no cytotoxicity to FLT3-independent cells, and the biochem. analyses showed that its effects were related to the inhibition of FLT3 signal pathways. Addnl., compound 50 induced apoptosis in MV4-11 cell as demonstrated by flow cytometry. Moreover, compound 50 showed enhanced metabolic stability. Altogether, it was concluded that compound 50 could be a promising FLT3 inhibitor for further developing therapeutic remedy of AML. In the experiment, the researchers used many compounds, for example, 1-Boc-4-(4-Nitrophenyl)piperazine (cas: 182618-86-6Reference of 182618-86-6).

1-Boc-4-(4-Nitrophenyl)piperazine (cas: 182618-86-6) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. 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.Reference of 182618-86-6

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

Discovery of benzo[d]oxazole derivatives as the potent type-I FLT3-ITD inhibitors was written by Bao, Jiyin;Liu, Haichun;Zhi, Yanle;Yang, Wenqianzi;Zhang, Jiawei;Lu, Tao;Wang, Yue;Lu, Shuai. And the article was included in Bioorganic Chemistry in 2020.Safety of 1-Boc-4-(4-Nitrophenyl)piperazine This article mentions the following:

A series of compounds I [R¹ = H, Me, F, MeO; R² = diethylamino, piperidinyl, piperazin-1-yl, etc.; R³ = Ph, pyridin-3-yl, pyridin-4-yl, etc.] were designed and synthesized based on benzo[d]oxazole-2-amine scaffold to discover new potent Fms-like tyrosine kinase 3 inhibitors. During the medicinal chem. works, flexible mol. docking was used to provide design rationale and study the binding modes of the target compounds Through the mixed SAR exploration based on the enzymic and cellular activities, compound I [R¹ = MeO; R² = piperazin-1-yl; R³ = 3-carbamoylphenyl] was identified with potent FLT3-ITD inhibitory (IC₅₀: 0.41 nM) and anti-proliferative (IC₅₀: 0.037娓璏 against MV4-11 cells) activities. And the binding mode of I [R¹ = MeO; R² = piperazin-1-yl; R³ = 3-carbamoylphenyl] with ”DFG-in” FLT3 was simulated by a 20-ns mol. dynamics run, providing some insights into further medicinal chem. efforts toward novel FLT3 inhibitors in AML therapy. In the experiment, the researchers used many compounds, for example, 1-Boc-4-(4-Nitrophenyl)piperazine (cas: 182618-86-6Safety of 1-Boc-4-(4-Nitrophenyl)piperazine).

1-Boc-4-(4-Nitrophenyl)piperazine (cas: 182618-86-6) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. 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.Safety of 1-Boc-4-(4-Nitrophenyl)piperazine

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

Improved synthesis of 4-[4-(5-oxo-1,5-dihydro-[1,2,4 triazoyl-4-yl) phenyl]piperazine-1-carboxylic t-butyl ester was written by Sheng, Chunquan;Zhang, Wannian;Xu, Hui;Che, Xiaoying;Zhang, Min;Yao, Jianzhong;Miao, Zhenyuan. And the article was included in Zhongguo Yaowu Huaxue Zazhi in 2006.Computed Properties of C15H21N3O4 This article mentions the following:

To improve the synthetic process of 4-[4-(5-oxo-1,5-dihydro-[1,2,4] triazoyl-4-yl) phenyl] piperazine-1-carboxylic t-Bu ester, which was used as the key intermediate of triazole antifungal agents, the product was synthesized from 1-(4-nitrophenyl) piperazine by Boc protection, reduction of nitro group, acylation, hydrazinolysis and cyclization. The new synthetic process had several advantages such as facile reaction condition, convenient operation and purification without chromatog. The overall yield was improved from 39.10% to 71.94%. In the experiment, the researchers used many compounds, for example, 1-Boc-4-(4-Nitrophenyl)piperazine (cas: 182618-86-6Computed Properties of C15H21N3O4).

1-Boc-4-(4-Nitrophenyl)piperazine (cas: 182618-86-6) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. 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. Computed Properties of C15H21N3O4

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

Discovery of the selective and efficacious inhibitors of FLT3 mutations was written by Zhi, Yanle;Li, Baoquan;Yao, Chao;Li, Hongmei;Chen, Puzhou;Bao, Jiyin;Qin, Tianren;Wang, Yue;Lu, Tao;Lu, Shuai. And the article was included in European Journal of Medicinal Chemistry in 2018.Reference of 182618-86-6 This article mentions the following:

Fms-like tyrosine kinase 3 (FLT3) is among the most frequently mutated protein in acute myeloid leukemia (AML), which has been confirmed as an important drug target for AML chemotherapy. Starting from the lead compound LT-106-175, a series of 1-H-pyrazole-3-carboxamide derivatives were synthesized to improve the FLT3 inhibitory potency and selectivity. Among them, compound 50 (4-((2-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)amino)-N-(4-(piperazin-1-yl)phenyl)-1H-pyrazole-3-carboxamide) was identified as a highly potent and selective FLT3 inhibitor (IC₅₀ = 0.213 nM), which showed equal activities against various mutants of FLT3 including FLT3 (ITD)-D835V and FLT3 (ITD)-F691L that is resistant to quizartinib. Compound 50 also exhibited efficacy against the human AML cell line MV4-11 (IC₅₀ = 16.1 nM) harboring FLT3-ITD mutants. Inversely, compound 50 displayed no cytotoxicity to FLT3-independent cells, and the biochem. analyses showed that its effects were related to the inhibition of FLT3 signal pathways. Addnl., compound 50 induced apoptosis in MV4-11 cell as demonstrated by flow cytometry. Moreover, compound 50 showed enhanced metabolic stability. Altogether, it was concluded that compound 50 could be a promising FLT3 inhibitor for further developing therapeutic remedy of AML. In the experiment, the researchers used many compounds, for example, 1-Boc-4-(4-Nitrophenyl)piperazine (cas: 182618-86-6Reference of 182618-86-6).

1-Boc-4-(4-Nitrophenyl)piperazine (cas: 182618-86-6) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. 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.Reference of 182618-86-6

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

Discovery of the selective and efficacious inhibitors of FLT3 mutations was written by Zhi, Yanle;Li, Baoquan;Yao, Chao;Li, Hongmei;Chen, Puzhou;Bao, Jiyin;Qin, Tianren;Wang, Yue;Lu, Tao;Lu, Shuai. And the article was included in European Journal of Medicinal Chemistry in 2018.Reference of 182618-86-6 This article mentions the following:

Fms-like tyrosine kinase 3 (FLT3) is among the most frequently mutated protein in acute myeloid leukemia (AML), which has been confirmed as an important drug target for AML chemotherapy. Starting from the lead compound LT-106-175, a series of 1-H-pyrazole-3-carboxamide derivatives were synthesized to improve the FLT3 inhibitory potency and selectivity. Among them, compound 50 (4-((2-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)amino)-N-(4-(piperazin-1-yl)phenyl)-1H-pyrazole-3-carboxamide) was identified as a highly potent and selective FLT3 inhibitor (IC₅₀ = 0.213 nM), which showed equal activities against various mutants of FLT3 including FLT3 (ITD)-D835V and FLT3 (ITD)-F691L that is resistant to quizartinib. Compound 50 also exhibited efficacy against the human AML cell line MV4-11 (IC₅₀ = 16.1 nM) harboring FLT3-ITD mutants. Inversely, compound 50 displayed no cytotoxicity to FLT3-independent cells, and the biochem. analyses showed that its effects were related to the inhibition of FLT3 signal pathways. Addnl., compound 50 induced apoptosis in MV4-11 cell as demonstrated by flow cytometry. Moreover, compound 50 showed enhanced metabolic stability. Altogether, it was concluded that compound 50 could be a promising FLT3 inhibitor for further developing therapeutic remedy of AML. In the experiment, the researchers used many compounds, for example, 1-Boc-4-(4-Nitrophenyl)piperazine (cas: 182618-86-6Reference of 182618-86-6).

1-Boc-4-(4-Nitrophenyl)piperazine (cas: 182618-86-6) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. 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.Reference of 182618-86-6

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

Design, synthesis and antitubercular evaluation of novel series of N-[4-(piperazin-1-yl)phenyl]cinnamamide derivatives was written by Patel, Kavitkumar N.;Telvekar, Vikas N.. And the article was included in European Journal of Medicinal Chemistry in 2014.Application of 182618-86-6 This article mentions the following:

The analogs of N-[4-(piperazin-1-yl)phenyl]cinnamamide were designed and synthesized by a mol. hybridization approach in which part C of the designed mol. was linked through amide and carbamate functionality that improves the physicochem. properties and govern the pharmacokinetic and pharmacodynamic behavior. The systematic modification was done around the Part C to explore the structure activity relationship of antitubercular cinnamamides. All 52 compounds were evaluated for antitubercular activity against Mycobacterium tuberculosis (M. tb) using Resazurin microtitre plate assay (REMA). Compound I with trifluoromethyl substitution exhibited good antitubercular activity of 3.125 μg/mL. The synthesized N-[4-(piperazin-1-yl)phenyl]cinnamamide derivatives showed promising activity against M. tb. In the experiment, the researchers used many compounds, for example, 1-Boc-4-(4-Nitrophenyl)piperazine (cas: 182618-86-6Application of 182618-86-6).

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. 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. Application of 182618-86-6

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