Tag: 200.278

Nagao, Satoshi et al. published their research in Bioorganic & Medicinal Chemistry in 2014 | CAS: 147081-29-6

(S)-tert-Butyl 3-methylpiperazine-1-carboxylate (cas: 147081-29-6) 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: 147081-29-6

Synthesis and structure-activity relationships of novel, potent, orally active hypoxia-inducible factor-1 inhibitors was written by Nagao, Satoshi;Yamane, Yoshinobu;Funasaka, Setsuo;Tanaka, Keigo;Miyazaki, Kazuki;Kotake, Yoshihiko;Kamata, Jun-ichi;Watanabe-Miyano, Saori;Toyama, Osamu;Ozawa, Yoichi;Mizui, Yoshiharu;Okamoto, Kiyoshi;Ito, Daisuke. And the article was included in Bioorganic & Medicinal Chemistry in 2014.SDS of cas: 147081-29-6 This article mentions the following:

Hypoxia-inducible factor-1 (HIF-1) is the chief transcription factor regulating hypoxia-driven gene expression. HIF-1 overexpression is associated with poor prognosis in several cancers and therefore represents an attractive target for novel antitumor agents. The authors explored small mol. inhibitors of the HIF-1 pathway. Using high-throughput-screening, the authors identified a benzanilide compound (IC50 = 560 nM) as a seed. Subsequent extensive derivatization led to the discovery of compounds I and II d, with anti-HIF-1 activities in vitro (IC50 = 21 and 0.47 nM, resp.), and in vivo. Addnl., I (12.5-100 mg/kg) also displayed in vivo antitumor efficacy, without influencing body weight In the experiment, the researchers used many compounds, for example, (S)-tert-Butyl 3-methylpiperazine-1-carboxylate (cas: 147081-29-6SDS of cas: 147081-29-6).

(S)-tert-Butyl 3-methylpiperazine-1-carboxylate (cas: 147081-29-6) 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: 147081-29-6

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

 

Tagat, Jayaram R. et al. published their research in Journal of Medicinal Chemistry in 2004 | CAS: 147081-29-6

(S)-tert-Butyl 3-methylpiperazine-1-carboxylate (cas: 147081-29-6) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 °C and boils at 125–130 °C. 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.Application of 147081-29-6

Piperazine-Based CCR5 Antagonists as HIV-1 Inhibitors. IV. Discovery of 1-[(4,6-Dimethyl-5-pyrimidinyl)carbonyl]- 4-[4-{2-methoxy-1(R)-4-(trifluoromethyl)phenyl}ethyl-3(S)-methyl-1-piperazinyl]- 4-methylpiperidine (Sch-417690/Sch-D), a Potent, Highly Selective, and Orally Bioavailable CCR5 Antagonist was written by Tagat, Jayaram R.;McCombie, Stuart W.;Nazareno, Dennis;Labroli, Marc A.;Xiao, Yushi;Steensma, Ruo W.;Strizki, Julie M.;Baroudy, Bahige M.;Cox, Kathleen;Lachowicz, Jean;Varty, Geoffrey;Watkins, Robert. And the article was included in Journal of Medicinal Chemistry in 2004.Application of 147081-29-6 This article mentions the following:

The nature and the size of the benzylic substituent are shown to be the key to controlling receptor selectivity (CCR5 vs. M1, M2) and potency in the title compounds Optimization of the lead benzylic Me compound 3 led to the methoxymethyl analog 30, which had excellent receptor selectivity and oral bioavailability in rats and monkeys. Compound 30 (Sch-417690/Sch-D), a potent inhibitor of HIV-1 entry into target cells, is currently in clin. trials. In the experiment, the researchers used many compounds, for example, (S)-tert-Butyl 3-methylpiperazine-1-carboxylate (cas: 147081-29-6Application of 147081-29-6).

(S)-tert-Butyl 3-methylpiperazine-1-carboxylate (cas: 147081-29-6) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 °C and boils at 125–130 °C. 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.Application of 147081-29-6

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

 

Zhao, Hong-Yi et al. published their research in Journal of Medicinal Chemistry in 2022 | CAS: 216854-23-8

(S)-tert-Butyl piperidin-3-ylcarbamate (cas: 216854-23-8) 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. Piperidine derivatives are being utilized in different ways as anticancer, antiviral, antimalarial, antimicrobial, antifungal, antihypertension, analgesic, anti-inflammatory, anti-Alzheimer, antipsychotic and/or anticoagulant agents.Related Products of 216854-23-8

Discovery of Potent PROTACs Targeting EGFR Mutants through the Optimization of Covalent EGFR Ligands was written by Zhao, Hong-Yi;Wang, Hai-Peng;Mao, Yu-Ze;Zhang, Hao;Xin, Minhang;Xi, Xiao-Xiao;Lei, Hao;Mao, Shuai;Li, Dong-Hui;Zhang, San-Qi. And the article was included in Journal of Medicinal Chemistry in 2022.Related Products of 216854-23-8 This article mentions the following:

To overcome the intractable problem of drug resistance, proteolysis targeting chimeras (PROTACs) targeting EGFR mutants were developed by optimizing covalent EGFR ligands. Covalent or reversible covalent pyrimidine- or purine-containing PROTACs were designed, synthesized, and evaluated. As a consequence, covalent PROTAC I, with a novel purine-containing EGFR ligand, was discovered as a highly potent degrader against EGFRL858R/T790M and EGFRdel19, reaching the lowest DC50 values among all reported EGFR-targeting PROTACs. Furthermore, I exhibited excellent cellular activity against the H1975 and HCC827 cell lines with high selectivity. Mechanism investigation indicated that the lysosome was involved in the degradation process. Importantly, the covalent binding strategy was proven to be an effective approach for the design of PROTACs targeting EGFRL858R/T790M, which laid the practical foundation for further development of potent EGFR-targeting PROTACs. In the experiment, the researchers used many compounds, for example, (S)-tert-Butyl piperidin-3-ylcarbamate (cas: 216854-23-8Related Products of 216854-23-8).

(S)-tert-Butyl piperidin-3-ylcarbamate (cas: 216854-23-8) 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. Piperidine derivatives are being utilized in different ways as anticancer, antiviral, antimalarial, antimicrobial, antifungal, antihypertension, analgesic, anti-inflammatory, anti-Alzheimer, antipsychotic and/or anticoagulant agents.Related Products of 216854-23-8

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Zhao, Hong-Yi et al. published their research in Journal of Medicinal Chemistry in 2022 | CAS: 216854-23-8

(S)-tert-Butyl piperidin-3-ylcarbamate (cas: 216854-23-8) 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. Piperidine derivatives are being utilized in different ways as anticancer, antiviral, antimalarial, antimicrobial, antifungal, antihypertension, analgesic, anti-inflammatory, anti-Alzheimer, antipsychotic and/or anticoagulant agents.Related Products of 216854-23-8

Discovery of Potent PROTACs Targeting EGFR Mutants through the Optimization of Covalent EGFR Ligands was written by Zhao, Hong-Yi;Wang, Hai-Peng;Mao, Yu-Ze;Zhang, Hao;Xin, Minhang;Xi, Xiao-Xiao;Lei, Hao;Mao, Shuai;Li, Dong-Hui;Zhang, San-Qi. And the article was included in Journal of Medicinal Chemistry in 2022.Related Products of 216854-23-8 This article mentions the following:

To overcome the intractable problem of drug resistance, proteolysis targeting chimeras (PROTACs) targeting EGFR mutants were developed by optimizing covalent EGFR ligands. Covalent or reversible covalent pyrimidine- or purine-containing PROTACs were designed, synthesized, and evaluated. As a consequence, covalent PROTAC I, with a novel purine-containing EGFR ligand, was discovered as a highly potent degrader against EGFRL858R/T790M and EGFRdel19, reaching the lowest DC50 values among all reported EGFR-targeting PROTACs. Furthermore, I exhibited excellent cellular activity against the H1975 and HCC827 cell lines with high selectivity. Mechanism investigation indicated that the lysosome was involved in the degradation process. Importantly, the covalent binding strategy was proven to be an effective approach for the design of PROTACs targeting EGFRL858R/T790M, which laid the practical foundation for further development of potent EGFR-targeting PROTACs. In the experiment, the researchers used many compounds, for example, (S)-tert-Butyl piperidin-3-ylcarbamate (cas: 216854-23-8Related Products of 216854-23-8).

(S)-tert-Butyl piperidin-3-ylcarbamate (cas: 216854-23-8) 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. Piperidine derivatives are being utilized in different ways as anticancer, antiviral, antimalarial, antimicrobial, antifungal, antihypertension, analgesic, anti-inflammatory, anti-Alzheimer, antipsychotic and/or anticoagulant agents.Related Products of 216854-23-8

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Zhao, Hong-Yi et al. published their research in Journal of Medicinal Chemistry in 2022 | CAS: 216854-23-8

(S)-tert-Butyl piperidin-3-ylcarbamate (cas: 216854-23-8) 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. Piperidine derivatives are being utilized in different ways as anticancer, antiviral, antimalarial, antimicrobial, antifungal, antihypertension, analgesic, anti-inflammatory, anti-Alzheimer, antipsychotic and/or anticoagulant agents.Related Products of 216854-23-8

Discovery of Potent PROTACs Targeting EGFR Mutants through the Optimization of Covalent EGFR Ligands was written by Zhao, Hong-Yi;Wang, Hai-Peng;Mao, Yu-Ze;Zhang, Hao;Xin, Minhang;Xi, Xiao-Xiao;Lei, Hao;Mao, Shuai;Li, Dong-Hui;Zhang, San-Qi. And the article was included in Journal of Medicinal Chemistry in 2022.Related Products of 216854-23-8 This article mentions the following:

To overcome the intractable problem of drug resistance, proteolysis targeting chimeras (PROTACs) targeting EGFR mutants were developed by optimizing covalent EGFR ligands. Covalent or reversible covalent pyrimidine- or purine-containing PROTACs were designed, synthesized, and evaluated. As a consequence, covalent PROTAC I, with a novel purine-containing EGFR ligand, was discovered as a highly potent degrader against EGFRL858R/T790M and EGFRdel19, reaching the lowest DC50 values among all reported EGFR-targeting PROTACs. Furthermore, I exhibited excellent cellular activity against the H1975 and HCC827 cell lines with high selectivity. Mechanism investigation indicated that the lysosome was involved in the degradation process. Importantly, the covalent binding strategy was proven to be an effective approach for the design of PROTACs targeting EGFRL858R/T790M, which laid the practical foundation for further development of potent EGFR-targeting PROTACs. In the experiment, the researchers used many compounds, for example, (S)-tert-Butyl piperidin-3-ylcarbamate (cas: 216854-23-8Related Products of 216854-23-8).

(S)-tert-Butyl piperidin-3-ylcarbamate (cas: 216854-23-8) 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. Piperidine derivatives are being utilized in different ways as anticancer, antiviral, antimalarial, antimicrobial, antifungal, antihypertension, analgesic, anti-inflammatory, anti-Alzheimer, antipsychotic and/or anticoagulant agents.Related Products of 216854-23-8

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem