Tag: 291.3886

Discovery of a novel series of imidazo[1′,2′:1,6]pyrido[2,3-d]pyrimidin derivatives as potent cyclin-dependent kinase 4/6 inhibitors was written by Shi, Chen;Wang, Qian;Liao, Xuemei;Ge, Hui;Huo, Guoyong;Zhang, Leduo;Chen, Na;Zhai, Xiong;Hong, Yuan;Wang, Li;Wang, Zhe;Shi, Weijun;Mao, Yu;Yu, Jianxin;Ke, Ying;Xia, Guangxin. And the article was included in European Journal of Medicinal Chemistry in 2020.Quality Control of tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate This article mentions the following:

CDK4/6 has been identified as an attractive therapeutic target for treatment of cancer. For unmet clin. needs, a novel class of imidazo [1′,2′:1,6]pyrido [2,3-d]pyrimidin derivatives, which had distinctive triheteroaryl structure, had been discovered as CDK4/6 inhibitors. The compounds 10b (I) and 10c (II), displayed the low nanomolar range activities on CDK4/6, desirable antiproliferative activities, excellent metabolic properties, and acceptable pharmacokinetic characters. In Colo-205 and U87MG xenograft models, compounds 10b and 10c also showed significant tumor growth inhibitions with controllable toxicities. All data confirmed that imidazo [1′,2′:1,6]pyrido [2,3-d]pyrimidin derivatives 10b and 10c could be promising drug candidates for cancer therapy. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate (cas: 304897-49-2Quality Control of tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate).

tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate (cas: 304897-49-2) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. 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.Quality Control of tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate

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

Identification of novel potent HIV-1 inhibitors by exploiting the tolerant regions of the NNRTIs binding pocket was written by Sun, Yanying;Kang, Dongwei;Da, Feng;Zhang, Tao;Li, Pei;Zhang, Baodan;De Clercq, Erik;Pannecouque, Christophe;Zhan, Peng;Liu, Xinyong. And the article was included in European Journal of Medicinal Chemistry in 2021.Application In Synthesis of tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate This article mentions the following:

With our previously identified potent NNRTIs 25a and HBS-11c as leads, series of novel thiophene[3,2-d]pyrimidine and thiophene[2,3-d]pyrimidine derivatives were designed via mol. hybridization strategy. All the target compounds were evaluated for their anti-HIV-1 activity and cytotoxicity in MT-4 cells. Compounds 16a1 and 16b1 turned out to be the most potent inhibitors against WT and mutant HIV-1 strains (L100I, K103N, and E138K), with EC50 values ranging from 0.007渭M to 0.043渭M. Gratifyingly, 16b1 exhibited significantly reduced cytotoxicity (CC50 > 217.5渭M) and improved water solubility (S = 49.3渭g/mL at pH 7.0) compared to the lead 25a (S < 1渭g/mL at pH 7.0, CC50 = 2.30渭M). Moreover, mol. docking was also conducted to rationalize the structure-activity relationships of these novel derivatives and to understand their key interactions with the binding pocket. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate (cas: 304897-49-2Application In Synthesis of tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate).

tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate (cas: 304897-49-2) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. 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 In Synthesis of tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate

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

A novel series of 2-carboxytetrahydroquinolines provides new insights into the eastern region of glycine site NMDA antagonists was written by Dannhardt, Gerd;v. Gruchalla, Markus;Kohl, Beate K.;Parsons, C. G.. And the article was included in Archiv der Pharmazie (Weinheim, Germany) in 2000.Computed Properties of C16H25N3O2 This article mentions the following:

A series of potent 4-substituted tetrahydroquinolines has been synthesized and biol. tested in order to refine the eastern region of the pharmacophore model for glycine site NMDA antagonists concerning the assessment of lipophilicity, flexibility, and hydrogen bonding. Displacement studies on rat cortical membranes using [³H]-5,7-dichlorokynurenic acid as a radioligand indicated that binding affinities are markedly enhanced when addnl. hydrogen-accepting groups are introduced into the eastern region of the 2-carboxytetrahydroquinolines. Among the most potent ligands were some urea, sulfonylurea, and crown ether compounds as interesting leads for new diagnostics, especially for the evaluation of PET tracers, which allow biodistribution studies and NMDA receptor studies in the living organism. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate (cas: 304897-49-2Computed Properties of C16H25N3O2).

tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate (cas: 304897-49-2) 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. 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.Computed Properties of C16H25N3O2

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

Identification of novel potent HIV-1 inhibitors by exploiting the tolerant regions of the NNRTIs binding pocket was written by Sun, Yanying;Kang, Dongwei;Da, Feng;Zhang, Tao;Li, Pei;Zhang, Baodan;De Clercq, Erik;Pannecouque, Christophe;Zhan, Peng;Liu, Xinyong. And the article was included in European Journal of Medicinal Chemistry in 2021.Application In Synthesis of tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate This article mentions the following:

With our previously identified potent NNRTIs 25a and HBS-11c as leads, series of novel thiophene[3,2-d]pyrimidine and thiophene[2,3-d]pyrimidine derivatives were designed via mol. hybridization strategy. All the target compounds were evaluated for their anti-HIV-1 activity and cytotoxicity in MT-4 cells. Compounds 16a1 and 16b1 turned out to be the most potent inhibitors against WT and mutant HIV-1 strains (L100I, K103N, and E138K), with EC50 values ranging from 0.007μM to 0.043μM. Gratifyingly, 16b1 exhibited significantly reduced cytotoxicity (CC50 > 217.5μM) and improved water solubility (S = 49.3μg/mL at pH 7.0) compared to the lead 25a (S < 1μg/mL at pH 7.0, CC50 = 2.30μM). Moreover, mol. docking was also conducted to rationalize the structure-activity relationships of these novel derivatives and to understand their key interactions with the binding pocket. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate (cas: 304897-49-2Application In Synthesis of tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate).

tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate (cas: 304897-49-2) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. 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 In Synthesis of tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate

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

A novel series of 2-carboxytetrahydroquinolines provides new insights into the eastern region of glycine site NMDA antagonists was written by Dannhardt, Gerd;v. Gruchalla, Markus;Kohl, Beate K.;Parsons, C. G.. And the article was included in Archiv der Pharmazie (Weinheim, Germany) in 2000.Computed Properties of C16H25N3O2 This article mentions the following:

A series of potent 4-substituted tetrahydroquinolines has been synthesized and biol. tested in order to refine the eastern region of the pharmacophore model for glycine site NMDA antagonists concerning the assessment of lipophilicity, flexibility, and hydrogen bonding. Displacement studies on rat cortical membranes using [³H]-5,7-dichlorokynurenic acid as a radioligand indicated that binding affinities are markedly enhanced when addnl. hydrogen-accepting groups are introduced into the eastern region of the 2-carboxytetrahydroquinolines. Among the most potent ligands were some urea, sulfonylurea, and crown ether compounds as interesting leads for new diagnostics, especially for the evaluation of PET tracers, which allow biodistribution studies and NMDA receptor studies in the living organism. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate (cas: 304897-49-2Computed Properties of C16H25N3O2).

tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate (cas: 304897-49-2) 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. 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.Computed Properties of C16H25N3O2

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

Discovery of a novel series of imidazo[1′,2′:1,6]pyrido[2,3-d]pyrimidin derivatives as potent cyclin-dependent kinase 4/6 inhibitors was written by Shi, Chen;Wang, Qian;Liao, Xuemei;Ge, Hui;Huo, Guoyong;Zhang, Leduo;Chen, Na;Zhai, Xiong;Hong, Yuan;Wang, Li;Wang, Zhe;Shi, Weijun;Mao, Yu;Yu, Jianxin;Ke, Ying;Xia, Guangxin. And the article was included in European Journal of Medicinal Chemistry in 2020.Quality Control of tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate This article mentions the following:

CDK4/6 has been identified as an attractive therapeutic target for treatment of cancer. For unmet clin. needs, a novel class of imidazo [1′,2′:1,6]pyrido [2,3-d]pyrimidin derivatives, which had distinctive triheteroaryl structure, had been discovered as CDK4/6 inhibitors. The compounds 10b (I) and 10c (II), displayed the low nanomolar range activities on CDK4/6, desirable antiproliferative activities, excellent metabolic properties, and acceptable pharmacokinetic characters. In Colo-205 and U87MG xenograft models, compounds 10b and 10c also showed significant tumor growth inhibitions with controllable toxicities. All data confirmed that imidazo [1′,2′:1,6]pyrido [2,3-d]pyrimidin derivatives 10b and 10c could be promising drug candidates for cancer therapy. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate (cas: 304897-49-2Quality Control of tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate).

tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate (cas: 304897-49-2) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. 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.Quality Control of tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate

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

Identification of novel potent HIV-1 inhibitors by exploiting the tolerant regions of the NNRTIs binding pocket was written by Sun, Yanying;Kang, Dongwei;Da, Feng;Zhang, Tao;Li, Pei;Zhang, Baodan;De Clercq, Erik;Pannecouque, Christophe;Zhan, Peng;Liu, Xinyong. And the article was included in European Journal of Medicinal Chemistry in 2021.Application In Synthesis of tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate This article mentions the following:

With our previously identified potent NNRTIs 25a and HBS-11c as leads, series of novel thiophene[3,2-d]pyrimidine and thiophene[2,3-d]pyrimidine derivatives were designed via mol. hybridization strategy. All the target compounds were evaluated for their anti-HIV-1 activity and cytotoxicity in MT-4 cells. Compounds 16a1 and 16b1 turned out to be the most potent inhibitors against WT and mutant HIV-1 strains (L100I, K103N, and E138K), with EC50 values ranging from 0.007μM to 0.043μM. Gratifyingly, 16b1 exhibited significantly reduced cytotoxicity (CC50 > 217.5μM) and improved water solubility (S = 49.3μg/mL at pH 7.0) compared to the lead 25a (S < 1μg/mL at pH 7.0, CC50 = 2.30μM). Moreover, mol. docking was also conducted to rationalize the structure-activity relationships of these novel derivatives and to understand their key interactions with the binding pocket. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate (cas: 304897-49-2Application In Synthesis of tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate).

tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate (cas: 304897-49-2) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. 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 In Synthesis of tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate

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

A novel series of 2-carboxytetrahydroquinolines provides new insights into the eastern region of glycine site NMDA antagonists was written by Dannhardt, Gerd;v. Gruchalla, Markus;Kohl, Beate K.;Parsons, C. G.. And the article was included in Archiv der Pharmazie (Weinheim, Germany) in 2000.Computed Properties of C16H25N3O2 This article mentions the following:

A series of potent 4-substituted tetrahydroquinolines has been synthesized and biol. tested in order to refine the eastern region of the pharmacophore model for glycine site NMDA antagonists concerning the assessment of lipophilicity, flexibility, and hydrogen bonding. Displacement studies on rat cortical membranes using [³H]-5,7-dichlorokynurenic acid as a radioligand indicated that binding affinities are markedly enhanced when addnl. hydrogen-accepting groups are introduced into the eastern region of the 2-carboxytetrahydroquinolines. Among the most potent ligands were some urea, sulfonylurea, and crown ether compounds as interesting leads for new diagnostics, especially for the evaluation of PET tracers, which allow biodistribution studies and NMDA receptor studies in the living organism. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate (cas: 304897-49-2Computed Properties of C16H25N3O2).

tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate (cas: 304897-49-2) 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. 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.Computed Properties of C16H25N3O2

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