Tag: 311.3616

Gao, Longfei et al. published their research in Scientific Reports in 2019 | CAS: 1226056-71-8

N-Benzyl-2-(pyrimidin-4-ylamino)thiazole-4-carboxamide (cas: 1226056-71-8) belongs to thiazole derivatives. Thiazoles frequently appear in peptide studies. Thiazoles can also be used as protected formyl groups, which can be released in later stages of complex natural product synthesis. There are numerous natural products that possess a thiazole ring with broad pharmacological activities. Thiamine, also known as vitamin B1, possesses a thiazole ring linked with 2-methylpyrimidine-4-amine as hydrochloride salt.Category: thiazole

Suppression of glioblastoma by a drug cocktail reprogramming tumor cells into neuronal like cells was written by Gao, Longfei;Huang, Shichao;Zhang, Hong;Hua, Wei;Xin, Shunmei;Cheng, Lin;Guan, Wuqiang;Yu, Yongchun;Mao, Ying;Pei, Gang. And the article was included in Scientific Reports in 2019.Category: thiazole This article mentions the following:

Glioblastoma (GBM) is the most common and aggressive malignant tumor in adult brain. Even with the current standard therapy including surgical resection followed by postoperative radiotherapy and chemotherapy with temozolomide (Temo), GBM patients still have a poor median survival. Reprogramming of tumor cells into non-malignant cells might be a promising therapeutic strategy for malignant tumors, including GBM. Based on previous studies using small mols. to reprogram astrocytes into neuronal cells, here we further identified a FTT cocktail of three commonly used drugs (Fasudil, Tranilast, and Temo) to reprogram patient-derived GBM cells, either cultured in serum containing or serum-free medium, into neuronal like cells. FTT-treated GBM cells displayed a neuronal like morphol., expressed neuronal genes, exhibited neuronal electrophysiol. properties, and showed attenuated malignancy. More importantly, FTT cocktail more significantly suppressed tumor growth and prolonged survival in GBM patient derived xenograft than Temo alone. Our study provided preclin. evidence that the neuronal reprogramming drug cocktail might be a promising strategy to improve the existing treatment for GBM. In the experiment, the researchers used many compounds, for example, N-Benzyl-2-(pyrimidin-4-ylamino)thiazole-4-carboxamide (cas: 1226056-71-8Category: thiazole).

N-Benzyl-2-(pyrimidin-4-ylamino)thiazole-4-carboxamide (cas: 1226056-71-8) belongs to thiazole derivatives. Thiazoles frequently appear in peptide studies. Thiazoles can also be used as protected formyl groups, which can be released in later stages of complex natural product synthesis. There are numerous natural products that possess a thiazole ring with broad pharmacological activities. Thiamine, also known as vitamin B1, possesses a thiazole ring linked with 2-methylpyrimidine-4-amine as hydrochloride salt.Category: thiazole

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Gao, Longfei et al. published their research in Scientific Reports in 2019 | CAS: 1226056-71-8

N-Benzyl-2-(pyrimidin-4-ylamino)thiazole-4-carboxamide (cas: 1226056-71-8) belongs to thiazole derivatives. Thiazoles frequently appear in peptide studies. Thiazoles can also be used as protected formyl groups, which can be released in later stages of complex natural product synthesis. There are numerous natural products that possess a thiazole ring with broad pharmacological activities. Thiamine, also known as vitamin B1, possesses a thiazole ring linked with 2-methylpyrimidine-4-amine as hydrochloride salt.Category: thiazole

Suppression of glioblastoma by a drug cocktail reprogramming tumor cells into neuronal like cells was written by Gao, Longfei;Huang, Shichao;Zhang, Hong;Hua, Wei;Xin, Shunmei;Cheng, Lin;Guan, Wuqiang;Yu, Yongchun;Mao, Ying;Pei, Gang. And the article was included in Scientific Reports in 2019.Category: thiazole This article mentions the following:

Glioblastoma (GBM) is the most common and aggressive malignant tumor in adult brain. Even with the current standard therapy including surgical resection followed by postoperative radiotherapy and chemotherapy with temozolomide (Temo), GBM patients still have a poor median survival. Reprogramming of tumor cells into non-malignant cells might be a promising therapeutic strategy for malignant tumors, including GBM. Based on previous studies using small mols. to reprogram astrocytes into neuronal cells, here we further identified a FTT cocktail of three commonly used drugs (Fasudil, Tranilast, and Temo) to reprogram patient-derived GBM cells, either cultured in serum containing or serum-free medium, into neuronal like cells. FTT-treated GBM cells displayed a neuronal like morphol., expressed neuronal genes, exhibited neuronal electrophysiol. properties, and showed attenuated malignancy. More importantly, FTT cocktail more significantly suppressed tumor growth and prolonged survival in GBM patient derived xenograft than Temo alone. Our study provided preclin. evidence that the neuronal reprogramming drug cocktail might be a promising strategy to improve the existing treatment for GBM. In the experiment, the researchers used many compounds, for example, N-Benzyl-2-(pyrimidin-4-ylamino)thiazole-4-carboxamide (cas: 1226056-71-8Category: thiazole).

N-Benzyl-2-(pyrimidin-4-ylamino)thiazole-4-carboxamide (cas: 1226056-71-8) belongs to thiazole derivatives. Thiazoles frequently appear in peptide studies. Thiazoles can also be used as protected formyl groups, which can be released in later stages of complex natural product synthesis. There are numerous natural products that possess a thiazole ring with broad pharmacological activities. Thiamine, also known as vitamin B1, possesses a thiazole ring linked with 2-methylpyrimidine-4-amine as hydrochloride salt.Category: thiazole

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Lee, Ha Won et al. published their research in Journal of the American Society of Nephrology in 2015 | CAS: 1226056-71-8

N-Benzyl-2-(pyrimidin-4-ylamino)thiazole-4-carboxamide (cas: 1226056-71-8) belongs to thiazole derivatives. Thiazole rings are planar and aromatic. Thiazoles are characterized by larger pi-electron delocalization than the corresponding oxazoles and have therefore greater aromaticity. Thiazole is a versatile building block for the construction and lead generation of new drug discoveries. Numerous diazole-based compounds are in clinical use as anticancer, antileukemic, antiinflammatory, antiviral, antifungal, antirheumatic, immunomodulator, and antiparasitic agents.Reference of 1226056-71-8

A podocyte-based automated screening assay identifies protective small molecules was written by Lee, Ha Won;Khan, Samia Q.;Faridi, Mohd. Hafeez;Wei, Changli;Tardi, Nicholas J.;Altintas, Mehmet M.;Elshabrawy, Hatem A.;Mangos, Steve;Quick, Kevin L.;Sever, Sanja;Reiser, Jochen;Gupta, Vineet. And the article was included in Journal of the American Society of Nephrology in 2015.Reference of 1226056-71-8 This article mentions the following:

Podocyte injury and loss mark an early step in the pathogenesis of various glomerular diseases, making these cells excellent targets for therapeutics. However, cell-based high-throughput screening assays for the rational development of podocyte-directed therapeutics are currently lacking. Here, we describe a novel high-content screening-based phenotypic assay that analyzes thousands of podocytes per assay condition in 96-well plates to quant. measure dose-dependent changes in multiple cellular features. Our assay consistently produced a Z’ value >0.44, making it suitable for compound screening. On screening with >2100 pharmacol. active agents, we identified 24 small mols. that protected podocytes against injury in vitro (1% hit rate). Among the identified hits, we confirmed an 尾1-integrin agonist, pyrintegrin, as a podocyte-protective agent. Treatment with pyrintegrin prevented damage-induced decreases in F-actin stress fibers, focal adhesions, and active 尾1-integrin levels in cultured cells. In vivo, administration of pyrintegrin protected mice from LPS-induced podocyte foot process effacement and proteinuria. Anal. of the murine glomeruli showed that LPS administration reduced the levels of active 尾1 integrin in the podocytes, which was prevented by cotreatment with pyrintegrin. In rats, pyrintegrin reduced peak proteinuria caused by puromycin aminonucleoside-induced nephropathy. Our findings identify pyrintegrin as a potential therapeutic candidate and show the use of podocyte-based screening assays for identifying novel therapeutics for proteinuric kidney diseases. In the experiment, the researchers used many compounds, for example, N-Benzyl-2-(pyrimidin-4-ylamino)thiazole-4-carboxamide (cas: 1226056-71-8Reference of 1226056-71-8).

N-Benzyl-2-(pyrimidin-4-ylamino)thiazole-4-carboxamide (cas: 1226056-71-8) belongs to thiazole derivatives. Thiazole rings are planar and aromatic. Thiazoles are characterized by larger pi-electron delocalization than the corresponding oxazoles and have therefore greater aromaticity. Thiazole is a versatile building block for the construction and lead generation of new drug discoveries. Numerous diazole-based compounds are in clinical use as anticancer, antileukemic, antiinflammatory, antiviral, antifungal, antirheumatic, immunomodulator, and antiparasitic agents.Reference of 1226056-71-8

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Lee, Ha Won et al. published their research in Journal of the American Society of Nephrology in 2015 | CAS: 1226056-71-8

N-Benzyl-2-(pyrimidin-4-ylamino)thiazole-4-carboxamide (cas: 1226056-71-8) belongs to thiazole derivatives. Thiazole rings are planar and aromatic. Thiazoles are characterized by larger pi-electron delocalization than the corresponding oxazoles and have therefore greater aromaticity. Thiazole is a versatile building block for the construction and lead generation of new drug discoveries. Numerous diazole-based compounds are in clinical use as anticancer, antileukemic, antiinflammatory, antiviral, antifungal, antirheumatic, immunomodulator, and antiparasitic agents.Reference of 1226056-71-8

A podocyte-based automated screening assay identifies protective small molecules was written by Lee, Ha Won;Khan, Samia Q.;Faridi, Mohd. Hafeez;Wei, Changli;Tardi, Nicholas J.;Altintas, Mehmet M.;Elshabrawy, Hatem A.;Mangos, Steve;Quick, Kevin L.;Sever, Sanja;Reiser, Jochen;Gupta, Vineet. And the article was included in Journal of the American Society of Nephrology in 2015.Reference of 1226056-71-8 This article mentions the following:

Podocyte injury and loss mark an early step in the pathogenesis of various glomerular diseases, making these cells excellent targets for therapeutics. However, cell-based high-throughput screening assays for the rational development of podocyte-directed therapeutics are currently lacking. Here, we describe a novel high-content screening-based phenotypic assay that analyzes thousands of podocytes per assay condition in 96-well plates to quant. measure dose-dependent changes in multiple cellular features. Our assay consistently produced a Z’ value >0.44, making it suitable for compound screening. On screening with >2100 pharmacol. active agents, we identified 24 small mols. that protected podocytes against injury in vitro (1% hit rate). Among the identified hits, we confirmed an β1-integrin agonist, pyrintegrin, as a podocyte-protective agent. Treatment with pyrintegrin prevented damage-induced decreases in F-actin stress fibers, focal adhesions, and active β1-integrin levels in cultured cells. In vivo, administration of pyrintegrin protected mice from LPS-induced podocyte foot process effacement and proteinuria. Anal. of the murine glomeruli showed that LPS administration reduced the levels of active β1 integrin in the podocytes, which was prevented by cotreatment with pyrintegrin. In rats, pyrintegrin reduced peak proteinuria caused by puromycin aminonucleoside-induced nephropathy. Our findings identify pyrintegrin as a potential therapeutic candidate and show the use of podocyte-based screening assays for identifying novel therapeutics for proteinuric kidney diseases. In the experiment, the researchers used many compounds, for example, N-Benzyl-2-(pyrimidin-4-ylamino)thiazole-4-carboxamide (cas: 1226056-71-8Reference of 1226056-71-8).

N-Benzyl-2-(pyrimidin-4-ylamino)thiazole-4-carboxamide (cas: 1226056-71-8) belongs to thiazole derivatives. Thiazole rings are planar and aromatic. Thiazoles are characterized by larger pi-electron delocalization than the corresponding oxazoles and have therefore greater aromaticity. Thiazole is a versatile building block for the construction and lead generation of new drug discoveries. Numerous diazole-based compounds are in clinical use as anticancer, antileukemic, antiinflammatory, antiviral, antifungal, antirheumatic, immunomodulator, and antiparasitic agents.Reference of 1226056-71-8

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica