Category: 144060-98-0

Zhang, Qian; Liu, Xiaobo; Gan, Wenhui; Wu, Jinjin; Zhou, Hualan; Yang, Zunhua; Zhang, Yiling; Liao, Min; Yuan, Ping; Xu, Shan; Zheng, Pengwu; Zhu, Wufu published an article in ACS Omega. The title of the article was 《Discovery of Triazolo-pyridazine/-pyrimidine Derivatives Bearing Aromatic (Heterocycle)-Coupled Azole Units as Class II c-Met Inhibitors》.Application of 144060-98-0 The author mentioned the following in the article:

Two series of novel triazolo-pyridazine/-pyrimidine derivatives were designed, synthesized, and evaluated for their inhibitory activity against c-Met kinase, as well as three c-Met overexpressed cancer cell lines (A549, MCF-7, and HeLa) and one normal human hepatocytes cell line LO2 in vitro. The most promising compound I exhibited significant cytotoxicity against A549, MCF-7, and HeLa cell lines with IC50 values of 1.06 +/- 0.16, 1.23 +/- 0.18, and 2.73 +/- 0.33μM, resp. Moreover, the inhibitory activity of compound I against c-Met kinase (IC50 = 0.090μM) was equal to that of Foretinib (IC50 = 0.019μM). The result of the acridine orange single staining test demonstrated that compound I could remarkably induce apoptosis of A549 cells. The results of apoptosis and cycle distribution of cells showed that compound I could induce late apoptosis of A549 cells and stimulate A549 cells arresting in the G0/G1 phase. Structure-activity relationships (SARs), pharmacol. results, and docking studies indicated that the introduction of 5-methylthiazole fragment to the five-atom moiety was beneficial for the activity. So far, the existing data indicated that I may become a potential class II c-Met inhibitor. After reading the article, we found that the author used 4-Methyl-2-(pyridin-4-yl)thiazole-5-carboxylic acid(cas: 144060-98-0Application of 144060-98-0)

4-Methyl-2-(pyridin-4-yl)thiazole-5-carboxylic acid(cas: 144060-98-0) belongs to pyridine. Pyridine, its benzo and pyridine-based compounds play diverse roles in organic chemistry. As ligands, solvents, and catalysts they facilitate reactions; thus descriptions of these new ligands and their applications abound each year.Application of 144060-98-0

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

Li, Guoliang; He, Yundong; Zhou, Wenbo; Wang, Peng; Zhang, Yong; Tong, Weiguang; Wu, Haigang; Liu, Mingyao; Ye, Xiyun; Chen, Yihua published an article on February 1 ,2014. The article was titled 《Identification, synthesis and photo-protection evaluation of arylthiazole derivatives as a novel series of sunscreens》, and you may find the article in Heterocycles.Recommanded Product: 144060-98-0 The information in the text is summarized as follows:

A series of arylthiazole derivatives I [R3 = C6H5, C6H5CH2, C6H5CH2CH2], II [R1 = C6H5, 4-BrC6H4, 3-H3COC6H4, 2-H3COC6H4], III [n= 1, 2, 3, 5; R = H, n-Pr, n-Bu, Et; R2 = OMe, OEt] and IV [R1 = H, CF3, OMe, Cl; R2 = H, Cl; R3 = H, Cl] was designed and synthesized. Addnl., phenylfuran derivative V [X = O; Y = C; R = H], phenylthiophene derivative V [X = S; Y = C; R = H], phenyloxazole derivative V [X = O; Y = N; R = Me], N-(Ethoxycarbonylmethyl)-2-phenyl-4-thiazolecarboxamide and N-(Ethoxycarbonylmethyl)-3-phenyl-5-methyl-4-isooxazolecarboxamide were also prepared All the synthesized compounds were evaluated for their photo-protective effect against UVB exposure induced cellular damage in keratinocytes cell (HaCaT) and their structure-activity relationship (SAR) was discussed. Among the tested compounds, compound III [n = 1; R = Et; R2 = OEt] significantly protected the dorsal skin of BALB/c-nu mice against UVB-induced decrustation in vivo. The in vitro and in vivo data for these arylthiazole derivatives suggest further studies for their potential use as photo-protection agents as well as sunscreen candidates. After reading the article, we found that the author used 4-Methyl-2-(pyridin-4-yl)thiazole-5-carboxylic acid(cas: 144060-98-0Recommanded Product: 144060-98-0)

4-Methyl-2-(pyridin-4-yl)thiazole-5-carboxylic acid(cas: 144060-98-0) belongs to pyridine. Pyridine, its benzo and pyridine-based compounds play diverse roles in organic chemistry. As ligands, solvents, and catalysts they facilitate reactions; thus descriptions of these new ligands and their applications abound each year.Recommanded Product: 144060-98-0

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

In 2013,New Journal of Chemistry included an article by Zhou, Xiaojing; Zhang, Zhijuan; Li, Baiyan; Yang, Fen; Peng, Yu; Li, Guanghua; Shi, Zhan; Feng, Shouhua; Li, Jing. Electric Literature of C10H8N2O2S. The article was titled 《Two three-dimensional metal-organic frameworks constructed by thiazole-spaced pyridinecarboxylates exhibiting selective gas sorption or antiferromagnetic coupling》. The information in the text is summarized as follows:

The ligand of 2-(4-pyridyl)-4-methylthiazole-5-carboxylic acid (HL) was employed to react with Cd(NO3)2·6H2O or a 50% aqueous solution of Mn(NO3)2, to yield two isomorphous three-dimensional (3D) coordination compounds, [Cd(L)2](H2O)4(DMF) (1) and [Mn(L)2](H2O)3(DMF) (2). The structures and properties of the compounds were characterized by several techniques. Both compounds are three-dimensional (3D) neutral frameworks possessing permanent pores that give rise to straight 1-dimensional channels. Compound 1 displays adsorption selectivity for CO2, while the low pressure sorption of H2, N2, CH4, CO, O2 at 298 K are negligible; Compound 2 shows weak anti-ferromagnetic coupling between the magnetic centers. After reading the article, we found that the author used 4-Methyl-2-(pyridin-4-yl)thiazole-5-carboxylic acid(cas: 144060-98-0Electric Literature of C10H8N2O2S)

4-Methyl-2-(pyridin-4-yl)thiazole-5-carboxylic acid(cas: 144060-98-0) belongs to pyridine. Pyridine, its benzo and pyridine-based compounds play diverse roles in organic chemistry. As ligands, solvents, and catalysts they facilitate reactions; thus descriptions of these new ligands and their applications abound each year.Electric Literature of C10H8N2O2S

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

In 2018,Turkish Journal of Chemistry included an article by Kayagil, Ismail; Mutlu, Ayse Guel; Bayhan, Ulkue; Yilmaz, Inanc; Demirayak, Seref. Electric Literature of C10H8N2O2S. The article was titled 《Synthesis and characterizations of novel thiazolyl-thiadiazole derivatives as telomerase activators》. The information in the text is summarized as follows:

Pyridine-3/4-thiocarboxamide derivatives were used as starting materials for the synthesis of the target compounds The pyridine-3/4-thiocarboxamide derivatives were reacted with Et 2-chloroacetoacetate in ethanol to give the thiazole derivatives The two Et thiazole-carboxylate derivatives thus obtained were treated with sodium hydroxide solution and ethanol and converted to carboxylic acids. The carboxylic acid derivatives were reacted with thiosemicarbazide in phosphoroxy trichloride and aminothiadiazole rings (5, 6) were formed. Thus, two thiazolyl-thiadiazole amine derivatives were obtained. These two derivatives were converted into two chloroacetamidothiadiazole derivatives by reaction with chloroacetylchloride over the amino group in the presence of triethylamine in acetone. After all these steps, the starting materials needed to reach the target compounds were obtained. With the two derivatives obtained in this last step, phenol and thiophenol derivatives were reacted in acetone in the presence of potassium carbonate. The target compounds, thiazolyl-thiadiazole derivatives (TDA1-6) , are completely unique and their structure has been elucidated by elemental anal., IR, NMR, and MS spectral data. After all these synthesis steps, telomerase activity studies were performed on the target compounds obtained. For this purpose, a PCR ELISA-based TRAP method was used on the heart of zebrafish. According to the enzyme assay results, derivative TDA8 has shown an increase of telomerase enzyme activity. After reading the article, we found that the author used 4-Methyl-2-(pyridin-4-yl)thiazole-5-carboxylic acid(cas: 144060-98-0Electric Literature of C10H8N2O2S)

4-Methyl-2-(pyridin-4-yl)thiazole-5-carboxylic acid(cas: 144060-98-0) belongs to pyridine. Pyridine, its benzo and pyridine-based compounds play diverse roles in organic chemistry. As ligands, solvents, and catalysts they facilitate reactions; thus descriptions of these new ligands and their applications abound each year.Electric Literature of C10H8N2O2S

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

《Identification of 1,3-thiazole-5-carboxylic Acid Derivatives as Inhibitors of Protein Kinase CK2》 was written by Protopopov, Mykola V.; Volynets, Galyna P.; Starosyla, Sergiy A.; Vdovin, Vasyl S.; Lukashov, Sergiy S.; Bilokin, Yaroslav V.; Bdzhola, Volodymyr G.; Yarmoluk, Sergiy M.. Application In Synthesis of 4-Methyl-2-(pyridin-4-yl)thiazole-5-carboxylic acid And the article was included in Current Enzyme Inhibition on August 31 ,2018. The article conveys some information:

Serine/threonine protein kinase CK2 is involved in the regulation of a number of cellular functions such as cell growth, proliferation, differentiation and apoptosis. Increased activity of CK2 is associated with the development of different types of cancer, inflammatory response, pain and virus infections. Therefore, protein kinase CK2 is an attractive mol. target for the development of small-mol. inhibitors which can be important compounds for pharmaceutical application. The main aim of this research is to identify novel chem. class of CK2 inhibitors with good lead-like properties. In order to find novel CK2 inhibitors, virtual screening experiments were performed using Autodock software. Best-scored compounds were tested in vitro using P32 radioactive kinase assay. Small-mol. inhibitors of protein kinase CK2 were identified among the derivatives of 1,3-thiazole-5-carboxylic acid. The most active compound inhibited CK2 with IC50 value of 0.4 μM. Ligand efficiency for studied derivatives of 1,3-thiazole-5-carboxylic acid was in the range from 0.45 to 0.56 kcal/mol/non-hydrogen atom. Considering the fact that the lower limit for ligand efficiency parameter is 0.3, the identified CK2 inhibitors among the derivatives of 1,3-thiazole-5-carboxylic acid are excellent candidates for further lead optimization. The results came from multiple reactions, including the reaction of 4-Methyl-2-(pyridin-4-yl)thiazole-5-carboxylic acid(cas: 144060-98-0Application In Synthesis of 4-Methyl-2-(pyridin-4-yl)thiazole-5-carboxylic acid)

4-Methyl-2-(pyridin-4-yl)thiazole-5-carboxylic acid(cas: 144060-98-0) belongs to pyridine. Pyridine-based materials are valued for their optical and physical properties as well as their medical potential. Additionally, pyridine-based natural products continue to be discovered and studied for their properties and to understand their biosynthesis.Application In Synthesis of 4-Methyl-2-(pyridin-4-yl)thiazole-5-carboxylic acid

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

In 2015,Angewandte Chemie, International Edition included an article by Adams, Luke A.; Sharma, Pooja; Mohanty, Biswaranjan; Ilyichova, Olga V.; Mulcair, Mark D.; Williams, Martin L.; Gleeson, Ellen C.; Totsika, Makrina; Doak, Bradley C.; Caria, Sofia; Rimmer, Kieran; Horne, James; Shouldice, Stephen R.; Vazirani, Mansha; Headey, Stephen J.; Plumb, Brent R.; Martin, Jennifer L.; Heras, Begona; Simpson, Jamie S.; Scanlon, Martin J.. Related Products of 144060-98-0. The article was titled 《Application of Fragment-Based Screening to the Design of Inhibitors of Escherichia coli DsbA》. The information in the text is summarized as follows:

The thiol-disulfide oxidoreductase enzyme DsbA catalyzes the formation of disulfide bonds in the periplasm of Gram-neg. bacteria. DsbA substrates include proteins involved in bacterial virulence. In the absence of DsbA, many of these proteins do not fold correctly, which renders the bacteria avirulent. Thus DsbA is a critical mediator of virulence and inhibitors may act as antivirulence agents. Biophys. screening has been employed to identify fragments that bind to DsbA from Escherichia coli. Elaboration of one of these fragments produced compounds that inhibit DsbA activity in vitro. In cell-based assays, the compounds inhibit bacterial motility, but have no effect on growth in liquid culture, which is consistent with selective inhibition of DsbA. Crystal structures of inhibitors bound to DsbA indicate that they bind adjacent to the active site. Together, the data suggest that DsbA may be amenable to the development of novel antibacterial compounds that act by inhibiting bacterial virulence.4-Methyl-2-(pyridin-4-yl)thiazole-5-carboxylic acid(cas: 144060-98-0Related Products of 144060-98-0) was used in this study.

4-Methyl-2-(pyridin-4-yl)thiazole-5-carboxylic acid(cas: 144060-98-0) belongs to pyridine. Pyridine, its benzo and pyridine-based compounds play diverse roles in organic chemistry. As ligands, solvents, and catalysts they facilitate reactions; thus descriptions of these new ligands and their applications abound each year.Related Products of 144060-98-0

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

《Design, synthesis, and biological evaluation of [1,2,4]triazolo[4,3-a] pyrazine derivatives as novel dual c-Met/VEGFR-2 inhibitors》 was published in Frontiers in Chemistry (Lausanne, Switzerland) in 2022. These research results belong to Liu, Xiaobo; Li, Yuzhen; Zhang, Qian; Pan, Qingshan; Zheng, Pengwu; Dai, Xinyang; Bai, Zhaoshi; Zhu, Wufu. HPLC of Formula: 144060-98-0 The article mentions the following:

In this study, a series of novel [1,2,4]triazolo[4,3-a]pyrazine derivatives, I (R = 4-methyl-2-phenyl-1,3-thiazol-5-yl, 4-(4-methyl-1,3-thiazol-2-yl)pyridine, 3-(thiophen-2-yl)-1H-pyrazol-5-yl, etc.; R1 = H, Me; X = H, F) evaluated for their inhibitory activities toward c-Met/VEGFR-2 kinases and antiproliferative activities against tested three cell lines in vitro was designed and synthesized. Most of the compounds I showed satisfactory activity compared with lead compound foretinib. Among them, the most promising compound I (R = 1-(4-chlorophenyl)-5-(trifluoromethyl)-1H-pyrazol-4-yl, R1 = Me; X = F) (II) exhibited excellent antiproliferative activities against A549, MCF-7, and Hela cancer cell lines with IC50 values of 0.98 ± 0.08, 1.05 ± 0.17, and 1.28 ± 0.25μM, resp., as well as excellent kinase inhibitory activities (c-Met IC50 = 26.00 nM and VEGFR-2 IC50 = 2.6μM). Moreover, compound II inhibited the growth of A549 cells in G0/G1 phase in a dose-dependent manner, and induced the late apoptosis of A549 cells. Its intervention on intracellular c-Met signaling of A549 was verified by the result of Western blot. Fluorescence quant. PCR showed that compound 17l inhibited the growth of A549 cells by inhibiting the expression of c-Met and VEGFR-2, and its hemolytic toxicity was low. Mol. docking and mol. dynamics simulation indicated that compound II could bind to c-Met and VEGFR-2 protein, which was similar to that of foretinib. In the experiment, the researchers used 4-Methyl-2-(pyridin-4-yl)thiazole-5-carboxylic acid(cas: 144060-98-0HPLC of Formula: 144060-98-0)

4-Methyl-2-(pyridin-4-yl)thiazole-5-carboxylic acid(cas: 144060-98-0) belongs to pyridine. Pyridine-based materials are valued for their optical and physical properties as well as their medical potential. Additionally, pyridine-based natural products continue to be discovered and studied for their properties and to understand their biosynthesis.HPLC of Formula: 144060-98-0

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

《Design, synthesis, and biological evaluation of [1,2,4]triazolo[4,3-a] pyrazine derivatives as novel dual c-Met/VEGFR-2 inhibitors》 was published in Frontiers in Chemistry (Lausanne, Switzerland) in 2022. These research results belong to Liu, Xiaobo; Li, Yuzhen; Zhang, Qian; Pan, Qingshan; Zheng, Pengwu; Dai, Xinyang; Bai, Zhaoshi; Zhu, Wufu. Synthetic Route of C10H8N2O2S The article mentions the following:

In this study, a series of novel [1,2,4]triazolo[4,3-a]pyrazine derivatives, I (R = 4-methyl-2-phenyl-1,3-thiazol-5-yl, 4-(4-methyl-1,3-thiazol-2-yl)pyridine, 3-(thiophen-2-yl)-1H-pyrazol-5-yl, etc.; R1 = H, Me; X = H, F) evaluated for their inhibitory activities toward c-Met/VEGFR-2 kinases and antiproliferative activities against tested three cell lines in vitro was designed and synthesized. Most of the compounds I showed satisfactory activity compared with lead compound foretinib. Among them, the most promising compound I (R = 1-(4-chlorophenyl)-5-(trifluoromethyl)-1H-pyrazol-4-yl, R1 = Me; X = F) (II) exhibited excellent antiproliferative activities against A549, MCF-7, and Hela cancer cell lines with IC50 values of 0.98 ± 0.08, 1.05 ± 0.17, and 1.28 ± 0.25μM, resp., as well as excellent kinase inhibitory activities (c-Met IC50 = 26.00 nM and VEGFR-2 IC50 = 2.6μM). Moreover, compound II inhibited the growth of A549 cells in G0/G1 phase in a dose-dependent manner, and induced the late apoptosis of A549 cells. Its intervention on intracellular c-Met signaling of A549 was verified by the result of Western blot. Fluorescence quant. PCR showed that compound 17l inhibited the growth of A549 cells by inhibiting the expression of c-Met and VEGFR-2, and its hemolytic toxicity was low. Mol. docking and mol. dynamics simulation indicated that compound II could bind to c-Met and VEGFR-2 protein, which was similar to that of foretinib. In the experiment, the researchers used 4-Methyl-2-(pyridin-4-yl)thiazole-5-carboxylic acid(cas: 144060-98-0Synthetic Route of C10H8N2O2S)

4-Methyl-2-(pyridin-4-yl)thiazole-5-carboxylic acid(cas: 144060-98-0) belongs to pyridine. Pyridine-based materials are valued for their optical and physical properties as well as their medical potential. Additionally, pyridine-based natural products continue to be discovered and studied for their properties and to understand their biosynthesis.Synthetic Route of C10H8N2O2S

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