Category: 18213-75-7

Antitumor activity of eighty-four synthesized N-heteroaromatic compounds was written by Hayashi, Eisaku;Higashino, Takeo;Iijima, Chihoko;Oishi, Etsuo;Makino, Hirokazu;Irie, Toshio;Yamamoto, Fusako;Yokoyama, Yoko;Iwai, Yoshihisa. And the article was included in Yakugaku Zasshi in 1977.Product Details of 18213-75-7 This article mentions the following:

Eighty-four compounds (mainly N-heteroaromatic compounds) were synthesized and their antitumor activity was examined Four quinoline derivatives had some antitumor effect on the solid type of Ehrlich carcinoma. These compounds were, 3-hydroxy-6-quinolinecarbonitrile (I) [63124-12-9], 6-bromoquinaldic acid 1-oxide [65147-79-7], 8-(hydroxyimino)-5,6,7,8-tetrahydroquinoline [58509-59-4] and 1-(hydroxyimino)-1,2,3,4-tetrahydroacridine [34043-68-0]. No other derivatives were found effective. In the experiment, the researchers used many compounds, for example, 5-Amino-1-methyl-1H-pyrazole-4-carboxamide (cas: 18213-75-7Product Details of 18213-75-7).

5-Amino-1-methyl-1H-pyrazole-4-carboxamide (cas: 18213-75-7) belongs to pyrazole derivatives. Pyrazole is a weak base, with pKb 11.5 (pKa of the conjugated acid 2.49 at 25 鎺矯).Pyrazole used as a ligand to prepare organometallic compounds. Pyrazole rings have been used as core components of several leading non-steroidal anti-inflammatory drugs (NSAIDs) and antihypertensive drugs. It has also been found to be useful as a bifunctional ligand for metal catalysis.Product Details of 18213-75-7

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Condensed pyrimidine systems. 4. Synthesis and transformations of 6-(trifluoromethyl)-1H-pyrazolo[3,4-d]pyrimidin-4(5H)-ones was written by Bol’but, A. V.;Korol’ov, O. K.;Vovk, M. V.. And the article was included in Zhurnal Organichnoi ta Farmatsevtichnoi Khimii in 2006.HPLC of Formula: 18213-75-7 This article mentions the following:

1-R-6-Trifluoromethyl-1H-pyrazolo[3,4-d]pyrimidin-4(5H)-ones (2a–d; R = Me, PhCH₂, Ph, 3-ClC₆H₄) were prepared by heterocyclization of 5-aminopyrazole-4-carboxamides with Me trifluoroacetate. The pyrimidinones 2 were converted into the corresponding 4-alkoxy, chloro, amino and hydrazino derivatives and 7-R-5-trifluoromethyl-7H-pyrazolo[4,3-e]tetrazolo[1,5-c]pyrimidines (7a–c; R = PhCH₂, Ph, 3-ClC₆H₄). In the experiment, the researchers used many compounds, for example, 5-Amino-1-methyl-1H-pyrazole-4-carboxamide (cas: 18213-75-7HPLC of Formula: 18213-75-7).

5-Amino-1-methyl-1H-pyrazole-4-carboxamide (cas: 18213-75-7) belongs to pyrazole derivatives. The 1H-pyrazole provides an excellent means by which to provide the requisite hydrogen bond acceptor閳ユ徆onor motifs, whether as a monocyclic ring or as a fused indazole ring. Protonation of pyrazole in strong acid leads to pyrazolium cations, which undergo electrophilic substitution preferentially at C3 rather than C4. The pyrazole anion is not reactive toward nucleophiles but is mostly reactive to electrophiles.HPLC of Formula: 18213-75-7

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Condensed pyrimidine systems. 5.6-methyl-functionalized in pyrazolo[3,4-d]pyrimidin-4(5H)-ones was written by Bol’but, A. V.;Vovk, M. V.. And the article was included in Zhurnal Organichnoi ta Farmatsevtichnoi Khimii in 2006.HPLC of Formula: 18213-75-7 This article mentions the following:

The cyclocondensation of chloroacetyl chloride with 5-amino-1H-pyrazole-4-carboxamide derivatives gave 6-(chloromethyl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one derivatives Reaction of the latter with thiourea or sodium azide gave 6-[[amino(imino)thio]methyl]-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one and 6-(azidomethyl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one derivatives The latter compounds were then converted into corresponding 6-(aminomethyl), 6-(amidomethyl)- and 6-(thiomethyl) derivatives In the experiment, the researchers used many compounds, for example, 5-Amino-1-methyl-1H-pyrazole-4-carboxamide (cas: 18213-75-7HPLC of Formula: 18213-75-7).

5-Amino-1-methyl-1H-pyrazole-4-carboxamide (cas: 18213-75-7) belongs to pyrazole derivatives. Pyrazoles, a five-membered heterocycle containing two adjacent nitrogen atoms, are the core structures found in a number of molecules that possess a wide range of pharmaceutical and agricultural activities. Pyrazoles can be selectively lithiated at different carbons and subsequently react with electrophiles depending on the substitution patterns.HPLC of Formula: 18213-75-7

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Pyrazolo-pyrimidines: A novel heterocyclic scaffold for potent and selective p38α inhibitors was written by Das, Jagabandhu;Moquin, Robert V.;Pitt, Sidney;Zhang, Rosemary;Shen, Ding Ren;McIntyre, Kim W.;Gillooly, Kathleen;Doweyko, Arthur M.;Sack, John S.;Zhang, Hongjian;Kiefer, Susan E.;Kish, Kevin;McKinnon, Murray;Barrish, Joel C.;Dodd, John H.;Schieven, Gary L.;Leftheris, Katerina. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2008.Computed Properties of C5H8N4O This article mentions the following:

The synthesis and structure-activity relationships (SAR) of p38α MAP kinase inhibitors based on a pyrazolo-pyrimidine scaffold are described. These studies led to the identification of compound I as a potent and selective inhibitor of p38α MAP kinase with excellent cellular potency toward the inhibition of TNFα production I was highly efficacious in vivo in inhibiting TNFα production in an acute murine model of TNFα production X-ray co-crystallog. of a pyrazolopyrimidine analog bound to unphosphorylated p38α is also disclosed. In the experiment, the researchers used many compounds, for example, 5-Amino-1-methyl-1H-pyrazole-4-carboxamide (cas: 18213-75-7Computed Properties of C5H8N4O).

5-Amino-1-methyl-1H-pyrazole-4-carboxamide (cas: 18213-75-7) belongs to pyrazole derivatives. The strategies for the synthesis of pyrazoles generally can be applied for the construction of indazoles. Pyrazole the presence of this nucleus in pharmacological agents of diverse therapeutic categories such as celecoxib, a potent anti-inflammatory, the antidepressant agent fezolamide have proved the pharmacological potential of the pyrazole moiety. Computed Properties of C5H8N4O

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

NVP-BHG712: Effects of Regioisomers on the Affinity and Selectivity toward the EPHrin Family was written by Troester, Alix;Heinzlmeir, Stephanie;Berger, Benedict-Tilman;Gande, Santosh L.;Saxena, Krishna;Sreeramulu, Sridhar;Linhard, Verena;Nasiri, Amir H.;Bolte, Michael;Mueller, Susanne;Kuster, Bernhard;Medard, Guillaume;Kudlinzki, Denis;Schwalbe, Harald. And the article was included in ChemMedChem in 2018.Formula: C5H8N4O This article mentions the following:

Erythropoietin-producing hepatocellular (EPH) receptors are transmembrane receptor tyrosine kinases. Their extracellular domains bind specifically to ephrin A/B ligands, and this binding modulates intracellular kinase activity. EPHs are key players in bidirectional intercellular signaling, controlling cell morphol., adhesion, and migration. They are increasingly recognized as cancer drug targets. We analyzed the binding of NVP-BHG712 (NVP) to EPHA2 and EPHB4. Unexpectedly, all tested com. available NVP samples turned out to be a regioisomer (NVPiso) of the inhibitor, initially described in a Novartis patent application. They only differ by the localization of a single Me group on either one of two adjacent nitrogen atoms. The two compounds of identical mass revealed different binding modes. Furthermore, both in vitro and in vivo experiments showed that the isomers differ in their kinase affinity and selectivity. In the experiment, the researchers used many compounds, for example, 5-Amino-1-methyl-1H-pyrazole-4-carboxamide (cas: 18213-75-7Formula: C5H8N4O).

5-Amino-1-methyl-1H-pyrazole-4-carboxamide (cas: 18213-75-7) belongs to pyrazole derivatives. The 1H-pyrazole provides an excellent means by which to provide the requisite hydrogen bond acceptor–donor motifs, whether as a monocyclic ring or as a fused indazole ring. Pyrazoles and pyrimidines have diverse biological and pharmacological activities. There are a number of antimicrobial compounds containing pyrazole moiety as the core unit. Pyrazofurin is important antimicrobial drug and 2-methylpyrimidine-4-ylamine derivatives I and II were found to be effective inhibitors of Escherichia coli PDHc-E1 with antibacterial and antifungal activity.Formula: C5H8N4O

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Pyrimidinone Nicotinamide Mimetics as Selective Tankyrase and Wnt Pathway Inhibitors Suitable for in Vivo Pharmacology was written by Johannes, Jeffrey W.;Almeida, Lynsie;Barlaam, Bernard;Boriack-Sjodin, P. Ann;Casella, Robert;Croft, Rosemary A.;Dishington, Allan P.;Gingipalli, Lakshmaiah;Gu, Chungang;Hawkins, Janet L.;Holmes, Jane L.;Howard, Tina;Huang, Jian;Ioannidis, Stephanos;Kazmirski, Steven;Lamb, Michelle L.;McGuire, Thomas M.;Moore, Jane E.;Ogg, Derek;Patel, Anil;Pike, Kurt G.;Pontz, Timothy;Robb, Graeme R.;Su, Nancy;Wang, Haiyun;Wu, Xiaoyun;Zhang, Hai-Jun;Zhang, Yue;Zheng, Xiaolan;Wang, Tao. And the article was included in ACS Medicinal Chemistry Letters in 2015.Product Details of 18213-75-7 This article mentions the following:

The canonical Wnt pathway plays an important role in embryonic development, adult tissue homeostasis, and cancer. Germline mutations of several Wnt pathway components, such as Axin, APC, and ss-catenin, can lead to oncogenesis. Inhibition of the poly(ADP-ribose) polymerase (PARP) catalytic domain of the tankyrases (TNKS1 and TNKS2) is known to inhibit the Wnt pathway via increased stabilization of Axin. In order to explore the consequences of tankyrase and Wnt pathway inhibition in preclin. models of cancer and its impact on normal tissue, the authors sought a small mol. inhibitor of TNKS1/2 with suitable physicochem. properties and pharmacokinetics for hypothesis testing in vivo. Starting from a 2-Ph quinazolinone hit I, the authors discovered the pyrrolopyrimidinone compound II (AZ6102), which is a potent TNKS1/2 inhibitor that has 100-fold selectivity against other PARP family enzymes and shows 5 nM Wnt pathway inhibition in DLD-1 cells. Moreover, compound II can be formulated well in a clin. relevant i.v. solution at 20 mg/mL, has demonstrated good pharmacokinetics in preclin. species, and shows low Caco2 efflux to avoid possible tumor resistance mechanisms. In the experiment, the researchers used many compounds, for example, 5-Amino-1-methyl-1H-pyrazole-4-carboxamide (cas: 18213-75-7Product Details of 18213-75-7).

5-Amino-1-methyl-1H-pyrazole-4-carboxamide (cas: 18213-75-7) belongs to pyrazole derivatives. An alternative way to synthesize multisubstituted pyrazoles is the Csingle bondH arylation of simple pyrazoles. Pyrazole rings have been used as core components of several leading non-steroidal anti-inflammatory drugs (NSAIDs) and antihypertensive drugs. It has also been found to be useful as a bifunctional ligand for metal catalysis.Product Details of 18213-75-7

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Cyclic guanidines: synthesis and antiplatelet activity of 4,6,7,8-tetrahydro-1H-imidazo[1,2-a]pyrazolo[3,4-d]pyrimidin-7-ones and 1,4,6,7,8,9-hexahydropyrazolo[3′,4′:4,5]pyrimido[2,1-c][1,2,4]triazin-7-ones was written by Ferroni, R.;Simoni, D.;Orlandini, P.;Bardi, A.;Franze, G. P.;Guarneri, M.. And the article was included in Arzneimittel-Forschung in 1990.SDS of cas: 18213-75-7 This article mentions the following:

I (R = e.g., Me, Ph, 4-ClC₆H₄, R¹ = Bu, benzyl, or H) and II (R = e.g., Me, Ph, 4-ClC₆H₄) were prepared starting from 5-amino-4-cyano-1-(2,5-dichlorophenyl)pyrazole through a series of reactions. The compounds were tested for inhibition against blood platelet aggregation induced by ADP or collagen. Among the compounds tested I (R = 2,5-dichlorophenyl, R¹ = CH₂Ph), showed the highest activity. An increase in lipophilicity of the substituent was accompanied by an increase in the platelet aggregation inhibitory activity. Structure-activity relations are discussed. In the experiment, the researchers used many compounds, for example, 5-Amino-1-methyl-1H-pyrazole-4-carboxamide (cas: 18213-75-7SDS of cas: 18213-75-7).

5-Amino-1-methyl-1H-pyrazole-4-carboxamide (cas: 18213-75-7) belongs to pyrazole derivatives. An alternative way to synthesize multisubstituted pyrazoles is the Csingle bondH arylation of simple pyrazoles. Pyrazoles can be selectively lithiated at different carbons and subsequently react with electrophiles depending on the substitution patterns.SDS of cas: 18213-75-7

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics