Category: 599183-36-5

Related Products of 599183-36-5. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: 3-Iodo-1H-indazol-5-amine, is researched, Molecular C7H6IN3, CAS is 599183-36-5, about Identification of 3-sulfonylindazole derivatives as potent and selective 5-HT6 antagonists. Author is Liu, Kevin G.; Robichaud, Albert J.; Greenfield, Alexander A.; Lo, Jennifer R.; Grosanu, Cristina; Mattes, James F.; Cai, Yanxuan; Zhang, Guo Ming; Zhang, Jean Y.; Kowal, Dianne M.; Smith, Deborah L.; Di, Li; Kerns, Edward H.; Schechter, Lee E.; Comery, Thomas A..

As part of our efforts to develop agents for cognitive enhancement, we have been focused on the 5-HT6 receptor in order to identify potent and selective ligands for this purpose. Herein we report the identification of a novel series of 3-sulfonylindazole derivatives with acyclic amino side chains as potent and selective 5-HT6 antagonists. The synthesis and detailed SAR of this class of compounds are reported.

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

Quality Control of 3-Iodo-1H-indazol-5-amine. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 3-Iodo-1H-indazol-5-amine, is researched, Molecular C7H6IN3, CAS is 599183-36-5, about The discovery of orally bioavailable tyrosine threonine kinase (TTK) inhibitors: 3-(4-(heterocyclyl)phenyl)-1H-indazole-5-carboxamides as anticancer agents. Author is Liu, Yong; Lang, Yunhui; Patel, Narendra Kumar; Ng, Grace; Laufer, Radoslaw; Li, Sze-Wan; Edwards, Louise; Forrest, Bryan; Sampson, Peter B.; Feher, Miklos; Ban, Fuqiang; Awrey, Donald E.; Beletskaya, Irina; Mao, Guodong; Hodgson, Richard; Plotnikova, Olga; Qiu, Wei; Chirgadze, Nickolay Y.; Mason, Jacqueline M.; Wei, Xin; Lin, Dan Chi-Chia; Che, Yi; Kiarash, Reza; Madeira, Brian; Fletcher, Graham C.; Mak, Tak W.; Bray, Mark R.; Pauls, Henry W..

The acetamido and carboxamido substituted 3-(1H-indazol-3-yl)benzenesulfonamides are potent TTK inhibitors. However, they display modest ability to attenuate cancer cell growth; their physicochem. properties, and attendant pharmacokinetic parameters, are not drug-like. By eliminating the polar 3-sulfonamide group and grafting a heterocycle at the 4 position of the Ph ring, potent inhibitors with oral exposure were obtained. An x-ray cocrystal structure and a refined binding model allowed for a structure guided approach. Systematic optimization resulted in novel TTK inhibitors, namely 3-(4-(heterocyclyl)phenyl)-1H-indazole-5-carboxamides. Compounds incorporating the 3-hydroxy-8-azabicyclo[3.2.1]octan-8-yl bicyclic system were potent (TTK IC50 < 10 nM, HCT116 GI50 < 0.1 μM), displayed low off-target activity (>500×), and microsomal stability (T1/2 > 30 min). A subset was tested in rodent PK and mouse xenograft models of human cancer. Compound I (CFI-401870) recapitulated the phenotype of TTK RNAi, demonstrated in vivo tumor growth inhibition upon oral dosing, and was selected for preclin. evaluation.

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

The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: 3-Iodo-1H-indazol-5-amine, is researched, Molecular C7H6IN3, CAS is 599183-36-5, about 3H-Pyrazolo[4,3-f]quinoline-Based Kinase Inhibitors Inhibit the Proliferation of Acute Myeloid Leukemia Cells In Vivo, the main research direction is pyrazoloquinoline preparation antitumor activity tyrosine kinase inhibition mol docking.Category: piperazines.

Herein, various 3H-pyrazolo[4,3-f]quinoline-containing compounds e.g., I were rapidly assembled via the Doebner-Povarov multicomponent reaction from the readily available 5-aminoindazoles, ketones and aldehydes in good yields. The most active compounds potently inhibit the recombinant FLT3 kinase and its mutant forms with nanomolar IC50 values. Docking studies with the FLT3 kinase showed a type I binding mode, where the 3H-pyrazolo group interacts with Cys694 in the hinge region. The compounds blocked the proliferation of AML cell lines harboring oncogenic FLT3-ITD mutations with remarkable IC50 values, which were comparable to the approved FLT3 inhibitor quizartinib. The compounds also inhibited the growth of leukemia in a mouse-disseminated AML model, and hence, the novel 3H-pyrazolo[4,3-f]quinoline-containing kinase inhibitors are potential lead compounds to develop into anticancer agents, especially for kinase-driven cancers.

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

The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: 3-Iodo-1H-indazol-5-amine, is researched, Molecular C7H6IN3, CAS is 599183-36-5, about 2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization, the main research direction is diaminopyrimidine MK2 inhibitor preparation structure inhibitor.Related Products of 599183-36-5.

We describe structure-based optimization of a series of novel 2,4-diaminopyrimidine MK2 inhibitors. Co-crystal structures (see accompanying Letter) demonstrated a unique inhibitor binding mode. Resulting inhibitors had IC50 values as low as 19 nM and moderate selectivity against a kinase panel. Compounds 15, 31a, and 31b inhibit TNFα production in peripheral human monocytes.

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

The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: 3-Iodo-1H-indazol-5-amine, is researched, Molecular C7H6IN3, CAS is 599183-36-5, about 2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization, the main research direction is diaminopyrimidine MK2 inhibitor preparation structure inhibitor.Related Products of 599183-36-5.

We describe structure-based optimization of a series of novel 2,4-diaminopyrimidine MK2 inhibitors. Co-crystal structures (see accompanying Letter) demonstrated a unique inhibitor binding mode. Resulting inhibitors had IC50 values as low as 19 nM and moderate selectivity against a kinase panel. Compounds 15, 31a, and 31b inhibit TNFα production in peripheral human monocytes.

Compound(599183-36-5)Related Products of 599183-36-5 received a lot of attention, and I have introduced some compounds in other articles, similar to this compound(3-Iodo-1H-indazol-5-amine), if you are interested, you can check out my other related articles.

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

The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: 3-Iodo-1H-indazol-5-amine, is researched, Molecular C7H6IN3, CAS is 599183-36-5, about 2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization, the main research direction is diaminopyrimidine MK2 inhibitor preparation structure inhibitor.Related Products of 599183-36-5.

We describe structure-based optimization of a series of novel 2,4-diaminopyrimidine MK2 inhibitors. Co-crystal structures (see accompanying Letter) demonstrated a unique inhibitor binding mode. Resulting inhibitors had IC50 values as low as 19 nM and moderate selectivity against a kinase panel. Compounds 15, 31a, and 31b inhibit TNFα production in peripheral human monocytes.

Compound(599183-36-5)Related Products of 599183-36-5 received a lot of attention, and I have introduced some compounds in other articles, similar to this compound(3-Iodo-1H-indazol-5-amine), if you are interested, you can check out my other related articles.

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