Category: 27489-62-9

《Selectivity and Physicochemical Optimization of Repurposed Pyrazolo[1,5-b]pyridazines for the Treatment of Human African Trypanosomiasis》 was written by Tear, Westley F.; Bag, Seema; Diaz-Gonzalez, Rosario; Ceballos-Perez, Gloria; Rojas-Barros, Domingo I.; Cordon-Obras, Carlos; Perez-Moreno, Guiomar; Garcia-Hernandez, Raquel; Martinez-Martinez, Maria Santos; Ruiz-Perez, Luis Miguel; Gamarro, Francisco; Gonzalez Pacanowska, Dolores; Caffrey, Conor R.; Ferrins, Lori; Manzano, Pilar; Navarro, Miguel; Pollastri, Michael P.. HPLC of Formula: 27489-62-9 And the article was included in Journal of Medicinal Chemistry in 2020. The article conveys some information:

From a high-throughput screen of 42 444 known human kinases inhibitors, a pyrazolo[1,5-b]pyridazine scaffold was identified to begin optimization for the treatment of human African trypanosomiasis. Previously reported data for analogous compounds against human kinases GSK-3β, CDK-2, and CDK-4 were leveraged to try to improve the selectivity of the series, resulting in 23a which showed selectivity for T. b. brucei over these three human enzymes. In parallel, properties known to influence the absorption, distribution, metabolism, and excretion (ADME) profile of the series were optimized resulting in 20g being progressed into an efficacy study in mice. Though 20g showed toxicity in mice, it also demonstrated CNS penetration in a PK study and significant reduction of parasitemia in four out of the six mice. The experimental process involved the reaction of trans-4-Aminocyclohexanol(cas: 27489-62-9HPLC of Formula: 27489-62-9)

trans-4-Aminocyclohexanol(cas: 27489-62-9) belongs to anime. Aniline, ethanolamines, and several other amines are major industrial commodities used in making rubber, dyes, pharmaceuticals, and synthetic resins and fibres and for a host of other applications. Most of the numerous methods for the preparation of amines may be broadly divided into two groups: (1) chemical reduction (replacement of oxygen with hydrogen atoms in the molecule) of members of several other classes of organic nitrogen compounds and (2) reactions of ammonia or amines with organic compounds.HPLC of Formula: 27489-62-9

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In 2018,Bioorganic & Medicinal Chemistry included an article by Hei, Yuan-Yuan; Shen, Ying; Wang, Jin; Zhang, Hao; Zhao, Hong-Yi; Xin, Minhang; Cao, Yong-Xiao; Li, Yan; Zhang, San-Qi. Name: trans-4-Aminocyclohexanol. The article was titled 《Synthesis and evaluation of 2,9-disubstituted 8-phenylthio/phenylsulfinyl-9H-purine as new EGFR inhibitors》. The information in the text is summarized as follows:

In present study, we described the synthesis and biol. evaluation of a new class of EGFR inhibitors containing 2,9-disubstituted 8-phenylthio/phenylsulfinyl-9H-purine scaffold. Thirty-one compounds were synthesized. Among them, compound I displayed the IC50 of 29.4 nM against HCC827 cell line and 1.9 nM against EGFRL858R. Compound II showed moderate inhibitory activity against EGFRL858R/T790M/C797S (IC50 = 114 nM). Western bolt assay suggested that compound I significantly inhibited EGFR phosphorylation. In vivo test, compound I remarkably exhibited inhibitory effect on tumor growth at 5.0 mg/kg by oral administration in established nude mouse HCC827 xenograft model. These results indicate that the 2,9-disubstituted 8-phenylsulfinyl/phenylsulfinyl-9H-purine derivatives can act as potent EGFR(L858R) inhibitors and effective anticancer agents. Addnl., optimization of compound C12 may result in discovering the fourth-generation EGFR-TKIs. In the experiment, the researchers used many compounds, for example, trans-4-Aminocyclohexanol(cas: 27489-62-9Name: trans-4-Aminocyclohexanol)

trans-4-Aminocyclohexanol(cas: 27489-62-9) belongs to anime. Examples of direct uses of amines and their salts are as corrosion inhibitors in boilers and in lubricating oils (morpholine), as antioxidants for rubber and roofing asphalt (diarylamines), as stabilizers for cellulose nitrate explosives (diphenylamine), as protectants against damage from gamma radiation (diarylamines), as developers in photography (aromatic diamines), as flotation agents in mining, as anticling and waterproofing agents for textiles, as fabric softeners, in paper coating, and for solubilizing herbicides.Name: trans-4-Aminocyclohexanol

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Application of 27489-62-9In 2021 ,《Template-Hopping Approach Leads to Potent, Selective, and Highly Soluble Bromo and Extraterminal Domain (BET) Second Bromodomain (BD2) Inhibitors》 appeared in Journal of Medicinal Chemistry. The author of the article were Aylott, Helen E.; Atkinson, Stephen J.; Bamborough, Paul; Bassil, Anna; Chung, Chun-wa; Gordon, Laurie; Grandi, Paola; Gray, James R. J.; Harrison, Lee A.; Hayhow, Thomas G.; Messenger, Cassie; Mitchell, Darren; Phillipou, Alexander; Preston, Alex; Prinjha, Rab K.; Rianjongdee, Francesco; Rioja, Inmaculada; Seal, Jonathan T.; Wall, Ian D.; Watson, Robert J.; Woolven, James M.; Demont, Emmanuel H.. The article conveys some information:

A number of reports have recently been published describing the discovery and optimization of bromo and extraterminal inhibitors which are selective for the second bromodomain (BD2); these include our own work toward GSK046 and GSK620. This paper describes our approach to mitigating the genotoxicity risk of GSK046 by replacement of the acetamide functionality with a heterocyclic ring. This was followed by a template-hopping and hybridization approach, guided by structure-based drug design, to incorporate learnings from other BD2-selective series, optimize the vector for the amide region, and explore the ZA cleft, leading to the identification of potent, selective, and bioavailable compounds GSK452, GSK737, and GSK217. The experimental process involved the reaction of trans-4-Aminocyclohexanol(cas: 27489-62-9Application of 27489-62-9)

trans-4-Aminocyclohexanol(cas: 27489-62-9) belongs to anime. Reduction of nitro compounds, RNO2, by hydrogen or other reducing agents produces primary amines cleanly (i.e., without a mixture of products), but the method is mostly used for aromatic amines because of the limited availability of aliphatic nitro compounds. Reduction of nitriles and oximes (R2C=NOH) also yields primary amines.Application of 27489-62-9

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Sato, Masanori; Kondo, Takekazu; Kohno, Yasushi; Seto, Shigeki published their research in Bioorganic & Medicinal Chemistry in 2021. The article was titled 《Discovery of benzo[f]pyrido[4,3-b][1,4]oxazepin-10-one derivatives as orally available bromodomain and extra-terminal domain (BET) inhibitors with efficacy in an in vivo psoriatic animal model》.Electric Literature of C6H13NO The article contains the following contents:

Several compounds I (R1 = H, F; R2 = H, F, Cl, OMe; X = O, S) starting from previously reported pyrido-benzodiazepinone derivative II were designed and synthesized to enhance BRD4 inhibitory activity while avoiding hERG inhibition. Mol. docking studies and structure-activity relationship studies led to the identification of 9-fluorobenzo[f]pyrido[4,3-b][1,4]oxazepin-10-one derivative I (X = O; R1 = F; R2 = H), which exhibited potent BRD4 inhibitory activity with excellent potency in imiquimod-induced psoriasis model mice.trans-4-Aminocyclohexanol(cas: 27489-62-9Electric Literature of C6H13NO) was used in this study.

trans-4-Aminocyclohexanol(cas: 27489-62-9) belongs to anime. The reaction of alkyl halides, R―X, where X is a halogen, or analogous reagents with ammonia (or amines) is useful with certain compounds. Not all alkyl halides are effective reagents; the reaction is sluggish with secondary alkyl groups and fails with tertiary ones. Its usefulness is largely confined to primary alkyl halides (those having two hydrogen atoms on the reacting site).Electric Literature of C6H13NO

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Reference of trans-4-AminocyclohexanolIn 2017 ,《Synthesis of 4-Heteroaryl-Quinazoline Derivatives as Potential Anti-breast Cancer Agents》 appeared in Journal of Heterocyclic Chemistry. The author of the article were Kassab, A. E.; Gedawy, E. M.; El-Nassan, H. B.. The article conveys some information:

The 4-heteroaryl or heteroalkyl-quinazoline derivatives e.g., I were prepared as dual epidermal growth factor receptor (EGFR) and vascular endothelial growth factor receptor-2 (VEGFR-2) inhibitors. These compounds were tested for their dual enzyme inhibition as well as their cytotoxic activity on MCF7 cell line. The results indicated that almost all the compounds showed moderate dual inhibition of both enzymes. The compound methyl1-(6,7-dimethoxyquinazolin-4-yl)piperidine-4-carboxylate showed the highest inhibitory activity against both enzymes with IC50 97.6 and 64.0 μM against EGFR and VEGFR-2 kinases, resp. Most of the test compounds showed potent to moderate antitumor activity on MCF7 cell line. Some of the compounds showed potent cytotoxic activity with IC50 values between 10 and 17 M. The results came from multiple reactions, including the reaction of trans-4-Aminocyclohexanol(cas: 27489-62-9Reference of trans-4-Aminocyclohexanol)

trans-4-Aminocyclohexanol(cas: 27489-62-9) belongs to anime. Large quantities of aliphatic amines are made synthetically. The most widely used industrial method is the reaction of alcohols with ammonia at a high temperature, catalyzed by metals or metal oxide catalysts (e.g., nickel or copper). Mixtures of primary, secondary, and tertiary amines are thereby produced.Reference of trans-4-Aminocyclohexanol

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In 2017,Povedailo, V. A.; Stupak, A. P.; Tsybulsky, D. A.; Shmanai, V. V.; Yakovlev, D. L. published 《Fluorescence Quenching of Carboxyfluoresceins Conjugated Convalently to Oligonucleotides》.Journal of Applied Spectroscopy published the findings.Reference of trans-4-Aminocyclohexanol The information in the text is summarized as follows:

Dynamic and static quenching of 6-(2′,7′-dimethoxy-4′,5′-dichloro)carboxyfluorescein (JOE) by nucleosides (deoxyadenosine, deoxycytidine, deoxyguanosine, thymidine, and deoxyuridine) in Tris-acetate buffer solution was analyzed using the Stern-Volmer equation. Only one of the five nucleosides, deoxyguanosine, exhibited predominantly static quenching. The fluorescence quantum yields in buffer solution of 5- and 6-carboxyfluorescein (FAM) and 5-and 6-JOE bound covalently to the oligonucleotide by a rigid linker (4-trans-aminocyclohexanol) were greater than those of their analogs with a flexible linker (6-aminohexanol). It was shown that fluorescence quenching in systems with a flexible linker occurred mainly through van-der-Waals contact of the fluorophore with guanine. An increase in the number of consecutively located guanines in the oligonucleotides and their duplexes bound to the dye by a linker decreased the fluorescence quantum yield. Quantum-chem. calculations using the Gaussian 09 program provided an interpretation for the low-frequency shifts of 5-FAM and 5-JOE absorption and fluorescence spectra relative to those of the 6-isomers. In the experiment, the researchers used trans-4-Aminocyclohexanol(cas: 27489-62-9Reference of trans-4-Aminocyclohexanol)

trans-4-Aminocyclohexanol(cas: 27489-62-9) belongs to anime. Examples of direct uses of amines and their salts are as corrosion inhibitors in boilers and in lubricating oils (morpholine), as antioxidants for rubber and roofing asphalt (diarylamines), as stabilizers for cellulose nitrate explosives (diphenylamine), as protectants against damage from gamma radiation (diarylamines), as developers in photography (aromatic diamines), as flotation agents in mining, as anticling and waterproofing agents for textiles, as fabric softeners, in paper coating, and for solubilizing herbicides.Reference of trans-4-Aminocyclohexanol

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Mishra, Sanket J.; Liu, Weiya; Beebe, Kristin; Banerjee, Monimoy; Kent, Caitlin N.; Munthali, Vitumbiko; Koren, John III; Taylor, John A. III; Neckers, Leonard M.; Holzbeierlein, Jeffrey; Blagg, Brian S. J. published their research in Journal of Medicinal Chemistry in 2021. The article was titled 《The Development of Hsp90β-Selective Inhibitors to Overcome Detriments Associated with pan-Hsp90 Inhibition》.Related Products of 27489-62-9 The article contains the following contents:

The 90 kD heat shock proteins (Hsp90) are mol. chaperones that are responsible for the folding of select proteins, many of which are directly associated with cancer progression. Consequently, inhibition of the Hsp90 protein folding machinery results in a combinatorial attack on numerous oncogenic pathways. Seventeen small-mol. inhibitors of Hsp90 have entered clin. trials for the treatment of cancer, all of which bind the Hsp90 N-terminus and exhibit pan-inhibitory activity against all four Hsp90 isoforms, which may lead to adverse effects. The development of Hsp90 isoform-selective inhibitors represents an alternative approach toward the treatment of cancer and may limit some of these detriments. Described herein, is a structure-based approach to develop isoform-selective inhibitors of Hsp90β, which induces the degradation of select Hsp90 clients without concomitant induction of Hsp90 levels. Together, these initial studies support the development of Hsp90β-selective inhibitors as a method for overcoming the detriments associated with pan-inhibition. In the experimental materials used by the author, we found trans-4-Aminocyclohexanol(cas: 27489-62-9Related Products of 27489-62-9)

trans-4-Aminocyclohexanol(cas: 27489-62-9) belongs to anime. Acylation is one of the most important reactions of primary and secondary amines; a hydrogen atom is replaced by an acyl group (a group derived from an acid, such as RCOOH or RSO3H, by removal of ―OH, such as RC(=O)―, RS(O)2―, and so on). Reagents may be acid chlorides (RCOC1, RSO2C1), anhydrides ((RCO)2O), or even esters (RCOOR′); the products are amides of the corresponding acids.Related Products of 27489-62-9

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Electric Literature of C6H13NOIn 2021 ,《Fragment-based Scaffold Hopping: Identification of Potent, Selective, and Highly Soluble Bromo and Extra Terminal Domain (BET) Second Bromodomain (BD2) Inhibitors》 was published in Journal of Medicinal Chemistry. The article was written by Seal, Jonathan T.; Atkinson, Stephen J.; Bamborough, Paul; Bassil, Anna; Chung, Chun-wa; Foley, James; Gordon, Laurie; Grandi, Paola; Gray, James R. J.; Harrison, Lee A.; Kruger, Ryan G.; Matteo, Jeanne J.; McCabe, Michael T.; Messenger, Cassie; Mitchell, Darren; Phillipou, Alex; Preston, Alex; Prinjha, Rab K.; Rianjongdee, Francesco; Rioja, Inmaculada; Taylor, Simon; Wall, Ian D.; Watson, Robert J.; Woolven, James M.; Wyce, Anastasia; Zhang, Xi-Ping; Demont, Emmanuel H.. The article contains the following contents:

The profound efficacy of pan-BET inhibitors is well documented, but these epigenetic agents have shown pharmacol.-driven toxicity in oncol. clin. trials. The opportunity to identify inhibitors with an improved safety profile by selective targeting of a subset of the eight bromodomains of the BET family has triggered extensive medicinal chem. efforts. In this article, we disclose the identification of potent and selective drug-like pan-BD2 inhibitors such as pyrazole 23 (GSK809) and furan 24 (GSK743) that were derived from the pyrrole fragment 6. We transpose the key learnings from a previous pyridone series (GSK620 2 as a representative example) to this novel class of inhibitors, which are characterized by significantly improved solubility relative to our previous research. The experimental process involved the reaction of trans-4-Aminocyclohexanol(cas: 27489-62-9Electric Literature of C6H13NO)

trans-4-Aminocyclohexanol(cas: 27489-62-9) belongs to anime. Amine, any member of a family of nitrogen-containing organic compounds that is derived, either in principle or in practice, from ammonia (NH3). Naturally occurring amines include the alkaloids, which are present in certain plants; the catecholamine neurotransmitters (i.e., dopamine, epinephrine, and norepinephrine); and a local chemical mediator, histamine, that occurs in most animal tissues.Electric Literature of C6H13NO

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In 2019,European Journal of Medicinal Chemistry included an article by Feng, Yue; Xie, Xiao-Yang; Yang, Yi-Qiu; Sun, Yu-Tong; Ma, Wen-Hui; Zhou, Peng-Jun; Li, Zi-Yao; Liu, Hui-Qiang; Wang, Yi-Fei; Huang, Yun-Sheng. Electric Literature of C6H13NO. The article was titled 《Synthesis and evaluation of pyrimidoindole analogs in umbilical cord blood ex-vivo expansion》. The information in the text is summarized as follows:

The synthesis of pyrimidoindole analogs I [R = dimethylamino, 3-chloro-4-fluoroanilino, 3,4-dimethoxyphenthylamino, etc.] and II [R1 = anilino, morpholino, indole-3-ethylamino, etc.] and identified 6 compounds to be potent in promoting HSC ex vivo expansion. In particular, analog I [R = 2-(6,7-dimethoxy-1,2,3,4-trtrahydroisoquinolino)ethylamino (III)] was found to be the most effective in stimulating ex-vivo expansion of UCB CD34+ cells and CD34+CD38- cells. Initial data indicated that compound III promoted the absolute number of long term HSCs and inhibited their differentiation. UCB HSCs expanded with III retained adequate multi-lineage differentiation capacity. In addition, compound III was not cytotoxic at its test concentrations, suggested that it merits further investigation for potential clin. applications. In the experiment, the researchers used many compounds, for example, trans-4-Aminocyclohexanol(cas: 27489-62-9Electric Literature of C6H13NO)

trans-4-Aminocyclohexanol(cas: 27489-62-9) belongs to anime. Many important products require amines as part of their syntheses. Methylamine is utilized in the production of the analgesic meperidine (trade name Demerol) and the photographic developer Metol (trademark), and dimethylamine is used in the synthesis of the antihistamine diphenhydramine (trade name Benadryl), the solvent dimethylformamide (DMF), and the rocket propellant 1,1-dimethylhydrazine. The synthesis of the insect repellent N,N-diethyl-m-toluamide (DEET) incorporates diethylamine while that of the synthetic fibre Kevlar requires aromatic amines.Electric Literature of C6H13NO

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In 2018,Sandfort, Frederik; Strieth-Kalthoff, Felix; Klauck, Felix J. R.; James, Michael J.; Glorius, Frank published 《Deaminative Borylation of Aliphatic Amines Enabled by Visible Light Excitation of an Electron Donor-Acceptor Complex》.Chemistry – A European Journal published the findings.Safety of trans-4-Aminocyclohexanol The information in the text is summarized as follows:

A deaminative strategy for the borylation of aliphatic primary amines is described. Alkyl radicals derived from the single-electron reduction of redox-active pyridinium salts, which can be isolated or generated in situ, were borylated in a visible light-mediated reaction with bis(catecholato)diboron. No catalyst or further additives were required. The key electron donor-acceptor complex was characterized in detail by both exptl. and computational investigations. The synthetic potential of this mild protocol was demonstrated through the late-stage functionalization of natural products and drug mols. In the experimental materials used by the author, we found trans-4-Aminocyclohexanol(cas: 27489-62-9Safety of trans-4-Aminocyclohexanol)

trans-4-Aminocyclohexanol(cas: 27489-62-9) belongs to anime. Large quantities of aliphatic amines are made synthetically. The most widely used industrial method is the reaction of alcohols with ammonia at a high temperature, catalyzed by metals or metal oxide catalysts (e.g., nickel or copper). Mixtures of primary, secondary, and tertiary amines are thereby produced.Safety of trans-4-Aminocyclohexanol

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