Category: 51644-96-3

Product Details of 51644-96-3In 2020 ,《Discovery of novel small molecule induced selective degradation of the bromodomain and extra-terminal (BET) bromodomain protein BRD4 and BRD2 with cellular potencies》 appeared in Bioorganic & Medicinal Chemistry. The author of the article were Jiang, Fei; Wei, Qingyun; Li, Huili; Li, Hongmei; Cui, Yong; Ma, Yu; Chen, Haifang; Cao, Peng; Lu, Tao; Chen, Yadong. The article conveys some information:

The BET proteins BRD2, BRD3, and BRD4 play important roles in transcriptional regulation and can be degraded by proteolysis-targeting chimeras (PROTACs) for BET proteins. However, the lack of intra-BET proteins selectivity limits the scope of current degraders as probes for target validation and could lead to unwanted side effects or toxicity in a therapeutic setting. We describe herein the design, synthesis, and evaluation of PROTAC BET degraders, based on the BET inhibitor with selectivity for the first Bromodomain benzo[cd]indole-2-one, alkylamide linker and cereblon ligand thalidomide. Compound 15 potently and rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3, which not only effectively inhibits cell growth in human acute leukemia cell lines, but also very effective in inhibiting solid tumors with low cytotoxic effect in the cell profiles of NCI 60 cell lines. Remarkable dependency on linker length was observed for BRD4-degrading and c-Myc-driven antiproliferative activities in acute myeloid leukemia cell line MV4-11. The small-mol. 15 represents a novel, potent, and selective class of BRD4 and BRD2 degraders for the development of therapeutics to treat cancers. The results came from multiple reactions, including the reaction of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Product Details of 51644-96-3)

Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Product Details of 51644-96-3

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Synthetic Route of C10H22N2O2In 2021 ,《Synthesis and structure-activity relationships of 3,4,5-trisubstituted-1,2,4-triazoles: high affinity and selective somatostatin receptor-4 agonists for Alzheimer′s disease treatment》 was published in RSC Medicinal Chemistry. The article was written by Neumann, William L.; Sandoval, Karin E.; Mobayen, Shirin; Minaeian, Mahsa; Kukielski, Stephen G.; Srabony, Khush N.; Frare, Rafael; Slater, Olivia; Farr, Susan A.; Niehoff, Michael L.; Hospital, Audrey; Kontoyianni, Maria; Crider, A. Michael; Witt, Ken A.. The article contains the following contents:

Somatostatin receptor-4 (SST4) is highly expressed in brain regions affiliated with learning and memory. SST4 agonist treatment may act to mitigate Alzheimer′s disease (AD) pathol. An integrated approach to SST4 agonist lead optimization is presented herein. High affinity and selective agonists with biol. efficacy were identified through iterative cycles of a structure-based design strategy encompassing computational methods, chem., and preclin. pharmacol. 1,2,4-Triazole derivatives of our previously reported hit (4) showed enhanced SST4 binding affinity, activity, and selectivity. Thirty-five compounds showed low nanomolar range SST4 binding affinity, 12 having a Ki < 1 nM. These compounds showed >500-fold affinity for SST4 as compared to SST2A. SST4 activities were consistent with the resp. SST4 binding affinities (EC50 < 10 nM for 34 compounds). Compound 208 (SST4Ki = 0.7 nM; EC50 = 2.5 nM; >600-fold selectivity over SST2A) display a favorable physiochem. profile, and was advanced to learning and memory behavior evaluations in the senescence accelerated mouse-prone 8 model of AD-related cognitive decline. Chronic administration enhanced learning with i.p. dosing (1 mg kg-1) compared to vehicle. Chronic administration enhanced memory with both i.p. (0.01, 0.1, 1 mg kg-1) and oral (0.01, 10 mg kg-1) dosing compared to vehicle. This study identified a novel series of SST4 agonists with high affinity, selectivity, and biol. activity that may be useful in the treatment of AD. The experimental process involved the reaction of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Synthetic Route of C10H22N2O2)

Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Synthetic Route of C10H22N2O2

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Category: esters-buliding-blocksIn 2019 ,《Thienopyrimidinone Derivatives That Inhibit Bacterial tRNA (Guanine37-N1)-Methyltransferase (TrmD) by Restructuring the Active Site with a Tyrosine-Flipping Mechanism》 was published in Journal of Medicinal Chemistry. The article was written by Zhong, Wenhe; Pasunooti, Kalyan Kumar; Balamkundu, Seetharamsing; Wong, Yee Hwa; Nah, Qianhui; Gadi, Vinod; Gnanakalai, Shanmugavel; Chionh, Yok Hian; McBee, Megan E.; Gopal, Pooja; Lim, Siau Hoi; Olivier, Nelson; Buurman, Ed T.; Dick, Thomas; Liu, Chuan Fa; Lescar, Julien; Dedon, Peter C.. The article contains the following contents:

Among the >120 modified ribonucleosides in the prokaryotic epitranscriptome, many tRNA (tRNA) modifications are critical to bacterial survival, which makes their synthetic enzymes ideal targets for antibiotic development. Here we performed a structure-based design of inhibitors of tRNA-(N1G37) methyltransferase, TrmD, which is an essential enzyme in many bacterial pathogens. On the basis of crystal structures of TrmDs from Pseudomonas aeruginosa and Mycobacterium tuberculosis, we synthesized a series of thienopyrimidinone derivatives with nanomolar potency against TrmD in vitro and discovered a novel active site conformational change triggered by inhibitor binding. This tyrosine-flipping mechanism is unique found in P. aeruginosa TrmD and renders the enzyme inaccessible to the cofactor S-adenosyl-L-methionine (SAM) and probably to the substrate tRNA. Biophys. and biochem. structure-activity relationship studies provided insights into the mechanisms underlying the potency of thienopyrimidinones as TrmD inhibitors, with several derivatives found to be active against Gram-pos. and mycobacterial pathogens. These results lay a foundation for further development of TrmD inhibitors as antimicrobial agents. In the experiment, the researchers used tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Category: esters-buliding-blocks)

Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Category: esters-buliding-blocks

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

《Discovery of a Napabucasin PROTAC as an Effective Degrader of the E3 Ligase ZFP91》 was written by Hanafi, Maha; Chen, Xinde; Neamati, Nouri. Formula: C10H22N2O2This research focused ontumorigenesis oncogenic pathways PROTACs STAT3 E3 ligase cytotoxicity degrader. The article conveys some information:

Napabucasin, undergoing multiple clin. trials, was reported to inhibit the signal transducer and transcription factor 3 (STAT3). To better elucidate its mechanism of action, we designed a napabucasin-based proteolysis targeting chimera (PROTAC), XD2-149(I) that resulted in inhibition of STAT3 signaling in pancreatic cancer cell lines without inducing proteasome-dependent degradation of STAT3. Proteomics anal. of XD2-149 revealed the downregulation of the E3 ubiquitin-protein ligase ZFP91. XD2-149 degrades ZFP91 with DC50 values in the nanomolar range. The cytotoxicity of XD2-149 was significantly, but not fully, reduced with ZFP91 knockdown providing evidence for its multi-targeted mechanism of action. The NQO1 inhibitor, dicoumarol, rescued the cytotoxicity of XD2-149 but not ZFP91 degradation, suggesting that the NQO1-induced cell death is independent of ZFP91. ZFP91 plays a role in tumorigenesis and is involved in multiple oncogenic pathways including NF-κB and HIF-1α. In addition to this study using tert-Butyl (5-aminopentyl)carbamate, there are many other studies that have used tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Formula: C10H22N2O2) was used in this study.

Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Formula: C10H22N2O2

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

《Discovery of Novel PDEδ Degraders for the Treatment of KRAS Mutant Colorectal Cancer》 was published in Journal of Medicinal Chemistry in 2020. These research results belong to Cheng, Junfei; Li, Yu; Wang, Xu; Dong, Guoqiang; Sheng, Chunquan. Safety of tert-Butyl (5-aminopentyl)carbamate The article mentions the following:

KRAS-PDEδ protein-protein interaction represents an appealing target for cancer therapy. However, fast release of high-affinity inhibitors from PDEδ hampered drug binding affinity and antiproliferative activity. To overcome the limitations, the first proteolysis-targeting chimeric (PROTAC) small mols. targeting PDEδ were designed. By employment of PDEδ inhibitor deltazinone (2) and cereblon ligand pomalidomide (6), a series of potent PROTAC PDEδ degraders were obtained. The most promising compound 17f(I) efficiently induced PDEδ degradation and demonstrated significantly improved antiproliferative potency in KRAS mutant SW480 cells. Compound 17f also achieved significant tumor growth inhibition in the SW480 colorectal cancer xenograft model. This proof-of-concept study provided a new strategy to validate the druggability of KRAS-PDEδ interaction and offered an effective lead compound for the treatment of KRAS mutant cancer. In the part of experimental materials, we found many familiar compounds, such as tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Safety of tert-Butyl (5-aminopentyl)carbamate)

Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Safety of tert-Butyl (5-aminopentyl)carbamate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Name: tert-Butyl (5-aminopentyl)carbamateIn 2018 ,《Development of a Multiplexed Activity-Based Protein Profiling Assay to Evaluate Activity of Endocannabinoid Hydrolase Inhibitors》 appeared in ACS Chemical Biology. The author of the article were Janssen, Antonius P. A.; van der Vliet, Daan; Bakker, Alexander T.; Jiang, Ming; Grimm, Sebastian H.; Campiani, Giuseppe; Butini, Stefania; van der Stelt, Mario. The article conveys some information:

Endocannabinoids, an important class of signaling lipids involved in health and disease, are predominantly synthesized and metabolized by enzymes of the serine hydrolase superfamily. Activity-based protein profiling (ABPP) using fluorescent probes, such as fluorophosphonate (FP)-TAMRA and β-lactone-based MB064, enables drug discovery activities for serine hydrolases. FP-TAMRA and MB064 have distinct, albeit partially overlapping, target profiles but cannot be used in conjunction due to overlapping excitation/emission spectra. The authors therefore synthesized a novel FP-probe with a green BODIPY as a fluorescent tag and studied its labeling profile in mouse proteomes. Surprisingly, the authors found that the reporter tag plays an important role in the binding potency and selectivity of the probe. A multiplexed ABPP assay was developed in which a probe cocktail of FP-BODIPY and MB064 visualized most endocannabinoid serine hydrolases in mouse brain proteomes in a single experiment The multiplexed ABPP assay was employed to profile endocannabinoid hydrolase inhibitor activity and selectivity in the mouse brain. In addition to this study using tert-Butyl (5-aminopentyl)carbamate, there are many other studies that have used tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Name: tert-Butyl (5-aminopentyl)carbamate) was used in this study.

Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Name: tert-Butyl (5-aminopentyl)carbamate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Safety of tert-Butyl (5-aminopentyl)carbamateIn 2021 ,《New Pyrimidine and Pyridine Derivatives as Multitarget Cholinesterase Inhibitors: Design, Synthesis, and In Vitro and In Cellulo Evaluation》 appeared in ACS Chemical Neuroscience. The author of the article were Bortolami, Martina; Pandolfi, Fabiana; Tudino, Valeria; Messore, Antonella; Madia, Valentina Noemi; De Vita, Daniela; Di Santo, Roberto; Costi, Roberta; Romeo, Isabella; Alcaro, Stefano; Colone, Marisa; Stringaro, Annarita; Espargaro, Alba; Sabate, Raimon; Scipione, Luigi. The article conveys some information:

A new series of pyrimidine and pyridine diamines was designed as dual binding site inhibitors of cholinesterases (ChEs), characterized by two small aromatic moieties separated by a diaminoalkyl flexible linker. Many compounds are mixed or uncompetitive acetylcholinesterase (AChE) and/or butyrylcholinesterase (BChE) nanomolar inhibitors, with compound 9 being the most active on Electrophorus electricus AChE (EeAChE) (Ki = 0.312μM) and compound 22 on equine BChE (eqBChE) (Ki = 0.099μM). Mol. docking and mol. dynamic studies confirmed the interaction mode of our compounds with the enzymic active site. UV-vis spectroscopic studies showed that these compounds can form complexes with Cu2+ and Fe3+ and that compounds I, II, and III have antioxidant properties. Interestingly, some compounds were also able to reduce Aβ42 and tau aggregation, with compound IV being the most potent (22.3 and 17.0% inhibition at 100μM on Aβ42 and tau, resp.). Moreover, the most active compounds showed low cytotoxicity on a human brain cell line and they were predicted as BBB-permeable. In the experimental materials used by the author, we found tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Safety of tert-Butyl (5-aminopentyl)carbamate)

Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Safety of tert-Butyl (5-aminopentyl)carbamate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

In 2017,Larson, Peter; Kucaba, Tamara A.; Xiong, Zhengming; Olin, Michael; Griffith, Thomas S.; Ferguson, David M. published 《Design and Synthesis of N1-Modified Imidazoquinoline Agonists for Selective Activation of Toll-like Receptors 7 and 8》.ACS Medicinal Chemistry Letters published the findings.Name: tert-Butyl (5-aminopentyl)carbamate The information in the text is summarized as follows:

A series of N1-modified imidazoquinolines were synthesized and screened for Toll-like receptors (TLR) 7 and 8 activities to identify recognition elements that confer high affinity binding and selectivity. These receptors are key targets in the development of immunomodulatory agents that signal the NF-κB mediated transcription of pro-inflammatory chemokines and cytokines. Results are presented showing both TLR7/8 activations are highly correlated to N1-substitution, with TLR8 selectivity achieved through inclusion of an ethyl-, propyl-, or butylamino group at this position. While the structure-activity relationship anal. indicates TLR7 activity is less sensitive to N1-modification, extension of the aminoalkyl chain length to pentyl and p-methylbenzyl elicited high affinity TLR7 binding. Cytokine profiles are also reported that show the pure TLR8 agonist [4-amino-2-butyl-1-(2-aminoethyl)-7-methoxycarbonyl-1H-imidazo[4,5-c]quinoline] (I) induces higher levels of IL-1β, IL-12, and IFNγ when compared with TLR7 selective or mixed TLR7/8 agonists. The results are consistent with previous work suggesting TLR8 agonists are Th1 polarizing and may help promote cell-mediated immunity. The experimental process involved the reaction of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Name: tert-Butyl (5-aminopentyl)carbamate)

Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Name: tert-Butyl (5-aminopentyl)carbamate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

In 2019,Journal of Organic Chemistry included an article by Biallas, Phillip; Mensak, Tobias M.; Kunz, Kevin-Alexander; Kirsch, Stefan F.. Quality Control of tert-Butyl (5-aminopentyl)carbamate. The article was titled 《The Deazidoalkoxylation: Sequential Nucleophilic Substitutions with Diazidated Diethyl Malonate》. The information in the text is summarized as follows:

Diazidated malonamides derived from amines and diazidated di-Et malonate react with lithiated alcs. through nucleophilic substitution reactions where azide acts as an unconventional leaving group. This deazidoalkoxylation leads to the formal construction of N,O-acetals, and the remaining azide functionality is a useful entry point for further functionalizations through, for example, standard cycloaddition chem. Thus, the presented chem. provides an easy route toward densely functionalized mols.: amines, alcs., and alkynes can be attached onto the small malonate core unit in a sequential manner. Safety: potentially hazardous geminal diazides should be handled with care. In the experiment, the researchers used tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Quality Control of tert-Butyl (5-aminopentyl)carbamate)

Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Quality Control of tert-Butyl (5-aminopentyl)carbamate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

The author of 《Rethinking Hydrolytic Imidazoline Ring Expansion: A Common Approach to the Preparation of Medium-Sized Rings via Side-Chain Insertion into [1.4]Oxa- and [1.4]Thiazepinone Scaffolds》 were Reutskaya, Elena; Osipyan, Angelina; Sapegin, Alexander; Novikov, Alexander S.; Krasavin, Mikhail. And the article was published in Journal of Organic Chemistry in 2019. Related Products of 51644-96-3 The author mentioned the following in the article:

The previously reported ring-expansion strategy involving hydrolytically prone imidazoline rings was thought to include the formation of a hydrated imidazoline intermediate. In this work, we accessed the latter via the addition of a 2-aminoethyl side chain onto a lactam moiety. This led to an efficient three-atom ring expansion of diarene-fused [1.4]oxazepines and [1.4]thiazepines and led us to propose to term this common approach the hydrated imidazoline ring expansion (HIRE) reaction. The strategy was extended to the insertion of longer (containing up to five atoms) side chains, and thus, larger (11- to 12-membered) diarene-fused rings were obtained via the homo-HIRE and homo2-HIRE reactions, resp. This underscores the utility of the HIRE reaction for the preparation of medium-sized rings, an important class of chem. tools for interrogation of various biol. targets. The experimental process involved the reaction of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Related Products of 51644-96-3)

Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Related Products of 51644-96-3

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics