Tag: 200-300

《Discovery of selective CDK9 degraders with enhancing antiproliferative activity through PROTAC conversion》 was written by Qiu, Xiaqiu; Li, Yuanqing; Yu, Bin; Ren, Jie; Huang, Huidan; Wang, Min; Ding, Hong; Li, Zhiyu; Wang, Jubo; Bian, Jinlei. Application of 51644-96-3This research focused ontriazine pomalidomide cyclin dependent kinase apoptosis pharmacokinetic antiapoptotic antiproliferative; AML; Antitumor; CDK9; Degrader; PROTAC. The article conveys some information:

Cyclin-dependent kinase 9 (CDK9) is an increasingly important potential cancer treatment target. Nowadays, developing selective CDK9 inhibitors has been extremely challenging as its ATP-binding sites are similar with other CDKs. Here, we report that the CDK9 inhibitor BAY-1143572 is converted into a series of proteolysis targeting chimeras (PROTACs) which leads to several compounds inducing the degradation of CDK9 in acute myeloid leukemia cells at a low nanomolar concentration In addition, the most potent PROTAC mol. could inhibit cell growth more effectively than warhead alone, with little inhibition of other kinases. This enhanced antiproliferative activity is mediated by a slight increase in kinase inhibitory activity and an increase in the level of apoptosis induction. Moreover, the most potent PROTAC mol. could induce the degradation of CDK9 in vivo. Our work provides evidence that the most potent PROTAC mol. represents a lead for further development and that CDK9 degradation is a potential valuable therapeutic strategy in acute myeloid leukemia. 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: 51644-96-3Application of 51644-96-3) 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).Application of 51644-96-3

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

Computed Properties of C10H22N2O2In 2018 ,《Two-step activity-based protein profiling of diacylglycerol lipase》 appeared in Organic & Biomolecular Chemistry. The author of the article were van Rooden, Eva J.; Kreekel, Roy; Hansen, Thomas; Janssen, Antonius P. A.; van Esbroeck, Annelot C. M.; den Dulk, Hans; van den Berg, Richard J. B. H. N.; Codee, Jeroen D. C.; van der Stelt, Mario. The article conveys some information:

Diacylglycerol lipases (DAGL) produce the endocannabinoid 2-arachidonoylglycerol, a key modulator of neurotransmitter release. Chem. tools that visualize endogenous DAGL activity are desired. Here, we report the design, synthesis and application of a triazole urea probe for DAGL equipped with a norbornene as a biorthogonal handle. The activity and selectivity of the probe was assessed with activity-based protein profiling. This probe was potent against endogenous DAGLα (IC50 = 5 nM) and it was successfully applied as a two-step activity-based probe for labeling of DAGLα using an inverse electron-demand Diels-Alder ligation in living cells. The results came from multiple reactions, including the reaction of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Computed Properties 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).Computed Properties of C10H22N2O2

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

《Studies towards the Total Synthesis of Drimentine C. Preparation of the AB and CDEF Ring Fragments》 was published in European Journal of Organic Chemistry in 2020. These research results belong to Pound, Sarah M.; Underwood, Steven J.; Douglas, Christopher J.. Quality Control of H-Trp-OMe.HCl The article mentions the following:

The drimentine family is a class of hybrid isoprenoids derived from actinomycete bacteria. Members of this family display weak antitumor and antibacterial activity. Herein we report our efforts toward the total synthesis of drimentine C (I) using three distinct approaches incorporating palladium-catalyzed cyanoamidation, reductive cross-coupling, and photoredox-catalyzed α-alkylation of an aldehyde as key steps. Our synthetic efforts use a convergent synthesis to assemble the terpenoid and alkaloid portions of drimentine C from readily available L-tryptophan, L-proline, and (+)-sclareolide. The experimental process involved the reaction of H-Trp-OMe.HCl(cas: 7524-52-9Quality Control of H-Trp-OMe.HCl)

H-Trp-OMe.HCl(cas:7524-52-9) is one of amino acid derivatives. Amino acid derivatives represent an important category of skin penetration promoters. These compounds possess hydrophobic chains attached to an amino acid headgroup via a biodegradable ester bond. Due to the amphiphilic nature of these derivatives, it is possible for them to enter into the SC lipid barrier and significantly disorganize skin membrane lipids.Quality Control of H-Trp-OMe.HCl

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

《Copper-promoted N-arylation of the indole side chain of tryptophan using triarylbismuthines》 was published in European Journal of Organic Chemistry in 2020. These research results belong to Le Roch, Adrien; Chan, Hwai-Chien; Gagnon, Alexandre. Category: esters-buliding-blocks The article mentions the following:

A simple protocol for the regioselective N-arylation of the indole side chain of tryptophan using triarylbismuth reagents as the arylating agent is reported. The reaction is catalyzed by copper(II) acetate, and operates in the presence of triethylamine or pyridine under air at 50°C. This reaction allows the transfer of aryl groups bearing electron neutral, donating or withdrawing substituents at any position of the ring, shows high functional group tolerance, and retains the integrity of the stereogenic center. The protocol was utilized to N-arylate tryptophan-containing di- and tripeptides.H-Trp-OMe.HCl(cas: 7524-52-9Category: esters-buliding-blocks) was used in this study.

H-Trp-OMe.HCl(cas:7524-52-9) is one of amino acid derivatives. Amino acid derivatives represent an important category of skin penetration promoters. These compounds possess hydrophobic chains attached to an amino acid headgroup via a biodegradable ester bond. Due to the amphiphilic nature of these derivatives, it is possible for them to enter into the SC lipid barrier and significantly disorganize skin membrane lipids.Category: esters-buliding-blocks

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

《Design, synthesis and bio-evaluation of C-1 alkylated tetrahydro-β-carboline derivatives as novel antifungal lead compounds》 was published in Bioorganic & Medicinal Chemistry Letters in 2020. These research results belong to Singh, Rahul; Jaisingh, Aanchal; Maurya, Indresh K.; Salunke, Deepak B.. Product Details of 7524-52-9 The article mentions the following:

The field of antifungal agent has become static and development of resistance by the pathogen as well as limited clin. efficacy of marketed drugs demand the constant development of new antifungals. The presence of hydrocarbon chain of specific length linked with various different heterocycles was found to be an important structural feature in various antifungal lead compounds Based on the prominent antimicrobial activity of β-carboline derivatives, a set of C1 alkylated tetrahydro-β-carboline derivatives were proposed to be active against fungi. To validate and confirm the role of suitable alkyl chains linked to a β-carboline scaffold, few related analogs having C1 aryl substituents were also synthesized in one step via classic Pictet-Spengler reaction. The synthesized library was evaluated for its antifungal activity against C. albicans, C. krusei, C. parapsilosis, C. kefyr, C. glabrata, C. tropicalis and C. neoformans. One of the library members I, with n-alkyl chain of eight carbons exhibited potent antifungal activity against C. glabrata and C. kefyr. The lead compound, being selectively toxic also demonstrated prominent synergy enhancing the potency of antifungal drugs up to 10-fold. The time kill kinetic studies confirmed the efficacy of compound I, where the results obtained were comparable to that of Amp B. FE-SEM anal. revealed the increased asymmetry, disintegration and roughness of cell surface which could be because of the possible interaction of compound I at membrane level or interference in cell wall structure. Apoptosis/necrosis detection assay confirmed the significant apoptotic activity in C. glabrata cells after I treatment which was responsible for the rapid killing of C. glabrata cells. After reading the article, we found that the author used H-Trp-OMe.HCl(cas: 7524-52-9Product Details of 7524-52-9)

H-Trp-OMe.HCl(cas:7524-52-9) is one of amino acid derivatives. Amino acid derivatives represent an important category of skin penetration promoters. These compounds possess hydrophobic chains attached to an amino acid headgroup via a biodegradable ester bond. Due to the amphiphilic nature of these derivatives, it is possible for them to enter into the SC lipid barrier and significantly disorganize skin membrane lipids.Product Details of 7524-52-9

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

Solodukhin, Nikolai N.; Borisova, Nataliya E.; Churakov, Andrei V.; Zaitsev, Kirill V. published an article in Journal of Fluorine Chemistry. The title of the article was 《Substituted 4-(1H-1,2,3-triazol-1-yl)-tetrafluorobenzoates: Selective synthesis and structure》.Application of 4522-93-4 The author mentioned the following in the article:

Regioselective, simple and fast synthesis of a series of [2 + 3]-cycloaddition products I (R = Ph, CMe2OH, CH2OH, etc.) in reaction between Et 4-azido-2,3,5,6-tetrafluorobenzoate and a number of substituted alkynes was elaborated under conditions of copper-catalyzed click chem. reaction. The optimized conditions include application of CuBr and Et3N in dichloromethane. The mol. structure of compound I (R = Ph) in solid state was established by X-ray anal. After reading the article, we found that the author used Ethyl 2,3,4,5,6-pentafluorobenzoate(cas: 4522-93-4Application of 4522-93-4)

Ethyl 2,3,4,5,6-pentafluorobenzoate(cas: 4522-93-4) belongs to esters. They are important in biology, being one of the main classes of lipids and comprising the bulk of animal fats and vegetable oils.Application of 4522-93-4 They perform as high-grade solvents for a broad array of plastics, plasticizers, resins, and lacquers, and are one of the largest classes of synthetic lubricants on the commercial market.

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

Lu, Jingzhi; Khetrapal, Navneet S.; Johnson, Jacob A.; Zeng, Xiao Cheng; Zhang, Jian published their research in Journal of the American Chemical Society on December 14 ,2016. The article was titled 《”π-Hole-π” interaction promoted photocatalytic hydrodefluorination via inner-sphere electron transfer》.Quality Control of Ethyl 2,3,4,5,6-pentafluorobenzoate The article contains the following contents:

We describe a metal-free, photocatalytic hydrodefluorination (HDF) of polyfluoroarenes (FA) using pyrene-based photocatalysts (Py). The weak “”π-hole-π”” interaction between Py and FA promotes the electron transfer against unfavorable energetics (ΔGET up to 0.63 eV) and initiates the subsequent HDF. The steric hindrance of Py and FA largely dictates the HDF reaction rate, pointing to an inner-sphere electron transfer pathway. This work highlights the importance of the size and shape of the photocatalyst and the substrate in controlling the electron transfer mechanism and rates as well as the overall photocatalytic processes. The results came from multiple reactions, including the reaction of Ethyl 2,3,4,5,6-pentafluorobenzoate(cas: 4522-93-4Quality Control of Ethyl 2,3,4,5,6-pentafluorobenzoate)

Ethyl 2,3,4,5,6-pentafluorobenzoate(cas: 4522-93-4) belongs to esters. Esters are more polar than ethers but less polar than alcohols. They participate in hydrogen bonds as hydrogen-bond acceptors, but cannot act as hydrogen-bond donors, unlike their parent alcohols. Quality Control of Ethyl 2,3,4,5,6-pentafluorobenzoate

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

Larionov, S. V.; Myachina, L. I.; Sheludyakova, L. A.; Korolkov, I. V.; Rakhmanova, M. I.; Plyusnin, P. E.; Vinogradov, A. S.; Karpov, V. M.; Platonov, V. E.; Fadeeva, V. P. published an article in Russian Journal of General Chemistry. The title of the article was 《Synthesis of Octafluorobiphenyl-4,4′-dicarboxylic acid and photoluminescent compounds based thereon》.Application In Synthesis of Ethyl 2,3,4,5,6-pentafluorobenzoate The author mentioned the following in the article:

Octafluorobiphenyl-4,4′-dicarboxylic acid (H2L) and its complexes with Tb(III) and Eu(III) [Ln2(H2O)4(L)3·3H2O and Ln2(phen)2(L)3·2H2O] have been prepared; their structure has been elucidated from IR spectroscopy and X-ray diffraction anal. data. Thermal properties of the compounds have been studied. The complexes of Tb(III) and Eu(III) exhibit green and red photoluminescence, resp. The results came from multiple reactions, including the reaction of Ethyl 2,3,4,5,6-pentafluorobenzoate(cas: 4522-93-4Application In Synthesis of Ethyl 2,3,4,5,6-pentafluorobenzoate)

Ethyl 2,3,4,5,6-pentafluorobenzoate(cas: 4522-93-4) belongs to esters.Application In Synthesis of Ethyl 2,3,4,5,6-pentafluorobenzoate They are important in biology, being one of the main classes of lipids and comprising the bulk of animal fats and vegetable oils.Esters typically have a pleasant smell; those of low molecular weight are commonly used as fragrances and are found in essential oils and pheromones.

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

In 2001,European Journal of Mass Spectrometry included an article by Sawada, Masami; Takai, Yoshio; Imamura, Hiroyuki; Yamada, Hitoshi; Takahashi, Shigetoshi; Yamaoka, Hiroshi; Hirose, Keiji; Tobe, Yoshito; Tanaka, Jyuichi. HPLC of Formula: 59410-82-1. The article was titled 《Chiral recognizable host-guest interactions detected by fast-atom bombardment mass spectrometry: application to the enantiomeric excess determination of primary amines》. The information in the text is summarized as follows:

The enantiomeric excess (ee) of organic amine compounds was determined using fast-atom bombardment (FAB) mass spectrometry based on the chiral host-guest complexation systems. The method uses a 1:1 mixture of the given chiral crown ether hosts (HRRRR and HSSSS-do), one of whose enantiomers is isotopically labeled, for the ee-determination of a given amine salt guest (G+). The peak intensity ratio {I[(HRRRR+G)+]/I[(HSSSS-do+G)+] = IRIS} of the two diastereomeric host-guest complex ions clearly changes with the change in the ee of the guest. The intensity excess (Ie) of the two complex ion peaks is newly defined as Ie = (IRIS-1)/(IRIS+1). The two sets of mass spectrometrically obtained Ie values vs. a set of ee values of phenylalanine Me ester and leucine Me ester hydrochlorides show excellent linear relations through the zero point (R2 = 0.9989 and R2 = 0.9970, resp.). This indicates the potential utility of the present ee-determination method to within ± 3% ee. Also, based on the solution equilibrium distributions of the complex ions, the linearity is math. justified. Therefore, the ee-determination can be simplified as ee (%)=(|Ie|/|Ie(100)|)|100: here, Ie(100) is the corresponding Ie value obtained using an enantiomerically pure (100% ee) guest as a reference The present chiral dimethoxyphenyl crown ether host pairs employed are effective (IRIS ≃ 1.5) for the ee-determination of most α-amino acid esters, but not effective (IRIS ≃ 1.0) for most simple alkylamines. In the experimental materials used by the author, we found H-Phg-OEt.HCl(cas: 59410-82-1HPLC of Formula: 59410-82-1)

H-Phg-OEt.HCl(cas: 59410-82-1) belongs to esters. They are important in biology, being one of the main classes of lipids and comprising the bulk of animal fats and vegetable oils. They perform as high-grade solvents for a broad array of plastics, plasticizers, resins, and lacquers, and are one of the largest classes of synthetic lubricants on the commercial market.HPLC of Formula: 59410-82-1

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

Quality Control of H-D-Phe(4-NO2)-OMe.HClOn September 4, 2019 ,《Chiral Gating for Size- and Shape-Selective Asymmetric Catalysis》 was published in Journal of the American Chemical Society. The article was written by Li, Xiaowei; Zhao, Yan. The article contains the following contents:

A poor or mediocre stereoselectivity is a key roadblock for a chiral catalyst to find practical adoptions. We report a facile method to create a tunable chiral space near a chiral catalyst to augment its selectivity. The space was created rationally through templated polymerization within cross-linked micelles, using readily available amino acid derivatives It provided gated entrance of reactants to the catalyst, enabling a mediocre prolinamide to catalyze aldol condensation in water with excellent yields and ee, in a size- and shape-selective manner. In the part of experimental materials, we found many familiar compounds, such as H-D-Phe(4-NO2)-OMe.HCl(cas: 67877-95-6Quality Control of H-D-Phe(4-NO2)-OMe.HCl)

H-D-Phe(4-NO2)-OMe.HCl(cas: 67877-95-6) belongs to esters. Esters are more polar than ethers but less polar than alcohols. They participate in hydrogen bonds as hydrogen-bond acceptors, but cannot act as hydrogen-bond donors, unlike their parent alcohols. Quality Control of H-D-Phe(4-NO2)-OMe.HCl

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