Tag: 200-300

Yi, Xinzeyu; Cao, Zhi; Yuan, Ying; Li, Wen; Cui, Xinyue; Chen, Zilin; Hu, Xiang; Yu, Aixi published their research in Journal of Controlled Release in 2021. The article was titled 《Design and synthesis of a novel mitochondria-targeted osteosarcoma theranostic agent based on a PIM1 kinase inhibitor》.Electric Literature of C11H24N2O2 The article contains the following contents:

Osteosarcoma (OS) is the most common malignancy of the skeletal system, with a poor prognosis and high rate of recurrence. Adequate surgical margin and adjuvant chemotherapy improve the overall survival and limb salvage rate of osteosarcoma patients. Previous studies have showed that OS exhibits an increase in the expression of proviral integration site for Moloney murine leukemia virus 1 (PIM1) kinase, and high levels of PIM1 are also associated with poor OS prognosis and metastasis. We exploited the overexpression of proto-oncogenic PIM1 in OS toward the development of a novel near-IR imaging and targeted therapeutic agent, namely QCAi-Cy7d by conjugating a PIM1 small mol. inhibitor and heptamethine cyanine dye, for simultaneous guiding surgery and chemotherapy. QCAi-Cy7d showed targeted imaging and anticancer activities against OS in vitro and vivo without any obvious toxicity, and its antitumoral activity was much greater than the parent PIMI inhibitor. These results demonstrated the potential of new conjugate of PIM1 inhibitor and near-IR imaging, supporting structure-based design and development of theranostic agents for precise tumor imaging and targeted treatment. The experimental process involved the reaction of N-Boc-1,6-Diaminohexane(cas: 51857-17-1Electric Literature of C11H24N2O2)

N-Boc-1,6-Diaminohexane(cas: 51857-17-1) can be used as a linear hexyl spacer (C6-spacer) to synthesize biodegradable poly(disulfide amine)s for gene delivery, a multifunctional dendrimer for theranostics and so on.Electric Literature of C11H24N2O2

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

Chen, Zimin; Yuan, Weiming published their research in Chemistry – A European Journal in 2021. The article was titled 《N-Cyanation of Primary and Secondary Amines with Cyanobenziodoxolone (CBX) Reagent》.Synthetic Route of C12H15ClN2O2 The article contains the following contents:

An efficient electrophilic N-cyanation of amines e.g., pyrrolidine with a stable and less-toxic 1-cyano-1,2-benziodoxol-3-(1H)-one reagent towards the synthesis of cyanamides e.g., Pyrrolidine-1-carbonitrile was disclosed. This synthetically practicable strategy allows the construction of a wide variety of cyanamides under very mild and simple conditions with a broad functional group compatibility, and showcases a huge potential in late-stage modification of complex mols. In addition to this study using H-Trp-OMe.HCl, there are many other studies that have used H-Trp-OMe.HCl(cas: 7524-52-9Synthetic Route of C12H15ClN2O2) 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.Synthetic Route of C12H15ClN2O2

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

Yan, Guoyi; Zhong, Xinxin; Pu, Chunlan; Yue, Lin; Shan, Huifang; Lan, Suke; Zhou, Meng; Hou, Xueyan; Yang, Jie; Li, Deyu; Fan, Shilong; Li, Rui published their research in Journal of Medicinal Chemistry in 2021. The article was titled 《Targeting Cysteine Located Outside the Active Site: An Effective Strategy for Covalent ALKi Design》.Category: esters-buliding-blocks The article contains the following contents:

Potent inhibitors of ALK are highly desired because of the occurrence of drug resistance. We herein firstly report the development of a rationally designed inhibitor, Con B-1, which can covalently bind to Cys1259, a cysteine located outside the ALK active site by linking a warhead with Ceritinib through a 2,2′-Oxybis(ethylamine) linker. The in vitro and in vivo assays showed ConB-1 is a potent selective ALKi with low toxicity to normal cells. In addition, the mol. showed significant improvement of anticancer activities and potential antidrug resistant activity compared with Ceritinib, demonstrating the covalent inhibitor of ALK can be a promising drug candidate for the treatment of NSCLC. This work may provide a novel perspective on the design of covalent inhibitors. In the experiment, the researchers used N-Boc-1,6-Diaminohexane(cas: 51857-17-1Category: esters-buliding-blocks)

N-Boc-1,6-Diaminohexane(cas: 51857-17-1) can be used as a linear hexyl spacer (C6-spacer) to synthesize biodegradable poly(disulfide amine)s for gene delivery, a multifunctional dendrimer for theranostics and so on.Category: esters-buliding-blocks

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

In 2019,ACS Infectious Diseases included an article by Rey-Varela, Diego; Cisneros-Sureda, Javier; Balado, Miguel; Rodriguez, Jaime; Lemos, Manuel L.; Jimenez, Carlos. Computed Properties of C10H22N2O2. The article was titled 《The Outer Membrane Protein FstC of Aeromonas salmonicida subsp. salmonicida Acts as Receptor for Amonabactin Siderophores and Displays a Wide Ligand Plasticity. Structure-Activity Relationships of Synthetic Amonabactin Analogues》. The information in the text is summarized as follows:

Amonabactins are a group of four related catecholate siderophores produced by several species of the genus Aeromonas, including A. hydrophila and the fish pathogen A. salmonicida subsp. salmonicida. Although the gene cluster encoding amonabactin biosynthesis also contains a gene that could encode the ferri-siderophore receptor (fstC), to date there is no exptl. evidence to explain its role. In this work, we report the identification of the amonabactins’ outer membrane receptor and the determination of the minimal structural parts of these siderophores involved in the mol. recognition by their cognate receptor. The four natural amonabactin forms (P750, T789, P693, and T732) and some mono and biscatecholate amonabactin analogs were chem. synthesized, and their siderophore activity on A. salmonicida FstC(+) and FstC(-) strains was evaluated. The results showed that each amonabactin form has quite different growth promotion activity, with P750 and T789 the most active. The outer membrane receptor FstC recognizes more efficiently biscatecholate siderophores in which the length of the linker between the two iron-binding catecholamide units is 15 atoms (P750 and T789) instead of 12 atoms (P693 and T732). Anal. of the siderophore activity of synthetic analogs indicated that the presence of Phe or Trp residues is not required for siderophore recognition. The results together point toward evidence that the amonabactin receptor FstC admits a high degree of ligand plasticity. We also showed that FstC is present in most Aeromonas species, including relevant human and animal pathogens as A. hydrophila. From the results obtained, we concluded that the ferri-amonabactin uptake pathway involving the outer membrane transporter FstC possesses a considerable functional plasticity that could be exploited for delivery of antimicrobial compounds into the cell. This would allow the use of the siderophore-based iron uptake mechanisms to combat infections caused by species of the genus Aeromonas. 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

In 2018,Ma, Xiaoshen; Kucera, Roman; Goethe, Olivia F.; Murphy, Stephen K.; Herzon, Seth B. published 《Directed C-H Bond Oxidation of (+)-Pleuromutilin》.Journal of Organic Chemistry published the findings.Quality Control of tert-Butyl (5-aminopentyl)carbamate The information in the text is summarized as follows:

Antibiotics derived from the diterpene fungal metabolite (+)-pleuromutilin (1) are useful agents for the treatment Gram-pos. infections in humans and farm animals. Pleuromutilins elicit slow rates of resistance development and minimal cross-resistance with existing antibiotics. Despite efforts aimed at producing new derivatives by semisynthesis, modification of the tricyclic core is underexplored, in part due to a limited number of functional group handles. Herein, we report methods to selectively functionalize the Me groups of (+)-pleuromutilin (1) by hydroxyl-directed iridium-catalyzed C-H silylation, followed by Tamao-Fleming oxidation These reactions provided access to C16, C17, and C18 monooxidized products, as well as C15/C16 and C17/C18 dioxidized products. Four new functionalized derivatives were prepared from the protected C17 oxidation product. C6 carboxylic acid, aldehyde, and normethyl derivatives were prepared from the C16 oxidation product. Many of these sequences were executed on gram scales. The efficiency and practicality of these routes provides an easy method to rapidly interrogate structure-activity relationships that were previously beyond reach. This study will inform the design of fully synthetic approaches to novel pleuromutilins and underscores the power of the hydroxyl-directed iridium-catalyzed C-H silylation reaction. After reading the article, we found that the author 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 synthesis and anticancer activities of peptide 5-fluorouracil derivatives》 was written by Yan, Xiaowei; Hu, Maolin; Miao, Qian; Wang, Shun; Zhao, Kejian. Computed Properties of C10H14ClNO2 And the article was included in Journal of Chemical Research on April 30 ,2009. The article conveys some information:

A new series of peptide 5-fluorouracil derivatives was designed and synthesized in order to test in vitro anticancer activities. The results indicated that peptide 5-fluorouracil derivatives possessed anticancer activities against human HL-60 and Bel-7402 cell lines. The structures of the compounds were determined by means of 1H NMR, 13C NMR, IR, mass spectra and elemental analyses. The experimental part of the paper was very detailed, including the reaction process of H-Phg-OEt.HCl(cas: 59410-82-1Computed Properties of C10H14ClNO2)

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.Computed Properties of C10H14ClNO2 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

《Nucleophilic substitution of pentafluorobenzenes with imidazole》 was written by Fujii, Shozo; Maki, Yasuo; Kimoto, Hiroshi. Application of 4522-93-4 And the article was included in Journal of Fluorine Chemistry on April 30 ,1989. The article conveys some information:

The imidazole substitution of pentafluorobenzenes (C6F5R; R = CN, NO2, CO2Et, CHO, I, Br, Cl, H) occurred mainly at the para-position to R and corresponding 1-(4′-R-tetrafluorophenyl)imidazoles were obtained in good yields. The reactivity varied markedly with the substituents: nitro- or cyanopentafluorobenzene easily reacted at ambient temperature without any bases; however, methyl- or methoxypentafluorobenzene failed to react even at 100° in the presence of a strong base.Ethyl 2,3,4,5,6-pentafluorobenzoate(cas: 4522-93-4Application of 4522-93-4) was used in this study.

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. 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.Application of 4522-93-4

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

Formula: C11H24N2O2In 2020 ,《Regioselective SN2-Type Reaction for the Oriented and Irreversible Immobilization of Antibodies to a Glass Surface Assisted by Boronate Formation》 appeared in ACS Applied Bio Materials. The author of the article were Adak, Avijit K.; Huang, Kuan-Ting; Li, Pei-Jhen; Fan, Chen-Yo; Lin, Po-Chiao; Hwang, Kuo-Chu; Lin, Chun-Cheng. The article conveys some information:

Antibodies have exquisite specificities for mol. recognition, which led to their incorporation into array sensors that are crucial for research, diagnostic, and therapeutic applications. Many of these platforms rely heavily on surface-bound reactive groups to covalently tether antibodies to solid substrates; however, this strategy is hindered by a lack of orientation control over antibody immobilization. Here, the authors report a mild electrophilic phenylsulfonate (tosylate) ester-containing boronic acid affinity ligand for attaching antibodies to glass slides. A high level of antibody coupling located near the Fc region of the boronated antibody complex could be achieved by the proximal nucleophilic amino acid driven substitution reaction at the phenylsulfonate center. This enabled the full-length antibodies to be permanently tethered onto surfaces in an oriented manner. The advantages of this strategy were demonstrated through the individual and multiplex detection of protein and serum biomarkers. This strategy not only confers stability to the immobilized antibodies but also presents a different direction for the irreversible attachment of antibodies to solid supports in an orientation-controlled way. In the experiment, the researchers used N-Boc-1,6-Diaminohexane(cas: 51857-17-1Formula: C11H24N2O2)

N-Boc-1,6-Diaminohexane(cas: 51857-17-1) is used to prepare 1,3-Bis[6-(Boc-amino)hexyl]urea by reacting with carbonyl dichloride in the presence of triethylamine. Further, it is used as a reagent for the introduction of a C6-spacer.Formula: C11H24N2O2

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

Electric Literature of C10H22N2O2In 2018 ,《Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression》 appeared in Journal of Medicinal Chemistry. The author of the article were Zhou, Bing; Hu, Jiantao; Xu, Fuming; Chen, Zhuo; Bai, Longchuan; Fernandez-Salas, Ester; Lin, Mei; Liu, Liu; Yang, Chao-Yie; Zhao, Yujun; McEachern, Donna; Przybranowski, Sally; Wen, Bo; Sun, Duxin; Wang, Shaomeng. The article conveys some information:

The bromodomain and extra-terminal (BET) family proteins, consisting of BRD2, BRD3, BRD4, and testis-specific BRDT members, are epigenetic “”readers”” and play a key role in the regulation of gene transcription. BET proteins are considered to be attractive therapeutic targets for cancer and other human diseases. Recently, heterobifunctional small-mol. BET degraders have been designed based upon the proteolysis targeting chimera (PROTAC) concept to induce BET protein degradation Herein, we present our design, synthesis, and evaluation of a new class of PROTAC BET degraders. One of the most promising compounds, 23, effectively degrades BRD4 protein at concentrations as low as 30 pM in the RS4;11 leukemia cell line, achieves an IC50 value of 51 pM in inhibition of RS4;11 cell growth and induces rapid tumor regression in vivo against RS4;11 xenograft tumors. These data establish that compound 23 (BETd-260/ZBC260) is a highly potent and efficacious BET degrader.tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Electric Literature of 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).Electric Literature of C10H22N2O2

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

Chen, Yun; Ning, Yi; Bai, Gang; Tong, Linjiang; Zhang, Tao; Zhou, Jinpei; Zhang, Huibin; Xie, Hua; Ding, Jian; Duan, Wenhu published an article in 2021. The article was titled 《Design, Synthesis, and Biological Evaluation of IRAK4-Targeting PROTACs》, and you may find the article in ACS Medicinal Chemistry Letters.Application In Synthesis of tert-Butyl (5-aminopentyl)carbamate The information in the text is summarized as follows:

Interleukin-1 receptor associated kinase 4 (IRAK4) is a promising therapeutic target for diffuse large B-cell lymphoma driven by MYD88 L265P mutant, acting both as a kinase and a scaffolding protein for downstream signaling mols. While previous efforts to modulate IRAK4 activity with kinase inhibitors alone displayed moderate efficacy, protein degradation may offer a solution to blocking both IRAK4 kinase activity and scaffolding capabilities. To this end, the potent IRAK4 degrader 9 was discovered, and it effectively inhibited the activation of downstream NF-κB signaling and outperformed the parent compound 1. In addition, compound 9 displayed a substantial advantage in reduction of the viability of OCI-LY10 and TMD8 cells over the parent compound 1. These results underline the potential that eliminating both the kinase and scaffolding functions of IRAK4 may result in superior and broader efficacy than inhibiting the kinase activity alone. The experimental process involved the reaction of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Application In Synthesis 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).Application In Synthesis of tert-Butyl (5-aminopentyl)carbamate

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