Tag: 200-300

D’yakonov, Vladimir A.; Tuktarova, Regina A.; Dzhemileva, Lilya U.; Ishmukhametova, Svetlana R.; Dzhemilev, Usein M. published an article in 2021. The article was titled 《Synthesis and anticancer activity of hybrid molecules based on lithocholic and (5Z,9Z)-tetradeca-5,9-dienedioic acids linked via mono(di,tri,tetra)ethylene glycol and α,ω-diaminoalkane units》, and you may find the article in Pharmaceuticals.Safety of N-Boc-1,6-Diaminohexane The information in the text is summarized as follows:

For first time, hybrid mols. were synthesized on basis of lithocholic and (5Z,9Z)-1,14-tetradeca-5,9-dienedicarboxylic acids, obtained in two stages using homo-cyclomagnesiation reaction of 2-(hepta-5,6-diene-1-yloxy)tetrahydro-2H-pyran at key stage. The resulting hybrid mols. containing 5Z,9Z-dienoic acids were of interest as novel synthetic biol. active precursors to create modern drugs for treatment of human oncol. diseases. The synthesized hybrid mols. were found to exhibit extremely high in vitro inhibitory activity against human topoisomerase I, which is 2-4 times higher than that of camptothecin, a known topoisomerase I inhibitor. Using flow cytometry and fluorescence microscopy, it was first shown that these new mols. are efficient apoptosis inducers in HeLa, U937, Jurkat, K562, and Hek293 cell cultures. In addition, results of investigations into effect of synthesized acids on mitochondria and studies of possible DNA damage in Jurkat tumor cells are also presented. In addition to this study using N-Boc-1,6-Diaminohexane, there are many other studies that have used N-Boc-1,6-Diaminohexane(cas: 51857-17-1Safety of N-Boc-1,6-Diaminohexane) was used in this study.

N-Boc-1,6-Diaminohexane(cas: 51857-17-1) is a compound useful in organic synthesis used in the preparation of mixed self-assembled monolayers (SAMs) that resist adsorption of proteins using the reaction of amines with a SAM that presents interchain carboxylic anhydride groupsSafety of N-Boc-1,6-Diaminohexane

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

《Synthesis and evaluation of novel peptidomimetics bearing p-aminobenzoic acid moiety as potential antidiabetic agents》 was written by Tang, Xue-Mei; Hu, Wen; Fan, Li; Wang, Hang; Tang, Min-Hui; Yang, Da-Cheng. Recommanded Product: 7524-52-9 And the article was included in Future Medicinal Chemistry in 2020. The article conveys some information:

Aim: Search for a new class of potential antidiabetic agents. Methodol.: A series of novel peptidomimetics bearing the p-aminobenzoic acid moiety (TM3-TM6) were designed and synthesized. For all synthetic target mols., the peroxisome proliferator response element (PPRE) activated activities have been evaluated and the toxicity were computed. Results & discussion: 46 new p-aminobenzoic acid derivatives have been characterized by 1H NMR, 13C NMR and high-resolution mass spectrometry (HRMS). The results of in vitro PPRE-activated activity, mol. docking study and toxicity prediction revealed that these compounds had potential antidiabetic activities and low toxicity. In particular compound 3b had up to 87% PPRE-activated activity compared with pioglitazone. This discovery may provide new insights for finding novel PPRE lead compoundH-Trp-OMe.HCl(cas: 7524-52-9Recommanded Product: 7524-52-9) 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.Recommanded Product: 7524-52-9

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

《Biotin-decorated all-HPMA polymeric micelles for paclitaxel delivery》 was published in Journal of Controlled Release in 2020. These research results belong to Wang, Yan; van Steenbergen, Mies J.; Beztsinna, Nataliia; Shi, Yang; Lammers, Twan; van Nostrum, Cornelus F.; Hennink, Wim E.. Reference of N-Boc-1,6-Diaminohexane The article mentions the following:

To avoid poly(ethylene glycol)-related issues of nanomedicines such as accelerated blood clearance, fully N-2-hydroxypropyl methacrylamide (HPMAm)-based polymeric micelles decorated with biotin for drug delivery were designed. To this end, a biotin-functionalized chain transfer agent (CTA), 4-cyano-4-[(dodecylsulfanylthiocarbonyl)-sulfanyl]pentanoic acid (biotin-CDTPA), was synthesized for reversible addition-fragmentation chain-transfer (RAFT) polymerization Amphiphilic poly(N-2-hydroxypropyl methacrylamide)-block-poly(N-2-benzoyloxypropyl methacrylamide) (p(HPMAm)-b-p(HPMAm-Bz)) with mol. weights ranging from 8 to 24 kDa were synthesized using CDTPA or biotin-CDTPA as CTA and 2,2′-azobis(2-methylpropionitrile) as initiator. The copolymers self-assembled in aqueous media into micelles with sizes of 40-90 nm which pos. correlated to the chain length of the hydrophobic block in the polymers, whereas the critical micelle concentrations decreased with increasing hydrophobic block length. The polymer with a mol. weight of 22.1 kDa was used to prepare paclitaxel-loaded micelles which had sizes between 61 and 70 nm, and a maximum loading capacity of around 10 wt%. A549 lung cancer cells overexpressing the biotin receptor, internalized the biotin-decorated micelles more efficiently than non-targeted micelles, while very low internalization of both types of micelles by HEK293 human embryonic kidney cells lacking the biotin receptor was observed As a consequence, the paclitaxel-loaded micelles with biotin decoration exhibited stronger cytotoxicity in A549 cells than non-targeted micelles. Overall, a synthetic pathway to obtain actively targeted poly(ethylene glycol)-free micelles fully based on a poly(HPMAm) backbone was established. These polymeric micelles are promising systems for the delivery of hydrophobic anticancer drugs. In the experiment, the researchers used N-Boc-1,6-Diaminohexane(cas: 51857-17-1Reference of N-Boc-1,6-Diaminohexane)

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.Reference of N-Boc-1,6-Diaminohexane

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

In 2017,Lv, Wei; Zhang, Guangming; Barinka, Cyril; Eubanks, James H.; Kozikowski, Alan P. published 《Design and Synthesis of Mercaptoacetamides as Potent, Selective, and Brain Permeable Histone Deacetylase 6 Inhibitors》.ACS Medicinal Chemistry Letters published the findings.Related Products of 51644-96-3 The information in the text is summarized as follows:

A series of non-hydroxamate HDAC6 inhibitors were prepared in our effort to develop potent and selective compounds for possible use in Central Nervous System (CNS) disorders, thus obviating the genotoxicity often associated with the hydroxamates. Halogens are incorporated in the cap groups of the designed mercaptoacetamides in order to increase brain accessibility. The indole analog and quinoline analog displayed potent HDAC6 inhibitory activity (IC50 11 nM and 2.8 nM) and excellent selectivity against HDAC1. Both compounds, together with their ester prodrug and disulfide prodrugs were found to be effective in promoting tubulin acetylation in HEK cells. The disulfide prodrugs also released a stable concentration of the indole and quinoline analogs upon microsomal incubation. Administration of disulfide prodrugs in vivo was found to trigger an increase of tubulin acetylation in mouse cortex. These results suggest that further exploration of these com-pounds for the treatment of CNS disorders is warranted. The experimental part of the paper was very detailed, including the reaction process 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

Name: H-Phg-OEt.HClOn March 1, 2017, Nishikawa, Yasuhiro; Nakamura, Hidetsugu; Ukai, Norimitsu; Adachi, Wakana; Hara, Osamu published an article in Tetrahedron Letters. The article was 《Tetraethylorthosilicate as a mild dehydrating reagent for the synthesis of N-formamides with formic acid》. The article mentions the following:

The synthesis of N-formamides with formic acid as a formyl source under mild conditions was achieved using tetraethylorthosilicate (TEOS), a low cost and environmentally benign reagent. The mild conditions in this system enable the formylation of a variety of amino acid derivatives including stereochem. labile phenylglycine Et ester with 96% ee. This new protocol could also be applied to simple amines including weakly basic aniline derivatives, giving various primary and secondary formamides. In the experimental materials used by the author, we found H-Phg-OEt.HCl(cas: 59410-82-1Name: H-Phg-OEt.HCl)

H-Phg-OEt.HCl(cas: 59410-82-1) belongs to esters. Esters are more polar than ethers but less polar than alcohols. Name: H-Phg-OEt.HCl They participate in hydrogen bonds as hydrogen-bond acceptors, but cannot act as hydrogen-bond donors, unlike their parent alcohols. This ability to participate in hydrogen bonding confers some water-solubility.

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

Recommanded Product: 169759-79-9On October 24, 2019 ,《One-pot synthesis of 2-substituted thieno[3,2-b]indoles from 3-aminothiophene-2-carboxylates through in situ generated 3-aminothiophenes》 was published in Tetrahedron Letters. The article was written by Irgashev, Roman A.; Steparuk, Alexander S.; Rusinov, Gennady L.. The article contains the following contents:

A convenient protocol for one-pot synthesis of thieno[3,2-b]indoles, bearing aromatic, thien-2-yl or styryl fragments at C-2 position, from easily accessible 5-substituted 3-aminothiophene-2-carboxylates using the Fischer indolization reaction was developed. Two main steps of this approach were the saponification of the starting 3-aminoesters with sodium hydroxide and next treatment of the crude 3-aminoacids sodium salts with arylhydrazines in glacial acetic acid solution The latter step included in-situ decarboxylation of the freed 3-aminothiophene-2-carboxylic acids to the 3-aminothiophenes and their acid promoted reaction with arylhydrazines to initially form arylhydrazones of 5-substituted thiophene-3(2H)-ones which smoothly cause indolization to afford the desired thieno[3,2-b]indoles. The experimental part of the paper was very detailed, including the reaction process of Methyl 4-amino-[2,2′-bithiophene]-5-carboxylate(cas: 169759-79-9Recommanded Product: 169759-79-9)

Methyl 4-amino-[2,2′-bithiophene]-5-carboxylate(cas: 169759-79-9) belongs to anime. To avoid the problem of multiple alkylation, methods have been devised for “blocking” substitution so that only one alkyl group is introduced. The Gabriel synthesis is one such method; it utilizes phthalimide, C6H4(CO)2NH, whose one acidic hydrogen atom has been removed upon the addition of a base such as KOH to form a salt.Recommanded Product: 169759-79-9

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

《A new precatalyst for the Suzuki reaction-a pyridyl-bridged dinuclear palladium complex as a source of mono-ligated palladium(0)》 was published in New Journal of Chemistry in 2004. These research results belong to Beeby, Andrew; Bettington, Sylvia; Fairlamb, Ian J. S.; Goeta, Andres E.; Kapdi, Anant R.; Niemelae, Elina H.; Thompson, Amber L.. Category: esters-buliding-blocks The article mentions the following:

A dinuclear pyridyl-bridged palladium complex, trans-(P,N)-[PdBr(μ-C5H4N-C2,N)(PPh3)]2 (I), was obtained from material isolated from the Suzuki cross-coupling reaction of 2-bromopyridine with 2,4-difluorophenylboronic acid in the presence of catalytic (PPh3)4Pd. I was an effective precatalyst for the Suzuki cross-coupling reactions of a variety organoboronic acids and aryl bromides, and represents a useful source of mono-ligated palladium(0), “”(Ph3P)Pd(0)””. In the experiment, the researchers used many compounds, for example, Methyl 4′-formyl-[1,1′-biphenyl]-2-carboxylate(cas: 144291-47-4Category: esters-buliding-blocks)

Methyl 4′-formyl-[1,1′-biphenyl]-2-carboxylate(cas: 144291-47-4) 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.Category: esters-buliding-blocks 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

Liu, Jin; Yuan, Lin; Ruan, Yong; Deng, Bulian; Yang, Zicao; Ren, Yichang; Li, Ling; Liu, Ting; Zhao, Huiting; Mai, Ruiyao; Chen, Jianjun published an article in 2022. The article was titled 《Novel CRBN-Recruiting Proteolysis-Targeting Chimeras as Degraders of Stimulator of Interferon Genes with In Vivo Anti-Inflammatory Efficacy》, and you may find the article in Journal of Medicinal Chemistry.Category: esters-buliding-blocks The information in the text is summarized as follows:

The activation of the cyclic GMP-AMP synthase-stimulator of interferon gene (STING) pathway has been associated with the pathogenesis of many autoimmune and inflammatory disorders, and small mols. targeting STING have emerged as a new therapeutic strategy for the treatment of these diseases. While several STING inhibitors have been identified with potent anti-inflammatory effects, we would like to explore STING degraders based on the proteolysis-targeting chimera (PROTAC) technol. as an alternative strategy to target the STING pathway. Thus, we designed and synthesized a series of STING protein degraders based on a small-mol. STING inhibitor (C-170) and pomalidomide (a CRBN ligand). These compounds demonstrated moderate STING-degrading activities. Among them, SP23 (I) achieved the highest degradation potency with a DC50 of 3.2μM. Importantly, SP23 exerted high anti-inflammatory efficacy in a cisplatin-induced acute kidney injury mouse model by modulating the STING signaling pathway. Taken together, SP23 represents the first PROTAC degrader of STING deserving further investigation as a new anti-inflammatory agent. 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: 51644-96-3Category: esters-buliding-blocks) 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).Category: esters-buliding-blocks

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

Lin, Xin; Tago, Kenji; Okazaki, Nozomi; So, Takanori; Takahashi, Kyoko; Mashino, Tadahiko; Tamura, Hiroomi; Funakoshi-Tago, Megumi published an article in 2021. The article was titled 《The indole-hydantoin derivative exhibits anti-inflammatory activity by preventing the transactivation of NF-κB through the inhibition of NF-κB p65 phosphorylation at Ser276》, and you may find the article in International Immunopharmacology.Synthetic Route of C12H15ClN2O2 The information in the text is summarized as follows:

Indole- and hydantoin-based derivatives both exhibit anti-inflammatory activity, suggesting that the structures of indole and hydantoin are functional for this activity. In the present study, we synthesized two types of indole-hydantoin derivatives, IH-1 (5-(1H-indole-3-ylmethylene) imidazolidine-2,4-dione) and IH-2 (5-(1H-indole-3-ylmethyl) imidazolidine-2,4-dione) and examined their effects on LPS-induced inflammatory responses in murine macrophage-like RAW264.7 cells. LPS-induced inflammatory responses were not affected by indole, hydantoin, or IH-2. In contrast, IH-1 significantly inhibited the LPS-induced production of nitric oxide (NO) and secretion of CCL2 and CXCL1 by suppressing the mRNA expression of inducible NO synthase (iNOS), CCL2, and CXCL1. IH-1 markedly inhibited the LPS-induced activation of NF-κB without affecting the degradation of IκBα or nuclear translocation of NF-κB. IH-1 markedly attenuated the transcriptional activity of NF-κB by suppressing the LPS-induced phosphorylation of the NF-κB p65 subunit at Ser276. Furthermore, IH-1 prevented the LPS-induced interaction of NF-κB p65 subunit with a transcriptional coactivator, cAMP response element-binding protein (CBP). Collectively, these results revealed the potential of the novel indole-hydantoin derivative, IH-1 as an anti-inflammatory drug. The experimental part of the paper was very detailed, including the reaction process of H-Trp-OMe.HCl(cas: 7524-52-9Synthetic Route of C12H15ClN2O2)

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

Yu, Ming-jun; Li, Chao; He, Meng; Zhu, Yu-ting; Yang, Rui; Deng, Sheng-song; Meng, Xiao-ming; Yao, Ri-sheng published their research in Medicinal Chemistry Research in 2021. The article was titled 《Structure-activity relationship studies on Pd176252 derivatives leading to discovery of novel GRP receptor antagonist with potent anticancer activity》.HPLC of Formula: 7524-52-9 The article contains the following contents:

Abstract: Gastrin-releasing peptide (GRP)/gastrin-releasing peptide receptor (GRPR) have various physiol. effects, and many studies report that GRPR is a potential anticancer target. Pd176252 is a typical small-mol. GRPR antagonist that exhibits anti-proliferation activity against most cancers. In this study, 31 novel Pd176252 analogs were designed, synthesized, and evaluated for anti-proliferation activity against human prostate cancer (PC3), mouse pancreatic cancer (Pan02), human gastric cancer (HGC-27), and hepatocellular carcinoma (HepG2) cell lines. Of all the compounds evaluated, 5a and 6e showed better anti-proliferation activity compared to Pd176252 against PC3 (half-maximal inhibitory concentration [IC50] = 4.97 and 9.88 μM, resp.), Pan02 (IC50 = 4.36 and 2.50 μM, resp.), and HGC-27 (IC50 = 4.36 and 2.50 μM, resp.), cell lines. Moreover, combining 5a or 6e with a histone deacetylase (HDAC) inhibitor further improved the in vitro anti-proliferation activity. Further research showed that 5a caused HGC-27 cell apoptosis by downregulating Bcl-2 and upregulating Bax. In addition, a mol. docking anal. showed that compounds 5a and 6e could bind to GRPR. In conclusion, compounds 5a and 6e are novel GRPR antagonists with potent anticancer activity. [graphic not available: see fulltext]H-Trp-OMe.HCl(cas: 7524-52-9HPLC of Formula: 7524-52-9) 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.HPLC of Formula: 7524-52-9

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