Category: 35444-44-1

Broto, Marta; McCabe, Rita; Galve, Roger; Marco, M.-Pilar published an article in 2017, the title of the article was A high throughput immunoassay for the therapeutic drug monitoring of tegafur.Quality Control of Methyl 6-chloro-6-oxohexanoate And the article contains the following content:

Cancer is a group of diseases in which abnormal cells grow and divide without control, with the potential to invade other parts of the body. Chemotherapy is a type of treatment that uses chem. agents to treat cancer. These drugs are toxic and produce undesirable adverse drug reactions due to their narrow therapeutic window and highly variable pharmacokinetics, thus, they need to be monitored to establish personalized treatment to achieve maximal efficiency and reduce drug toxicity. Nowadays, therapeutic drug monitoring (TDM) is not routinely used for chemotherapy agents, however, TDM has the potential to improve the clin. benefit of chemotherapy drugs. Tegafur, a prodrug of 5-fluorouracil (5FU), is one of the main anti-cancer drugs used worldwide. Herein, a reproducible and sensitive indirect competitive ELISA has been developed and validated in plasma samples. The assay reports an IC50 of 35.6 nM, reaching a limit of detection of 2.7 nM. It is highly reproducible and does not show cross-reactivity with any related compound In summary, this assay provides a sensitive, accurate and high throughput anal. method for tegafur quantification in plasma, which fits TDM requirements. The experimental process involved the reaction of Methyl 6-chloro-6-oxohexanoate(cas: 35444-44-1).Quality Control of Methyl 6-chloro-6-oxohexanoate

The Article related to therapeutic drug monitoring tegafur determination blood elisa hapten preparation, Pharmacology: Methods and other aspects.Quality Control of Methyl 6-chloro-6-oxohexanoate

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Rozhon, Wilfried; Wang, Wuyan; Berthiller, Franz; Mayerhofer, Juliane; Chen, Tingting; Petutschnig, Elena; Sieberer, Tobias; Poppenberger, Brigitte; Jonak, Claudia published an article in 2014, the title of the article was Bikinin-like inhibitors targeting GSK3/Shaggy-like kinases: characterisation of novel compounds and elucidation of their catabolism in planta.Category: chlorides-buliding-blocks And the article contains the following content:

Background: Plant GSK-3/Shaggy-like kinases are key players in brassinosteroid (BR) signalling which impact on plant development and participate in response to wounding, pathogens and salt stress. Bikinin was previously identified in a chem. genetics screen as an inhibitor targeting these kinases. To dissect the structural elements crucial for inhibition of GSK-3/Shaggy-like kinases by bikinin and to isolate more potent compounds we synthesized a number of related substances and tested their inhibitory activity in vitro and in vivo using Arabidopsis thaliana. Results: A pyridine ring with an amido succinic acid residue in position 2 and a halogen in position 5 were crucial for inhibitory activity. The compound with an iodine substituent in position 5, denoted iodobikinin, was most active in inhibiting BIN2 activity in vitro and efficiently induced brassinosteroid-like responses in vivo. Its Me ester, methyliodobikinin, showed improved cell permeability, making it highly potent in vivo although it had lower activity in vitro. HPLC anal. revealed that the Me residue was rapidly cleaved off in planta liberating active iodobikinin. In addition, we provide evidence that iodobikinin and bikinin are inactivated in planta by conjugation with glutamic acid or malic acid and that the latter process is catalyzed by the malate transferase SNG1. Conclusion: Brassinosteroids participate in regulation of many aspects of plant development and in responses to environmental cues. Thus compounds modulating their action are valuable tools to study such processes and may be an interesting opportunity to modify plant growth and performance in horticulture and agronomy. Here we report the development of bikinin derivatives with increased potency that can activate BR signalling and mimic BR action. Methyliodobikinin was 3.4 times more active in vivo than bikinin. The main reason for the superior activity of methyliodobikinin, the most potent compound, is its enhanced plant tissue permeability. Inactivation of bikinin and its derivatives in planta involves SNG1, which constitutes a novel pathway for modification of xenobiotic compounds The experimental process involved the reaction of Methyl 6-chloro-6-oxohexanoate(cas: 35444-44-1).Category: chlorides-buliding-blocks

The Article related to arabidopsis iodobikinin bikinin sng1 catabolism malate transferase, Plant Biochemistry: Other and other aspects.Category: chlorides-buliding-blocks

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

On December 14, 2016, Li, Jinbo; Huang, Lei; Xiao, Xiao; Chen, Yingjie; Wang, Xingxing; Zhou, Zhengquan; Zhang, Chenyu; Zhang, Yan published an article.Computed Properties of 35444-44-1 The title of the article was Photoclickable MicroRNA for the Intracellular Target Identification of MicroRNAs. And the article contained the following:

MicroRNAs (miRNAs) are important gene regulators that bind with target genes and repress target gene expression at post-transcriptional level. The identification of target genes associated with miRNAs inside different cells is of major challenge in miRNA chem.-biol. due to lack of functional miRNAs bearing appropriate tags. Here we report photo-clickable miRNAs as appropriately pre-tagged miRNAs that keep the intracellular function of miRNAs and allow the addition of mol. handles through photo-click reaction. The photo-clickable miRNAs upon transfection inside cells were able to form functional complexes with target genes and repress target gene expression. Target genes associated with the photo-clickable miRNA in the complex were then tagged with the mol. handle through photo-click reaction for pull-down and identification. Using photo-clickable miR-106a, miR-27 and miR-122, we firstly verified that their intracellular function was comparable to intact miRNAs, which showed obvious advantage over corresponding biotinylated miRNAs. After attaching the biotin handle to the associated complex containing the photo-clickable miRNAs through the tetrazole-ene photo-click reaction, target genes previously bound with these miRNAs inside cells were successfully pulled town and analyzed. The application of this strategy was demonstrated by the identification of several new target genes of miR-122, followed by revealing a novel regulatory pathway in HepG2 cells with regard to the role of PEG10 in miR-122-promoted cell apoptosis. The experimental process involved the reaction of Methyl 6-chloro-6-oxohexanoate(cas: 35444-44-1).Computed Properties of 35444-44-1

The Article related to photoclickable microrna target gene identification hela hepg2, Biochemical Genetics: Methods and other aspects.Computed Properties of 35444-44-1

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Yamazoe, Sayumi; Shestopalov, Ilya A.; Provost, Elayne; Leach, Steven D.; Chen, James K. published an article in 2012, the title of the article was Cyclic caged morpholinos: conformationally gated probes of embryonic gene function.Category: chlorides-buliding-blocks And the article contains the following content:

Next-generation cyclic caged morpholino-based antisense oligonucleotides were used as effective reverse-genetics tools in zebrafish embryos to study the timing of exocrine fate commitment in developing pancreas. The zebrafish pancreas transcription factor 1 alpha (ptf1a) gene was targeted. The experimental process involved the reaction of Methyl 6-chloro-6-oxohexanoate(cas: 35444-44-1).Category: chlorides-buliding-blocks

The Article related to cyclic caged morpholino oligonucleotide zebrafish embryo pancreas exocrine fate, Biochemical Genetics: Methods and other aspects.Category: chlorides-buliding-blocks

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

On December 31, 2010, Denora, Nunzio; Laquintana, Valentino; Trapani, Adriana; Lopedota, Angela; Latrofa, Andrea; Gallo, James M.; Trapani, Giuseppe published an article.Quality Control of Methyl 6-chloro-6-oxohexanoate The title of the article was Translocator Protein (TSPO) Ligand-Ara-C (Cytarabine) Conjugates as a Strategy To Deliver Antineoplastic Drugs and To Enhance Drug Clinical Potential. And the article contained the following:

The aim of this work was to evaluate TSPO ligand-Ara-C conjugation as an approach for the selective delivery of the antineoplastic agent to brain tumors as well as for overcome P-gp resistance induction observed for the majority of cytotoxic agents, enhancing the drug clin. potential. To this end, novel N-imidazopyridinacetyl-Ara-C conjugates have been prepared and evaluated for their cytotoxicity against glioma cell lines. Conjugate (I) resulted stable in both phosphate buffer and physiol. medium. In all cases, the release of free Ara-C from hydrolyzed conjugates was checked by HPLC and ESI-MS anal. Conjugates (II) and I displayed very high in vitro TSPO affinity and selectivity, and, hence, they may possess potential for targeted brain delivery. Due to the favorable features displayed by the conjugate I, it was further evaluated on glioma cell lines, expressing high levels of TSPO, in the presence and in the absence of specific nucleoside transport (NT) inhibitors. In contrast to that observed for the free Ara-C, the presence of NT inhibitors did not reduce the cytotoxic activity of I. Moreover, conjugate I, as N4-acyl derivative of Ara-C, should be resistant to inactivation by cytidine deaminase, and it may possess enhanced propensity to target brain tumor cells characterized by a reduced expression of NTs. In addition, this conjugate behaves as a clear P-gp modulator and thereby may be useful to reverse MDR. Transport studies across the MDCKII-MDR1 monolayer indicated that conjugate I should overcome the BBB by transcellular pathway. All these features may be useful for enhancing the clin. potential of the nucleoside drug Ara-C. The experimental process involved the reaction of Methyl 6-chloro-6-oxohexanoate(cas: 35444-44-1).Quality Control of Methyl 6-chloro-6-oxohexanoate

The Article related to translocator protein ligand cytarabine conjugate antineoplastic resistance, Pharmaceuticals: Pharmaceutics and other aspects.Quality Control of Methyl 6-chloro-6-oxohexanoate

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

On December 20, 2013, Allen, C. Liana; Miller, Scott J. published an article.Computed Properties of 35444-44-1 The title of the article was Chiral Copper(II) Complex-Catalyzed Reactions of Partially Protected Carbohydrates. And the article contained the following:

Catalyst-controlled regioselective functionalization of partially protected saccharide mols. is a highly important yet under-developed area of carbohydrate chem. Such reactions allow for the reduction of protecting group manipulation steps required in syntheses involving sugars. Herein, an approach to these processes using enantiopure copper-bis(oxazoline) catalysts to control couplings of electrophiles to various partially protected sugars is reported. In a number of cases, divergent regioselectivity was observed as a function of the enantiomer of catalyst that is used. The experimental process involved the reaction of Methyl 6-chloro-6-oxohexanoate(cas: 35444-44-1).Computed Properties of 35444-44-1

The Article related to regioselective functionalization partially protected saccharide copper phbox catalyst, Carbohydrates: Oligosaccharides and other aspects.Computed Properties of 35444-44-1

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

On December 9, 2010, Bovens, Stefanie; Schulze Elfringhoff, Alwine; Kaptur, Martina; Reinhardt, Dirk; Schafers, Michael; Lehr, Matthias published an article.Application In Synthesis of Methyl 6-chloro-6-oxohexanoate The title of the article was 1-(5-Carboxyindol-1-yl)propan-2-one Inhibitors of Human Cytosolic Phospholipase A2α: Effect of Substituents in Position 3 of the Indole Scaffold on Inhibitory Potency, Metabolic Stability, Solubility, and Bioavailability. And the article contained the following:

Indole-5-carboxylic acids with 3-aryloxy-2-oxopropyl residues in position 1 have been found to be potent inhibitors of human cytosolic phospholipase A2α (cPLA2α). In the course of structure-activity relationship studies, we investigated the effect of a substitution of indole 3 position with acyl, alkyl, and oxadiazole residues. The highest increase of inhibitory potency could be achieved by a 3-methyl-1,2,4-oxadiazol-5-yl-moiety. Appropriate compound 40 revealed an IC50 of 0.0021 μM against isolated cPLA2α. In a cellular assay applying human platelets 40 blocked cPLA2α activity even with an IC50 of 0.0006 μM. Metabolic stability and aqueous solubility of the target compounds were also determined Furthermore, one selected compound was tested for peroral bioavailability in mice. The experimental process involved the reaction of Methyl 6-chloro-6-oxohexanoate(cas: 35444-44-1).Application In Synthesis of Methyl 6-chloro-6-oxohexanoate

The Article related to carboxyindolyl propanone inhibitor cpla preparation structure stability solubility bioavailability, Pharmacology: Structure-Activity and other aspects.Application In Synthesis of Methyl 6-chloro-6-oxohexanoate

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

On November 1, 2014, Yang, Wei; Li, Lixuan; Ji, Xun; Wu, Xiaowei; Su, Mingbo; Sheng, Li; Zang, Yi; Li, Jia; Liu, Hong published an article.Formula: C7H11ClO3 The title of the article was Design, synthesis and biological evaluation of 4-anilinothieno[2,3-d]pyrimidine-based hydroxamic acid derivatives as novel histone deacetylase inhibitors. And the article contained the following:

A series of 4-anilinothieno[2,3-d]pyrimidine-based hydroxamic acid derivatives as novel HDACs inhibitors were designed, synthesized and evaluated. Most of these compounds displayed good to excellent inhibitory activities against HDAC1, 3, 6. The IC50 values of compound 10r against HDAC1, HDAC3, HDAC6 was 1.14 ± 0.03 nM, 3.56 ± 0.08 nM, 11.43 ± 0.12 nM. Compound 10r noticeably up-regulated the level of histone H3 acetylation compared to the SAHA. Most of the compounds showed the strong anti-proliferative activity against human cancer cell lines including RMPI8226 and HCT-116. The IC50 values of Compounds 10r and 10t against RPMI8226 was 2.39 ± 0.20 μM, 1.41 ± 0.44 μM, resp., and the HCT-116 was sensitive to the compounds 10h, 10m, 10r, 10w with the IC50 values <1.9 μM. The experimental process involved the reaction of Methyl 6-chloro-6-oxohexanoate(cas: 35444-44-1).Formula: C7H11ClO3

The Article related to anilinothieno pyrimidine hydroxamate derivative preparation histone deacetylase inhibitor cancer, hdacs, hdacs inhibitor, hydroxamic acid, thieno[2,3-d]pyrimidines, Pharmacology: Structure-Activity and other aspects.Formula: C7H11ClO3

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

On February 28, 2011, Yamaoka, Nagahisa; Kodama, Hidehiko; Izuhara, Yuko; Miyata, Toshio; Meguro, Kanji published an article.COA of Formula: C7H11ClO3 The title of the article was Structure-activity relationships of new N-acylanthranilic acid derivatives as plasminogen activator inhibitor-1 inhibitors. And the article contained the following:

Novel anthranilic acid derivatives having substituted N-acyl side chains were designed and synthesized for evaluation as plasminogen activator inhibitor-1 (PAI-1) inhibitors. Compounds with a 4-diphenylmethyl-1-piperazinyl moiety on the acyl side chains in general exhibited potent in vitro PAI-1 inhibitory activity and good pharmacokinetic profiles after oral administration in rats. Compound TM5275 was identified as a promising candidate for further pharmacol. evaluation. The experimental process involved the reaction of Methyl 6-chloro-6-oxohexanoate(cas: 35444-44-1).COA of Formula: C7H11ClO3

The Article related to acylanthranilate derivative preparation pai 1 inhibitor structure activity pharmacokinetics, Pharmacology: Structure-Activity and other aspects.COA of Formula: C7H11ClO3

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Jeong, Yong-Chul; Anwar, Muhammad; Bikadi, Zsolt; Hazai, Eszter; Moloney, Mark G. published an article in 2013, the title of the article was Natural product inspired antibacterial tetramic acid libraries with dual enzyme inhibition.Synthetic Route of 35444-44-1 And the article contains the following content:

The application of natural product inspired synthesis has identified novel antibacterial tetramic acids which exhibit wide ranging antibacterial activity, and which provide potential lead structures for antibacterial drug discovery. Their phenotypic activity appears to correlate with action at two enzymes, UPPS and RNAP, which operate in independent metabolic pathways. SAR maps and identification of their relevant binding sites by mol. modeling has been achieved, and characterization of the most active compounds suggests that these systems offer potential for topical antibiotics but that for oral and injectable use further optimization is required. The experimental process involved the reaction of Methyl 6-chloro-6-oxohexanoate(cas: 35444-44-1).Synthetic Route of 35444-44-1

The Article related to natural product antibacterial tetramic acid upps rna polymerase haemophilus, Pharmacology: Structure-Activity and other aspects.Synthetic Route of 35444-44-1

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics