Esters-buliding-blocks

Ugarenko, Michal published the artcileABT-737 overcomes Bcl-2 mediated resistance to doxorubicin-DNA adducts, Product Details of C10H18O4, the publication is Biochemical Pharmacology (2010), 79(3), 339-349, database is CAplus and MEDLINE.

Doxorubicin is an anthracycline anticancer agent that functions primarily by inhibiting topoisomerase II, but also forms covalent DNA adducts depending on the cellular availability of formaldehyde. The combination of formaldehyde-releasing prodrugs (such as AN-9) with doxorubicin has been shown to result in synergistic doxorubicin-DNA adduct formation and synergistic apoptosis in HL-60 leukemic cells, offering the potential for lower concentrations of doxorubicin to be used clin. to minimize side-effects. However, the overexpression of Bcl-2 confers resistance to doxorubicin/AN-9 DNA adduct forming treatments, thus limiting the therapeutic potential of this drug combination. The small mol. inhibitor, ABT-737, which binds to and inhibits Bcl-2, Bcl-xL and Bcl-w, was used in combination with doxorubicin/AN-9 treatments to overcome resistance to doxorubicin-DNA adducts in Bcl-2 overexpressing HL-60 cells (HL-60/Bcl-2). The combination treatment of doxorubicin and AN-9 (and all single agent controls) failed to induce an apoptotic response in HL-60/Bcl-2 cells, however, the addition of low nanomolar (sub-lethal) concentrations of ABT-737 was able to greatly increase apoptosis levels. Various control compounds were used to demonstrate that the mechanism of cell kill in response to the triple treatment’ (doxorubicin, AN-9 and ABT-737) is dependent on DNA adduct formation. Therefore, the ability of ABT-737 to inhibit Bcl-2 renders previously resistant HL-60 cancer cells highly sensitive to doxorubicin-DNA adducts, leading to a classical apoptotic response. In conclusion, the data obtained provides promising evidence that the anticancer activity of doxorubicin-DNA adducts can be substantially enhanced in Bcl-2 overexpressing cancers with the use of the small mol. Bcl-2 inhibitor, ABT-737.

Biochemical Pharmacology published new progress about 122110-53-6. 122110-53-6 belongs to esters-buliding-blocks, auxiliary class Aliphatic hydrocarbon chain,Ester,Inhibitor, name is (Pivaloyloxy)methyl butyrate, and the molecular formula is C12H10FeO4, Product Details of C10H18O4.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Tarasenko, Nataly published the artcileHistone deacetylase inhibitors: the anticancer, antimetastatic and antiangiogenic activities of AN-7 are superior to those of the clinically tested AN-9 (Pivanex), Product Details of C10H18O4, the publication is Clinical & Experimental Metastasis (2008), 25(7), 703-716, database is CAplus and MEDLINE.

Histone deacetylase inhibitory prodrugs that are metabolized to butyric acid and formaldehyde possess antineoplastic properties and low toxicity. We sought to characterize the antiangiogenic and antimetastatic activities of two lead prodrugs, pivaloyloxymethyl butyrate (AN-9) and butyroyloxymethyl-diethyl phosphate (AN-7) in murine cancer models. In the s.c. implanted human colon carcinoma HT-29 xenograft model AN-7, exhibited superior anticancer activity compared to AN-9, as was evident by the significantly greater inhibition of tumor growth and reduction of serum CEA. AN-7 was also more effective in reducing mean vessel d. (MVD) by 7-fold, bFGF, Ki-67 (7-fold) and HIF-1α in immunohistochem. stained tumor sections. Semi-quant. evaluation of the levels of bFGF, HDAC1 and HIF-1α by Western blot anal. showed a decrease in expression only in the tumors of mice treated with AN-7. The level of bFGF was reduced 3-fold in the tumor and that of TIMP1 was elevated (by 3-fold) in the serum of AN-7 treated mice. In a 4T1 metastatic breast carcinoma model, AN-7 inhibited the formation of lung lesions by 76% and AN-9 by 47%, further demonstrating the greater efficacy of AN-7 compared to AN-9 (P < 0.02). Both AN-7 and AN-9 exhibited antimetastatic and antiangiogenic activities by reducing vascularization, bFGF expression and HIF-1α. Yet, AN-7 was more potent than AN-9.

Clinical & Experimental Metastasis published new progress about 122110-53-6. 122110-53-6 belongs to esters-buliding-blocks, auxiliary class Aliphatic hydrocarbon chain,Ester,Inhibitor, name is (Pivaloyloxy)methyl butyrate, and the molecular formula is C17H18N3NaO3S, Product Details of C10H18O4.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Mansour, Oula C. published the artcileAn evaluation of the interaction of pixantrone with formaldehyde-releasing drugs in cancer cells, Synthetic Route of 122110-53-6, the publication is Cancer Chemotherapy and Pharmacology (2022), 89(6), 773-784, database is CAplus and MEDLINE.

Pixantrone is a synthetic aza-anthracenedione currently used in the treatment of non-Hodgkins lymphoma. The drug is firmly established as a poison of the nuclear enzyme topoisomerase II, however, pixantrone can also generate covalent drug-DNA adducts following activation by formaldehyde. While pixantrone-DNA adducts form proficiently in vitro, little evidence is presently at hand to indicate their existence within cells. The mol. nature of these lesions within cancer cells exposed to pixantrone and formaldehyde-releasing prodrugs was characterized along with the cellular responses to their formation. In vitro crosslinking assays, [14C] scintillation counting analyses and alk. comet assays were applied to characterize pixantrone-DNA adducts. Flow cytometry, cell growth inhibition and clonogenic assays were used to measure cancer cell kill and survival. Pixantrone-DNA adducts were not detectable in MCF-7 breast cancer cells exposed to [14C] pixantrone (10-40μM) alone, however the addition of the formaldehyde-releasing prodrug AN9 yielded readily measurable levels of the lesion at ∼ 1 adduct per 10 kb of genomic DNA. Co-administration with AN9 completely reversed topoisomerase II-associated DNA damage induction by pixantrone yet potentiated cell kill by the drug, suggesting that pixantrone-DNA adducts may promote a topoisomerase II-independent mechanism of cell death. Pixantrone-DNA adduct-forming treatments generally conferred mild synergism in multiple cell lines in various cell death and clonogenic assays, while pixantrone analogs either incapable or relatively defective in forming DNA adducts demonstrated antagonism when combined with AN9. The features unique to pixantrone-DNA adducts may be leveraged to enhance cancer cell kill and may be used to guide the design of pixantrone analogs that generate adducts with more favorable anticancer properties.

Cancer Chemotherapy and Pharmacology published new progress about 122110-53-6. 122110-53-6 belongs to esters-buliding-blocks, auxiliary class Aliphatic hydrocarbon chain,Ester,Inhibitor, name is (Pivaloyloxy)methyl butyrate, and the molecular formula is C10H18O4, Synthetic Route of 122110-53-6.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Cutts, Suzanne M. published the artcileFormaldehyde-releasing prodrugs in combination with adriamycin can overcome cellular drug resistance, Formula: C10H18O4, the publication is Oncology Research (2005), 15(4), 199-213, database is CAplus and MEDLINE.

The anticancer drug Adriamycin is widely used in cancer chemotherapy and is classified as a topoisomerase II inhibitor. However, in the presence of formaldehyde, Adriamycin also forms high levels of DNA adducts. In this study, a new series of butyric acid and formaldehyde-releasing drugs related to AN9 (pivaloyloxymethyl butyrate) was assessed for their ability to facilitate Adriamycin-DNA adduct formation in Adriamycin-sensitive and -resistant cell lines (HL60 and HL60/MX2; MES-SA and MES-SA/Dx5). Drugs that released two molar equivalents of formaldehyde per mol of prodrug were superior in their ability to enhance adduct formation compared to those that released one molar equivalent. Adduct formation (as assessed by binding of radiolabeled Adriamycin to genomic DNA) was always lower in the resistant cell lines compared to the sensitive cell lines. However, in growth inhibition experiments, prodrug combinations were able to overcome Adriamycin resistance to varying degrees, and the combination of Adriamycin with selected prodrugs that release two moles of formaldehyde totally overcame resistance in HL60/MX2 cells. These HL60-derived cells express altered levels of topoisomerase II and also express a mutant form of the enzyme. Combinations of Adriamycin with selected prodrugs that release one or two moles of formaldehyde partially overcame P-glycoprotein-mediated resistance in MES-SA/Dx5 cells. Formaldehyde-releasing prodrugs (as single agents) overcame both forms of resistance in the two resistant cell lines, demonstrating that they were not substrates of these resistance mechanisms. Collectively, these results suggest that changing the mechanism via which Adriamycin exerts its anticancer effect by dramatically increasing adduct levels (requiring coadministration of formaldehyde-releasing prodrugs) may be a useful means of cancer treatment, as well as for overcoming Adriamycin-induced resistance.

Oncology Research published new progress about 122110-53-6. 122110-53-6 belongs to esters-buliding-blocks, auxiliary class Aliphatic hydrocarbon chain,Ester,Inhibitor, name is (Pivaloyloxy)methyl butyrate, and the molecular formula is C10H18O4, Formula: C10H18O4.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Hoshino, Yasunobu published the artcileDysregulated B cell differentiation towards antibody-secreting cells in neuromyelitis optica spectrum disorder, Related Products of esters-buliding-blocks, the publication is Journal of Neuroinflammation (2022), 19(1), 6, database is CAplus and MEDLINE.

Anti-aquaporin 4 (AQP4) antibody (AQP4-Ab) is involved in the pathogenesis of neuromyelitis optica spectrum disorder (NMOSD). However, the mechanism involved in AQP4-Ab production remains unclear. We analyzed the immunophenotypes of patients with NMOSD and other neuroinflammatory diseases as well as healthy controls (HC) using flow cytometry. Transcriptome anal. of B cell subsets obtained from NMOSD patients and HCs was performed. The differentiation capacity of B cell subsets into antibody-secreting cells was analyzed. The frequencies of switched memory B (SMB) cells and plasmablasts were increased and that of naive B cells was decreased in NMOSD patients compared with relapsing-remitting multiple sclerosis patients and HC. SMB cells from NMOSD patients had an enhanced potential to differentiate into antibody-secreting cells when cocultured with T peripheral helper cells. Transcriptome anal. revealed that the profiles of B cell lineage transcription factors in NMOSD were skewed towards antibody-secreting cells and that IL-2 signaling was upregulated, particularly in naive B cells. Naive B cells expressing CD25, a receptor of IL-2, were increased in NMOSD patients and had a higher potential to differentiate into antibody-secreting cells, suggesting CD25+ naive B cells are committed to differentiate into antibody-secreting cells. To the best of our knowledge, this is the first study to demonstrate that B cells in NMOSD patients are abnormally skewed towards antibody-secreting cells at the transcriptome level during the early differentiation phase, and that IL-2 might participate in this pathogenic process. Our study indicates that CD25+ naive B cells are a novel candidate precursor of antibody-secreting cells in autoimmune diseases.

Journal of Neuroinflammation published new progress about 624-49-7. 624-49-7 belongs to esters-buliding-blocks, auxiliary class Inhibitor,Natural product, name is Dimethyl fumarate, and the molecular formula is C6H8O4, Related Products of esters-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Brear, Paul published the artcileNovel non-ATP competitive small molecules targeting the CK2 α/β interface, COA of Formula: C6H8O3, the publication is Bioorganic & Medicinal Chemistry (2018), 26(11), 3016-3020, database is CAplus and MEDLINE.

Increased CK2 levels are prevalent in many cancers. Combined with the critical role CK2 plays in many cell-signaling pathways, this makes it a prime target for down regulation to fight tumor growth. Herein, we report a fragment-based approach to inhibiting the interaction between CK2α and CK2β at the α-β interface of the holoenzyme. A fragment, CAM187, with an IC₅₀ of 44μM and a mol. weight of only 257gmol^-1 has been identified as the most promising compound Importantly, the lead fragment only bound at the interface and was not observed in the ATP binding site of the protein when co-crystallized with CK2α. The fragment-like mols. discovered in this study represent unique scaffolds to CK2 inhibition and leave room for further optimization.

Bioorganic & Medicinal Chemistry published new progress about 517-23-7. 517-23-7 belongs to esters-buliding-blocks, auxiliary class Tetrahydrofuran,Ketone,Ester, name is 3-Acetyldihydrofuran-2(3H)-one, and the molecular formula is C6H8O3, COA of Formula: C6H8O3.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Bailie, Alexandra E. published the artcileSynthesis of quinolone antibiotic analogues: a multistep synthetic chemistry experiment for undergraduates, Related Products of esters-buliding-blocks, the publication is Journal of Chemical Education (2021), 98(10), 3333-3340, database is CAplus.

A multistep synthesis of quinolone antibiotic analogs was developed as a laboratory experiment for intermediate/advanced undergraduate students. Students can synthesize a range of desfluoroenoxacin analogs via a five-step sequence. The experiment includes a range of key practical laboratory techniques including thin-layer chromatog. (TLC), liquid-liquid extraction, trituration, recrystallization and the characterization of compounds by IR and NMR spectroscopy. The experiment provides an opportunity for students to carry out fundamental organic chem. transformations from the curriculum such as the preparation of acyl chlorides, 1,4-conjugate addition-elimination, heterocycle synthesis, nucleophilic aromatic substitution and ester hydrolysis. The five-step sequence does not require column chromatog. and can be adapted to a range of laboratory settings.

Journal of Chemical Education published new progress about 924-99-2. 924-99-2 belongs to esters-buliding-blocks, auxiliary class Alkenyl,Amine,Aliphatic hydrocarbon chain,Ester, name is Ethyl 3-(dimethylamino)acrylate, and the molecular formula is C7H13NO2, Related Products of esters-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

RajanBabu, T. V. published the artcileHeterodimerization of Olefins. 1. Hydrovinylation Reactions of Olefins That Are Amenable to Asymmetric Catalysis, COA of Formula: C22H12F6O6S2, the publication is Journal of Organic Chemistry (2003), 68(22), 8431-8446, database is CAplus and MEDLINE.

Through a systematic examination of ligand and counterion effects, new protocols for a nearly quant. and highly selective codimerization of ethylene and various functionalized vinylarenes have been discovered. In a typical reaction, 4-bromostyrene and ethylene undergo codimerization in the presence of 0.0035 equiv each of [(allyl)NiBr]₂, triphenylphosphine, and AgOTf in CH₂Cl₂ at -56 °C to give 3-(4-bromophenyl)-1-butene in >98% yield and selectivity. Corresponding reactions with [(allyl)PdX]₂ are much less efficient and less selective and may require further optimization before a viable system can be identified. Another useful protocol that gives comparable yield and selectivity involves the use of a single-component catalyst prepared from allyl 2-diphenylphosphinobenzoate, Ni(COD)₂, and (C₆F₅)₃B. Recognition of a synergistic relationship between a chiral hemilabile ligand (for example, (R)-2-methoxy-2′-diphenylphosphino-1,1′-binaphthyl, MOP) and a highly dissociated counteranion (BARF or SbF₆) in an enantioselective version of the Ni-catalyzed reaction raises the prospects of developing a practical route for the synthesis of 3-arylbutenes. Several pharmaceutically relevant compounds, including widely used 2-arylpropionic acids, can be synthesized from these key intermediates. This reaction appears to be quite general. Synthesis of several new 2-diphenylphosphino-1,1-binaphthyl derivatives, prepared to probe the effect of hemilabile coordination on the efficiency and selectivity of the reaction, are also described.

Journal of Organic Chemistry published new progress about 126613-06-7. 126613-06-7 belongs to esters-buliding-blocks, auxiliary class Chiral Diphenols, name is (R)-[1,1′-Binaphthalene]-2,2′-diyl bis(trifluoromethanesulfonate), and the molecular formula is C22H12F6O6S2, COA of Formula: C22H12F6O6S2.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Caron, Aurore published the artcileNear-Infrared Photoinitiating Systems: Photothermal versus Triplet-Triplet Annihilation-Based Upconversion Polymerization, Computed Properties of 10287-53-3, the publication is Macromolecular Rapid Communications (2021), 42(11), 2100047, database is CAplus and MEDLINE.

NIR light-induced polymerization has attracted more and more attention in the photopolymerization field due to the possibility to use safer and more penetrating wavelengths, reducing the hazardousness. Here, a novel perspective for the free radical polymerization of acrylate-based monomers based on triplet-triplet annihilation upconversion (TTA-UC) is proposed, avoiding the introduction of heavy metals, usually required in the TTA processes. Thermal imaging experiments and Fourier transform IR spectroscopy are resp. used to record the temperature during NIR irradiation and measure the reactive function conversion. The competition between the TTA-UC and the NIR photothermal activation is investigated to compare the relative efficiency of both NIR processes. In view of the results obtained by the different methods, the photothermal effect seems to get the upper hand over the photoactivation of the system.

Macromolecular Rapid Communications published new progress about 10287-53-3. 10287-53-3 belongs to esters-buliding-blocks, auxiliary class Amine,Benzene,Ester, name is Ethyl 4-dimethylaminobenzoate, and the molecular formula is C11H15NO2, Computed Properties of 10287-53-3.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Borjigin, Timur published the artcileThe new LED-Sensitive photoinitiators of Polymerization: Copper complexes in free radical and cationic photoinitiating systems and application in 3D printing, Recommanded Product: Trimethylolpropane triacrylate, the publication is European Polymer Journal (2022), 110885, database is CAplus.

A ligand (A1) and four copper complexes (Cu1, Cu2, Cu3 and Cu4) were examined as photosensitizers in various photoinitiating systems (PISs). Interestingly, excellent photochem. reactivities were determined with the different compounds Especially, notable photoinitiation abilities were determined upon exposure to LED@405 nm during the free radical polymerization of acrylates and the cationic polymerization of epoxides when combined with an iodonium salt and an amine. With regards to their remarkable reactivities, the different photoinitiating systems were applied to 3D printing experiments By combining steady state photolysis and ESR spin trapping, the chem. mechanism supporting the polymerization processes could be fully detailed and proved. Among all PISs studied, the three-component PISs furnished the best monomer conversions during the free radical polymerization of trimethylolpropane triacrylate (TMPTA) and the cationic polymerization of (3,4-epoxycyclohexane)methyl 3,4-epoxycyclohexylcarboxylate (EPOX) monomers. The conversion process was monitored by real-time Fourier transform IR spectroscopy (RT-FTIR). Three-component PISs based on A1, Cu1 and Cu2 showed better performances than those based on Cu3, Cu4 and the different two-component PIS (comprising only the iodonium salt or the amine) in FRP experiments Based on the outstanding photoinitiation abilities of A1 and Cu1 with both TMPTA and EPOX, smooth and regular 3D patterns could be obtained by direct laser write experiments by generating interpenetrating polymer networks (IPN) with the blend of these two monomers.

European Polymer Journal published new progress about 15625-89-5. 15625-89-5 belongs to esters-buliding-blocks, auxiliary class Polymerization Reagents,Crosslinkers, name is Trimethylolpropane triacrylate, and the molecular formula is C15H20O6, Recommanded Product: Trimethylolpropane triacrylate.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics