Category: 55099-31-5

Zhang, Xuan published the artcileDiscovery of PROTAC BCL-XL degraders as potent anticancer agents with low on-target platelet toxicity, Related Products of bromides-buliding-blocks, the main research area is preparation PROTAC apoptosis BCLxL degrader cancer platelet toxicity; Apoptosis; BCL-X(L); Degradation; PROTAC; Platelet.

Anti-apoptotic protein BCL-XL plays a key role in tumorigenesis and cancer chemotherapy resistance, rendering it an attractive target for cancer treatment. However, BCL-XL inhibitors such as ABT-263 cannot be safely used in the clinic because platelets solely depend on BCL-XL to maintain their viability. To reduce the on-target platelet toxicity associated with the inhibition of BCL-XL, we designed and synthesized PROTAC BCL-XL degraders that recruit CRBN or VHL E3 ligase because both of these enzymes are poorly expressed in human platelets compared to various cancer cell lines. We confirmed that platelet-toxic BCL-XL/2 dual inhibitor ABT-263 can be converted into platelet-sparing CRBN/VHL-based BCL-XL specific degraders. A number of BCL-XL degraders are more potent in killing cancer cells than their parent compound ABT-263. Specifically, XZ739, a CRBN-dependent BCL-XL degrader, is 20-fold more potent than ABT-263 against MOLT-4 T-ALL cells and has >100-fold selectivity for MOLT-4 cells over human platelets. Our findings further demonstrated the utility of PROTAC technol. to achieve tissue selectivity through recruiting differentially expressed E3 ligases.

European Journal of Medicinal Chemistry published new progress about Antitumor agents (low). 55099-31-5 belongs to class bromides-buliding-blocks, name is Ethyl 10-bromodecanoate, and the molecular formula is C12H23BrO2, Related Products of bromides-buliding-blocks.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Murray, Michael published the artcileCarbon Chain Length Modulates MDA-MB-231 Breast Cancer Cell Killing Mechanisms by Mitochondrially Targeted Aryl-Urea Fatty Acids, Related Products of bromides-buliding-blocks, the main research area is aryl urea fatty acid preparation structure breast cancer mitochondrion; antitumor agents; apoptosis; breast cancer; fatty acids; lipid drugs.

Targeting the tumor cell mitochondrion could produce novel anticancer agents. We designed an aryl-urea fatty acid (1 g; 16({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)hexadecanoic acid) that disrupted the mitochondrion and decreased MDA-MB-231 breast cancer cell viability. To optimize the aryl-ureas the present study evaluated mitochondrial targeting by 1 g analogs containing alkyl chains between 10-17 carbons. Using the dye JC-1, the C12-C17 analogs efficiently disrupted the mitochondrial membrane potential (IC50s 3.5±1.2 to 7.6±1.1μM) and impaired ATP production; shorter analogs were less active. 7-Aminoactinomycin D/annexin V staining and flow cytometry showed that these agents activated the killing mechanisms of necrosis and apoptosis to varying extents (7-aminoactinomycin D/annexin V staining ratios 4.3-6.0). Indeed, 1 g and its C17 analog preferentially activated necrosis and apoptosis, resp. (ratios 2.1 and 16). Taken together, alkyl chain length is a determinant of mitochondrial targeting by aryl-ureas and can be varied to develop analogs that activate apoptosis or necrosis in a regulated fashion.

ChemMedChem published new progress about Antiproliferative agents. 55099-31-5 belongs to class bromides-buliding-blocks, name is Ethyl 10-bromodecanoate, and the molecular formula is C12H23BrO2, Related Products of bromides-buliding-blocks.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Strelyaeva, Angelina V. published the artcileThe study of external signs, microscopy and chemical composition of medicinal plant materials of Verinica beccabunga L. Herb, Quality Control of 55099-31-5, the main research area is external sign microscopy chem composition Verinica beccabunga.

Veronica beccabunga L. belongs to the class dicotyledons, order Lamiáles, family Scrophulariaceae. Representatives of the genus Veronica have long been used in folk medicine as antiinflammatory, antibacterial, antiseptic, wound healing, hemostatic, choleretic and antispasmodic drugs. Widely studied species are Veronica officinalis and Veronica chamaedrys. Veronica beccabunga L., which is the object of our study, remains a poorly studied plant. The study of external signs, microscopy and chem. composition of medicinal plant materials of Veronica beccabunga L. herb. Chromato-mass spectrometry was used in the work. When describing external signs and microscopy, diagnostic signs of Veronica beccabunga were revealed. 27 compounds were identified by chromatog.-mass spectrometry. The maximum content falls on: Citronellol epoxide (R or S) (30.5%), Linolenic acid, Et ester (15.18), Di-Et succinate (12.17%), Et palmitate (6.43%), Phytol (4.89%), Acetaldehyde Et amyl acetal (3.94%), Dibenzylamine (3.01%), Oleamide (2.77%), 2-(1-Methylbutyl)oxirane (2.7%), Bu octyl phthalate(1.7%), Et 10-bromodecanoate (1.68), Valeric acid, 4-methyl-, Et ester (1.58), Glycoside detected : 1-Benzyl-1H-benzimidazole 3-oxide (0.76%). The revealed morphol. and anatomical signs of Veronica beccabunga herb can be used to diagnose this species and develop authenticity indicators for promising medicinal herbs. 27 compounds were identified by chromatographymass spectrometry. Using the method of simple normalization, the relative percentage of identified compounds was determined

Pharmacognosy Journal published new progress about Anti-inflammatory agents. 55099-31-5 belongs to class bromides-buliding-blocks, name is Ethyl 10-bromodecanoate, and the molecular formula is C12H23BrO2, Quality Control of 55099-31-5.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Tron, Arnaud published the artcileReversible Photocapture of a [2]Rotaxane Harnessing a Barbiturate Template, COA of Formula: C12H23BrO2, the main research area is reversible photocapture rotaxane barbiturate template.

Photoirradiation of a hydrogen-bonded mol. complex comprising acyclic components, namely, a stoppered thread (1) with a central barbiturate motif and an optimized doubly anthracene-terminated acyclic Hamilton-like receptor (2b), leads to an interlocked architecture, which was isolated and fully characterized. The sole isolated interlocked photoproduct (Φ = 0.06) is a [2]rotaxane, with the dimerized anthracenes assuming a head-to-tail geometry, as evidenced by NMR spectroscopy and consistent with mol. simulation, physicochem., physicochem. (PM6). A different behavior was observed on irradiating homologous mol. complexes 1⊂2a, 1⊂2b, and 1⊂2c, where the spacers of 2a, 2b, and 2c incorporated 3, 6, and 9 methylene units, resp. While no evidence of interlocked structure formation was observed following irradiation of 1⊂2a, a kinetically labile rotaxane was obtained on irradiating the complex 1⊂2c, and ring slippage was revealed. A more stable [2]rotaxane was formed on irradiating 1⊂2b, whose capture is found to be fully reversible upon heating, thereby resetting the system, with some fatigue (38%) after four irradiation-thermal reversion cycles.

Journal of Organic Chemistry published new progress about [2+2] Photocycloaddition reaction. 55099-31-5 belongs to class bromides-buliding-blocks, name is Ethyl 10-bromodecanoate, and the molecular formula is C12H23BrO2, COA of Formula: C12H23BrO2.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Aimi, Takahiro published the artcileNucleophilic transformations of azido-containing carbonyl compounds via protection of the azido group, Related Products of bromides-buliding-blocks, the main research area is azido alc preparation; carbonyl compound azido nucleophile nucleophilic transformation.

Nucleophilic transformations of azido-containing carbonyl compounds, e.g., 4-(4-azidophenyl)benzaldehyde are discussed. The phosphazide formation from azides and di(tert-butyl)(4-(dimethylamino)phenyl)phosphine (Amphos) enabled transformations of carbonyl groups with nucleophiles such as lithium aluminum hydride and organometallic reagents RMgX (R = Et, Ph, 2-thienyl, etc.; X = Cl, Br). The good stability of the phosphazide moiety allowed to perform consecutive transformations of a diazide like 3-azido-5-(azidomethyl)benzaldehyde through triazole I formation and the Grignard reaction.

Chemical Communications (Cambridge, United Kingdom) published new progress about Alcohols Role: SPN (Synthetic Preparation), PREP (Preparation). 55099-31-5 belongs to class bromides-buliding-blocks, name is Ethyl 10-bromodecanoate, and the molecular formula is C12H23BrO2, Related Products of bromides-buliding-blocks.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Lalitha, R. published the artcilePhytochemical analysis of Scinaia bengalica by GCMS, COA of Formula: C12H23BrO2, the main research area is Scinaia marine extract phytochem GCMS.

Marine red algae consist of various medicinal activities. Marine sources are more active than the other natural sources. One of the most important red algae is Scinaia Bengalica (SB) known for its phytochem. anal. by GC-MS revealed 19 chem. constituents. SB consist major constituents like oleic acid, octanoic acid, 2 hexyl-1-octanol,hexadecanol, calcitriol, bromine compounds

International Journal of MediPharm Research published new progress about High resolution gas chromatography-high resolution mass spectrometry. 55099-31-5 belongs to class bromides-buliding-blocks, name is Ethyl 10-bromodecanoate, and the molecular formula is C12H23BrO2, COA of Formula: C12H23BrO2.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Zhai, Shiyang published the artcileDesign, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma, Formula: C12H23BrO2, the main research area is hepatocellular carcinoma mTOR HDAC1 antiproliferative drug deign mol docking; HDACs; Hepatocellular carcinoma; Hybrids; mTOR.

Hepatocellular carcinoma (HCC) is a major contributor to global cancer incidence and mortality. Many pathways are involved in the development of HCC and various proteins including mTOR and HDACs have been identified as potential drug targets for HCC treatment. In the present study, two series of novel hybrid mols. targeting mTOR and HDACs were designed and synthesized based on parent inhibitors (MLN0128 and PP121 for mTOR, SAHA for HDACs) by using a fusion-type mol. hybridization strategy. In vitro antiproliferative assays demonstrated that these novel hybrids with suitable linker lengths exhibited broad cytotoxicity against various cancer cell lines, with significant activity against HepG2 cells. Notably, DI06, an MLN0128-based hybrid, exhibited antiproliferative activity against HepG2 cells with an IC50 value of 1.61μM, which was comparable to those of both parent drugs (MLN0128, IC50 = 2.13μM and SAHA, IC50 = 2.26μM). In vitro enzyme inhibition assays indicated that DI06, DI07 and DI17 (PP121-based hybrid) exhibited nanomolar inhibitory activity against mTOR kinase and HDACs (e.g., HDAC1, HDAC2, HDAC3, HADC6 and HADC8). Cellular studies and western blot analyses uncovered that in HepG2 cells, DI06 and DI17 induced cell apoptosis by targeting mTOR and HDACs, blocked the cell cycle at the G0/G1 phase and suppressed cell migration. The potential binding modes of the hybrids (DI06 and DI17) with mTOR and HDACs were investigated by mol. docking. DI06 displayed better stability in rat liver microsomes than DI07 and DI17. Collectively, DI06 as a novel mTOR and HDACs inhibitor presented here warrants further investigation as a potential treatment of HCC.

European Journal of Medicinal Chemistry published new progress about Acetylation. 55099-31-5 belongs to class bromides-buliding-blocks, name is Ethyl 10-bromodecanoate, and the molecular formula is C12H23BrO2, Formula: C12H23BrO2.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary