Category: chlorides-buliding-blocks

Kumar, Praveen published the artcileAnticonvulsant and neurotoxicity evaluation of some novel 3-{[substituted]-amino}-2-phenyl-3H-quinazolin-4-one, Application of 4-(4-Chlorophenoxy)benzaldehyde, the main research area is anticonvulsant neurotoxicity aminophenylquinazolinone preparation structure activity.

Various 3-{[substituted]-amino}-2-phenyl-3H-quinazolin-4-one were synthesized and screened for anticonvulsant activity in maximal electroshock induced seizure (MES) and s.c. metrazol (scMET) induced seizure models in mice. The neurotoxicity was assessed using the Rotorod method. The 3-{[4-(4-Fluoro-phenoxy)-benzylidene]-amino}-2-phenyl-3H-quinazolin-4-one 7b and 3-{[4-(4-Chloro-3-methyl-phenoxy)-benzylidene]-amino}-2-phenyl-3H-quinazolin-4-one 7e emerged as the most promising compounds with anti-MES activity in mice i.p. All the compounds exhibited no neurotoxicity in Rotorod method.

International Journal of Pharmacology and Biological Sciences published new progress about Anticonvulsants. 61343-99-5 belongs to class chlorides-buliding-blocks, name is 4-(4-Chlorophenoxy)benzaldehyde, and the molecular formula is C13H9ClO2, Application of 4-(4-Chlorophenoxy)benzaldehyde.

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

Kohlmann, Anna published the artcileFragment Growing and Linking Lead to Novel Nanomolar Lactate Dehydrogenase Inhibitors, Formula: C7H6ClNO4, the main research area is preparation lactate dehydrogenase A inhibitor cancer.

Lactate dehydrogenase A (LDH-A) catalyzes the interconversion of lactate and pyruvate in the glycolysis pathway. Cancer cells rely heavily on glycolysis instead of oxidative phosphorylation to generate ATP, a phenomenon known as the Warburg effect. The inhibition of LDH-A by small mols. is therefore of interest for potential cancer treatments. We describe the identification and optimization of LDH-A inhibitors by fragment-based drug discovery. We applied ligand based NMR screening to identify low affinity fragments binding to LDH-A. The dissociation constants (Kd) and enzyme inhibition (IC50) of fragment hits were measured by surface plasmon resonance (SPR) and enzyme assays, resp. The binding modes of selected fragments were investigated by X-ray crystallog. Fragment growing and linking, followed by chem. optimization, resulted in nanomolar LDH-A inhibitors that demonstrated stoichiometric binding to LDH-A. Selected mols. inhibited lactate production in cells, suggesting target-specific inhibition in cancer cell lines.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 100959-51-1 belongs to class chlorides-buliding-blocks, name is 2-Chloro-5-methoxy-4-nitrophenol, and the molecular formula is C7H6ClNO4, Formula: C7H6ClNO4.

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

Nam, Nguyen-Hai published the artcileSynthesis, bioevaluation and docking study of 5-substituted phenyl-1,3,4-thiadiazole-based hydroxamic acids as histone deacetylase inhibitors and antitumor agents, Quality Control of 89978-31-4, the main research area is thiadiazole hydroxamic acid preparation histone deacetylase inhibitor antitumor; 5-phenyl-1,3,4-thiadiazole; cytotoxicity; heterocycle; histone deacetylase (HDAC) inhibitors.

Since the first histone deacetylase (HDAC) inhibitor (Zolinza, widely known as suberoylanilide hydroxamic acid; SAHA) was approved by the Food and Drug Administration for the treatment of T-cell lymphoma in 2006, the search for newer HDAC inhibitors has attracted a great deal of interest of medicinal chemists worldwide. As a continuity of the ongoing research in this area, the authors designed and synthesized a series of thiadiazole-based hydroxamic acids I [R = H, 2-Cl, 4-Me, etc.] as analogs of SAHA and evaluated their biol. activities. A number of compounds in this series, e.g. I [R = H], I [R = 2-Cl], I [R = 4-MeO], were found to possess potent anticancer cytotoxicity and HDAC inhibition effects. These compounds were generally two- to five-fold more potent in terms of cytotoxicity compared to SAHA against five cancer cell lines tested. Docking studies revealed that these hydroxamic acid displayed higher affinities than SAHA toward HDAC8.

Journal of Enzyme Inhibition and Medicinal Chemistry published new progress about Antitumor agents. 89978-31-4 belongs to class chlorides-buliding-blocks, name is 5-(2,6-Dichlorophenyl)-1,3,4-thiadiazol-2-amine, and the molecular formula is C8H5Cl2N3S, Quality Control of 89978-31-4.

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

Di Matteo, Mauro published the artcileSynthesis and biological characterization of 3-(imidazol-1-ylmethyl)piperidine sulfonamides as aromatase inhibitors, Category: chlorides-buliding-blocks, the main research area is imidazolylmethylpiperidine sulfonamide preparation aromatase inhibitor; Anticancer agents; Aromatase inhibitor; Imidazole; Sulfonamide; Synthesis.

The most frequently used treatment for hormone receptor pos. breast cancer in post-menopausal women are aromatase inhibitors. In order to develop new aromatase inhibitors, we designed and synthesized new imidazolylmethylpiperidine sulfonamides using the structure of the previously identified aromatase inhibitor SYN 20028567 as starting lead. By this approach, three new aromatase inhibitors with IC50 values that are similar to that of letrozole and SYN 20028567 were identified.

Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 7079-48-3 belongs to class chlorides-buliding-blocks, name is 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, and the molecular formula is C7H6ClFO2S, Category: chlorides-buliding-blocks.

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

Yan, Luping published the artcileStructure-Activity Relationships for the Marine Natural Product Sintokamides: Androgen Receptor N-Terminus Antagonists of Interest for Treatment of Metastatic Castration-Resistant Prostate Cancer, Application of Methyl 4,4,4-trichlorobutanoate, the main research area is marine sintokamide androgen receptor antagonist prostate cancer antitumor preparation.

Synthetic analogs of the marine natural product sintokamides have been prepared in order to investigate the structure-activity relationships for the androgen receptor N-terminal domain (AR NTD) antagonist activity of the sintokamide scaffold. An in vitro LNCaP cell-based transcriptional activity assay with an androgen-driven luciferase (Luc) reporter was used to monitor the potency of analogs. The data have shown that the chlorine atoms on the leucine side chains are essential for potent activity. Analogs missing the nonchlorinated Me groups of the leucine side chains (C-1 and C-17) are just as active and in some cases more active than the natural products. Analogs with the natural R configuration at C-10 and the unnatural R configuration at C-4 are most potent. Replacing the natural propionamide N-terminus cap with the more sterically hindered pivaloylamide N-terminus cap leads to enhanced potency. The tetramic acid fragment and the Me ether on the tetramic acid fragment are essential for activity. The SAR optimized analog 76 is more selective, easier to synthesize, more potent, and presumed to be more resistant to proteolysis than the natural sintokamides.

Journal of Natural Products published new progress about Antitumor agents. 19376-57-9 belongs to class chlorides-buliding-blocks, name is Methyl 4,4,4-trichlorobutanoate, and the molecular formula is C5H7Cl3O2, Application of Methyl 4,4,4-trichlorobutanoate.

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

Dickens, Michael P. published the artcile5-Deazaflavin derivatives as inhibitors of p53 ubiquitination by HDM2, Application In Synthesis of 93118-03-7, the main research area is deazaflavin derivative preparation p53 ubiquitination inhibitor SAR; Cancer; Deazaflavin; HDM2–p53; Ubiquitin E3 ligase; Ubiquitination inhibitors.

Based on previous reports of certain 5-deazaflavin derivatives being capable of activating the tumor suppressor p53 in cancer cells through inhibition of the p53-specific ubiquitin E3 ligase HDM2, we have conducted an structure-activity relation (SAR) anal. through systematic modification of the 5-deazaflavin template. This anal. shows that HDM2-inhibitory activity depends on a combination of factors. The most active compounds (e.g., I) contain a trifluoromethyl or chloro substituent at the deazaflavin C9 position and this activity depends to a large extent on the presence of at least one addnl. halogen or Me substituent of the Ph group at N10. Our SAR results, in combination with the HDM2 RING domain receptor recognition model we present, form the basis for the design of drug-like and potent activators of p53 for potential cancer therapy.

Bioorganic & Medicinal Chemistry published new progress about Antitumor agents. 93118-03-7 belongs to class chlorides-buliding-blocks, name is 2-Chloro-3-(trifluoromethyl)benzaldehyde, and the molecular formula is C8H4ClF3O, Application In Synthesis of 93118-03-7.

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

Peng, Zhenghong published the artcileDegrasyn-like symmetrical compounds: Possible therapeutic agents for multiple myeloma, Synthetic Route of 286474-59-7, the main research area is degrasyn analog preparation antitumor multiple myeloma; Degrasyn; Inhibitors; Jak2/Stat3; Multiple myeloma; Small molecules; Synthesis.

A series of degrasyn-like sym. compounds, e.g. I [R = indol-3-yl, 4-(piperidin-1-yl)phenyl, 6-methoxypyridin-2-yl, etc.] have been designed, synthesized, and screened against B cell malignancy (multiple myeloma, mantle cell lymphoma) cell lines. The lead compounds T5165804 and CP2005 showed higher nanomolar potency against these tumor cells in comparison to degrasyn and inhibited Usp9x activity in vitro and in intact cells. These observations suggest that this new class of compounds holds promise as cancer therapeutic agents.

Bioorganic & Medicinal Chemistry published new progress about Antitumor agents. 286474-59-7 belongs to class chlorides-buliding-blocks, name is 6-Chloro-2-fluoro-3-methylbenzaldehyde, and the molecular formula is C8H6ClFO, Synthetic Route of 286474-59-7.

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

Shono, Tatsuya published the artcileFormation of a reasonably stabilized trichloromethyl anion by the reaction of chloroform with electrogenerated base and its 1,4-addition to α,β-unsaturated carbonyl compounds, Recommanded Product: Methyl 4,4,4-trichlorobutanoate, the main research area is addition anion chloromethyl unsaturated carboxylate nitrile; ammonium tetraalkyl electrochem reduction pyrrolidinone; chloromethyl anion addition unsaturated carboxylate nitrile; carboxylate unsaturated addition chloromethyl anion; cyclopropanation chloroacetate anion; electrochem reduction pyrrolidinone tetraalkylammonium; nitrile unsaturated addition chloromethyl anion; pyrrolidinone reduction electrochem tetraalkylammonium; reduction electrochem pyrrolidinone tetraalkylammonium.

Electrochem. reduction of 2-pyrrolidinone in the presence of tetraalkylammonium salts gave the resp. tetraalkylammonium salts with pyrrolidinone. The latter reacted with CHCl3 to give Cl3C-, which underwent addition reactions with α,β-unsaturated carboxylates or nitriles. Thus, reaction of Cl2CHCO2Me in the presence of tetraalkylammonium salts with pyrrolidinone gave di-Me 1-chloro-1,2-cyclopropanedicarboxylates. Addition of CHCl3 to CH2:CHCO2Me in the presence of the tetraethylammonium-pyrrolidinone salt gave 87% Cl3CCH2CH2CO2Me.

Tetrahedron Letters published new progress about Addition reaction. 19376-57-9 belongs to class chlorides-buliding-blocks, name is Methyl 4,4,4-trichlorobutanoate, and the molecular formula is C5H7Cl3O2, Recommanded Product: Methyl 4,4,4-trichlorobutanoate.

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

Lee, Hyu Ji published the artcileIsoindol-1,3-dione and isoindol-1-one derivatives with high binding affinity to β-amyloid fibrils, HPLC of Formula: 99585-12-3, the main research area is isoindoledione derivative preparation amyloid fibril binding Alzheimer diagnostic probe; isoindolone derivative preparation amyloid fibril binding Alzheimer diagnostic probe; lactam aryl preparation amyloid fibril binding Alzheimer diagnostic probe; cyclic imide preparation amyloid fibril binding Alzheimer diagnostic probe.

Based on the structural features of Indoprofen and PIB, a series of isoindol-1,3-diones and isoindol-1-ones were designed and synthesized. These 23 compounds were evaluated by competitive binding assay against aggregated Aβ42 fibrils using [125I]TZDM. All the isoindolone derivatives showed very good binding affinities with Ki values in the subnanomolar range (0.42-0.94 nM). Among them, isoindol-1,3-diones (I, R1 = Br, R2 = Me2N, R3 = MeO; R1 = H, R2 = MeO, R3 = Me2N) and isoindol-1-ones (II, R4 = F, R5 = R7 = H, R6 = Me2N; R4 = H, R5 = Me, R6 = Me2N, R= MeO) exhibited excellent binding affinities (Ki = 0.42-0.44 and 0.46-0.49 nM), resp., than those of Indoprofen (Ki = 0.52 nM) and PIB (Ki = 0.70 nM). These results suggest that isoindolones could be served as a scaffold for potential AD diagnostic probes to monitor Aβ fibrils.

Bioorganic & Medicinal Chemistry Letters published new progress about Alzheimer disease. 99585-12-3 belongs to class chlorides-buliding-blocks, name is Methyl 4-chloro-2-methylbenzoate, and the molecular formula is C9H9ClO2, HPLC of Formula: 99585-12-3.

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

Huang, Hongbing published the artcileStructure- and property-based design of aminooxazoline xanthenes as selective, orally efficacious, and CNS penetrable BACE inhibitors for the treatment of Alzheimer’s disease, Related Products of chlorides-buliding-blocks, the main research area is aminooxazoline xanthene synthesis CNS penetrable antialzheimer agent structure activity; crystal structure aminooxazoline xanthene BACE beta secretase inhibitor pharmacokinetic; ketone demethylation methylation etherification acylation olefination cyclization Suzuki coupling.

A structure- and property-based drug design approach was employed to identify aminooxazoline xanthenes as potent and selective human β-secretase inhibitors. These compounds exhibited good isolated enzyme, cell potency, and selectivity against the structurally related aspartyl protease cathepsin D. Our efforts resulted in the identification of a potent, orally bioavailable CNS penetrant compound that exhibited in vivo efficacy. A single oral dose of compound (I) resulted in a significant reduction of CNS Aβ40 in naive rats.

Journal of Medicinal Chemistry published new progress about Alzheimer disease. 1072952-42-1 belongs to class chlorides-buliding-blocks, name is (5-Chloro-2-fluoro-4-methylphenyl)boronic acid, and the molecular formula is C7H7BClFO2, Related Products of chlorides-buliding-blocks.

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