Tag: M.W=150-200

Ai, Liankun published the artcileCopper-mediated construction of benzothieno[3,2-b]benzofurans by intramolecular dehydrogenative C-O coupling reaction, Category: chlorides-buliding-blocks, the publication is RSC Advances (2021), 11(57), 36305-36309, database is CAplus and MEDLINE.

An efficient method to synthesize benzothieno[3,2-b]benzofurans such as I [R = H, 3-Cl, 3-t-Bu; R¹ = H, 7,8-di-F, 8-Me, etc.] via intramol. dehydrogenative C-H/O-H coupling had been developed. Good to excellent yields (64-91%) could be obtained no matter if the substituted group was electron-donating or electron-withdrawing. Notably, three-to-six fused ring thienofuran compounds I could be constructed using this method. A reaction mechanism study showed that 1,1-diphenylethylene could be completely inhibited the reaction. Therefore, it was a radical pathway initiated by single electron transfer between the hydroxyl of the substrate and the copper catalyst.

RSC Advances published new progress about 1238196-66-1. 1238196-66-1 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Phenol,Boronic Acids,Boronic acid and ester, name is 4-Chloro-2-hydroxyphenylboronic acid, and the molecular formula is C6H6BClO3, Category: chlorides-buliding-blocks.

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

Yamamoto, Takeshi published the artcileHighly enantioselective synthesis of axially chiral biarylphosphonates: asymmetric Suzuki-Miyaura coupling using high-molecular-weight, helically chiral polyquinoxaline-based phosphines, Name: 4-Chloro-2-methylphenylboronic acid, the publication is Angewandte Chemie, International Edition (2011), 50(38), 8844-8847, S8844/1-S8844/74, database is CAplus and MEDLINE.

Axially-chiral 1-arylnaphthalene-2-phosphonates [(S)-3, aryl = 2-MeC₆H₄, 1-naphthyl, 4-MeO-2-MeC₆H₃, 2,3-Me₂C₆H₃, 2,5-Me₂C₆H₃, 4-Cl-2-MeC₆H₃] were prepared by Suzuki-Miyaura coupling of arylboronic acids with dialkyl 1-bromonaphthalene-2-phosphonates (alkyl = Me, Et), catalyzed by palladium complexes with helically-chiral polyquinoxaline phosphines. The 20-mer helically-chiral polyquinoxaline block 10-1-10 copolymers (L^1a-L^1d), containing the 5-arylphosphino group and bearing chiral (R)-2-butoxy auxiliaries were prepared by polymerization of 10 equiv of 4,5-di-(R)-sec-butoxymethyl-3,6-dimethyl-1,2-benzenediisocyanide [(R)-1], reaction with 1 equiv of 2,3-diisocyano-4-methyl-2′-diarylphosphinyl-1,1′-biphenyl [aryl = Ph, 3,5-Me₂C₆H₃, 4-MeC₆H₄, 3,5-(CF₃)₂C₆H₃], and again with 10 equiv of (R)-1, initiated by chiral palladium imidazolidinylphenylquinoxaline complex with subsequent HSiCl₃ reduction Analogous 950/50 polyphosphine copolymers (L^2a-L^2d) were prepared by copolymerization of (R)-1 with 2,3-diisocyano-4-methyl-2′-diarylthiophosphinyl-1,1′-biphenyl, catalyzed by achiral nickel complex [Ni(o-Tol)Cl(PMe₃)₂] and reduction The Suzuki-Miyaura coupling reactions were performed in the presence of 1 mol% of [PdCl(π-allyl)]₂ and 2 mol% of the helical ligands L¹ and L², yielding the phosphonates (S)-3 with 56-93% yields and 78-98% ee.

Angewandte Chemie, International Edition published new progress about 209919-30-2. 209919-30-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Boronic Acids,Boronic acid and ester, name is 4-Chloro-2-methylphenylboronic acid, and the molecular formula is C13H9ClN2O4, Name: 4-Chloro-2-methylphenylboronic acid.

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

Alsharif, Zakeyah A. published the artcileModular synthesis of thiazoline and thiazole derivatives by using a cascade protocol, Recommanded Product: 1-(4-Chlorophenyl)thiourea, the publication is RSC Advances (2017), 7(52), 32647-32651, database is CAplus and MEDLINE.

The first synthetic protocol by which both thiazolines I (R = Me, allylamino, pyridin-2-yl, (E)-2-[(4-chlorophenyl)methylidene]hydrazin-1-yl, etc.) and thiazoles II [R¹ = 4-chlorophenyl, 4-trifluoromethylphenyl, benzylamino, (4-carboxyphenyl)aminyl] can be prepared has been reported. Novel mols. I and II are efficiently synthesized by using readily available and inexpensive substrates. The reaction conditions are mild and pure products were obtained without work-up and column purification

RSC Advances published new progress about 3696-23-9. 3696-23-9 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Thiourea,Amine,Benzene,Amide, name is 1-(4-Chlorophenyl)thiourea, and the molecular formula is C7H7ClN2S, Recommanded Product: 1-(4-Chlorophenyl)thiourea.

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

Kharbanda, Chetna published the artcileNovel Piperine Derivatives with Antidiabetic Effect as PPAR-γ Agonists, HPLC of Formula: 3696-23-9, the publication is Chemical Biology & Drug Design (2016), 88(3), 354-362, database is CAplus and MEDLINE.

Piperine is an alkaloid responsible for the pungency of black pepper. In this study, piperine isolated from Piper nigrum L. was hydrolyzed under basic condition to obtain piperic acid and was used as precursor to carry out the synthesis of twenty piperine derivatives containing benzothiazole moiety. All the benzothiazole derivatives were evaluated for their antidiabetic potential by OGT test followed by assessment of active derivatives on STZ-induced diabetic model. It was observed that nine of twenty novel piperine analogs (5b, 6a-h), showed significantly higher antidiabetic activity in comparison with rosiglitazone (standard). Furthermore, these active derivatives were evaluated for their action as PPAR-γ agonists demonstrating their mechanism of action. The effects on body weight, lipid peroxidation, and hepatotoxicity after administration with active derivatives were also studied to further establish these derivatives as lead mols. for treatment of diabetes with lesser side-effects.

Chemical Biology & Drug Design published new progress about 3696-23-9. 3696-23-9 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Thiourea,Amine,Benzene,Amide, name is 1-(4-Chlorophenyl)thiourea, and the molecular formula is C7H7ClN2S, HPLC of Formula: 3696-23-9.

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

Elwaie, Tamer A. published the artcileHER2 Kinase-Targeted Breast Cancer Therapy: Design, Synthesis, and In Vitro and In Vivo Evaluation of Novel Lapatinib Congeners as Selective and Potent HER2 Inhibitors with Favorable Metabolic Stability, Recommanded Product: 3-Chloro-4-fluoronitrobenzene, the publication is Journal of Medicinal Chemistry (2020), 63(24), 15906-15945, database is CAplus and MEDLINE.

HER2 kinase as a well-established target for breast cancer (BC) therapy is associated with aggressive clin. outcomes; thus, herein we present structural optimization for HER2-selective targeting. HER2 profiling of the developed derivatives demonstrated potent and selective inhibitions (IC₅₀: 5.4-12 nM) compared to lapatinib (IC₅₀: 95.5 nM). Favorably, 17d exhibited min. off-target kinase activation. NCI-5-dose screening revealed broad-spectrum activities (GI₅₀: 1.43-2.09μM) and 17d had a remarkable selectivity toward BC. Our compounds revealed significant selective and potent antiproliferative activities (~20-fold) against HER2+ (AU565, BT474) compared to HER2(-) cells. At 0.1 IC₅₀, 15i, 17d, and 25b inhibited pERK1/2 and pAkt by immunoblotting. Furthermore, 17d demonstrated potent in vivo tumor regression against the BT474 xenograft model. Notably, a metastasis case was observed in the vehicle but not in the test mice groups. CD-1 mice metabolic stability assay revealed high stability and low intrinsic clearance of 17d (T_1/2 > 145 min and CL_int(mic) < 9.6 mL/min/kg).

Journal of Medicinal Chemistry published new progress about 350-30-1. 350-30-1 belongs to chlorides-buliding-blocks, auxiliary class Fluoride,Chloride,Nitro Compound,Benzene, name is 3-Chloro-4-fluoronitrobenzene, and the molecular formula is C6H3ClFNO2, Recommanded Product: 3-Chloro-4-fluoronitrobenzene.

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

Milik, Sandra N. published the artcileSurmounting the resistance against EGFR inhibitors through the development of thieno[2,3-d]pyrimidine-based dual EGFR/HER2 inhibitors, Category: chlorides-buliding-blocks, the publication is European Journal of Medicinal Chemistry (2018), 316-336, database is CAplus and MEDLINE.

In light of the emergence of resistance against the currently available EGFR inhibitors, our study focuses on tackling this problem through the development of dual EGFR/HER2 inhibitors with improved enzymic affinities. Guided by the binding mode of the marketed dual EGFR/HER2 inhibitor, Lapatinib, we proposed the design of dual EGFR/HER2 inhibitors based on the 6-phenylthieno[2,3-d]pyrimidine as a core scaffold and hinge binder. After two cycles of screening aiming to identify the optimum aniline headgroup and solubilizing group, we eventually identified 27b as a dual EGFR/HER2 inhibitor with IC₅₀ values of 91.7 nM and 1.2 μM, resp. Notably, 27b dramatically reduced the viability of various patient-derived cancer cells preferentially overexpressing EGFR/HER2 (A431, MDA-MBA-361 and SKBr3 with IC₅₀ values of 1.45, 3.5 and 4.83 μM, resp.). Addnl., 27b efficiently thwarted the proliferation of lapatinib-resistant human non-small lung carcinoma (NCI-H1975) cells, harboring T790 M mutation, with IC₅₀ of 4.2 μM. Consistently, 27b significantly blocked EGF-induced EGFR activation and inactivated its downstream AKT/mTOR/S6 signalling pathway triggering apoptotic cell death in NCI-H1975 cells. The present study presents a promising candidate for further design and development of novel EGFR/HER2 inhibitors capable of overcoming EGFR TKIs resistance.

European Journal of Medicinal Chemistry published new progress about 350-30-1. 350-30-1 belongs to chlorides-buliding-blocks, auxiliary class Fluoride,Chloride,Nitro Compound,Benzene, name is 3-Chloro-4-fluoronitrobenzene, and the molecular formula is C6H3ClFNO2, Category: chlorides-buliding-blocks.

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

Bolli, Martin H. published the artcileNovel S1P₁ Receptor Agonists – Part 3: From Thiophenes to Pyridines, COA of Formula: C6H4ClNO2, the publication is Journal of Medicinal Chemistry (2014), 57(1), 110-130, database is CAplus and MEDLINE.

In preceding communications the authors summarized the authors’ medicinal chem. efforts leading to the identification of thiophene derivatives acting as potent, selective, and orally active S1P₁ agonists. As a continuation of these efforts, the authors replaced the thiophene by a 2-, 3-, or 4-pyridine and obtained less lipophilic, potent, and selective S1P₁ agonists (e.g., efficiently reducing blood lymphocyte count in the rat). Structural features influencing the compounds’ receptor affinity profile and pharmacokinetics are discussed. In addition, the ability to penetrate brain tissue has been studied for several compounds As a typical example for these pyridine based S1P₁ agonists, N-((S)-3-{4-[5-(2-Diethylamino-6-methylpyridin4-yl)[1,2,4]oxadiazol-3-yl]-2-ethyl-6-methylphenoxy}-2-hydroxypropyl)-2-hydroxyacetamide showed EC₅₀ values of 0.6 and 352 nM for the S1P₁ and S1P₃ receptor, resp., displayed favorable PK properties, and penetrated well into brain tissue. In the rat, N-((S)-3-{4-[5-(2-Diethylamino-6-methylpyridin4-yl)[1,2,4]oxadiazol-3-yl]-2-ethyl-6-methylphenoxy}-2-hydroxypropyl)-2-hydroxyacetamide maximally reduced the blood lymphocyte count for at least 24 h after oral dosing of 3 mg/kg.

Journal of Medicinal Chemistry published new progress about 6313-54-8. 6313-54-8 belongs to chlorides-buliding-blocks, auxiliary class Pyridine,Chloride,Carboxylic acid, name is 2-Chloroisonicotinic acid, and the molecular formula is C6H4ClNO2, COA of Formula: C6H4ClNO2.

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

Ma, C. Derek published the artcileLiquid Crystal Interfaces Programmed with Enzyme-Responsive Polymers and Surfactants, Application of 3-Carboxy-N,N,N-trimethylpropan-1-aminium chloride, the publication is Small (2015), 11(43), 5747-5751, database is CAplus and MEDLINE.

General strategies that permit amplification and transduction of mol. recognition events over multiple length scales are of tremendous interest for a range of applications, including advanced sensor design and responsive smart materials. Liquid crystals (LCs) provide an exciting opportunity in this regard as the supramol. organization of mesogens within LC phases can be dynamically coupled to nanoscopic and mol.-scale interfacial events such that the LC generates a detectable optical signal on the micrometer length scale. While a number of examples of LC ordering transitions triggered by biomol. events do exist, rational design of such systems is not yet possible. As a first step toward establishing generalizable design strategies for signal propagation in nanoscale and microscale responsive materials, herein we report the synthesis and interfacial characterization of biol. active peptide-polymer amphiphiles (PPAs) at the interfaces of LCs and demonstrate their use in triggering LC ordering transitions in LC microdroplets in response to targeted biomol. events.

Small published new progress about 6249-56-5. 6249-56-5 belongs to chlorides-buliding-blocks, auxiliary class Phase Transfer Catalyst,Inhibitor,Natural product, name is 3-Carboxy-N,N,N-trimethylpropan-1-aminium chloride, and the molecular formula is C7H16ClNO2, Application of 3-Carboxy-N,N,N-trimethylpropan-1-aminium chloride.

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