Category: 24484-93-3

Ishida, Yoshiyuki published the artcileSequence selective dual-emission detection of (i, i + 1) bis-phosphorylated peptide using diazastilbene-type Zn(ii)-Dpa chemosensor, COA of Formula: C7H6ClNO2, the main research area is sequence selective dual emission bisphosphorylated peptide diazastilbene zinc chemosensor.

This paper describes a new fluorescent chemosensor for phosphorylated peptide, which comprises a rigid trans-4,4′-diazastilbene and two Zn(II)-Dpa (2,2′-dipicolylamine) units; this chemosensor sequence-selectively binds to a (i, i + 1) bis-phosphorylated peptide and displays a dual-emission fluorescence change.

Chemical Communications (Cambridge, United Kingdom) published new progress about Affinity. 24484-93-3 belongs to class pyridine-derivatives, name is Methyl 4-chloropicolinate, and the molecular formula is C7H6ClNO2, COA of Formula: C7H6ClNO2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Ishida, Yoshiyuki published the artcileSequence selective dual-emission detection of (i, i + 1) bis-phosphorylated peptide using diazastilbene-type Zn(ii)-Dpa chemosensor, COA of Formula: C7H6ClNO2, the main research area is sequence selective dual emission bisphosphorylated peptide diazastilbene zinc chemosensor.

This paper describes a new fluorescent chemosensor for phosphorylated peptide, which comprises a rigid trans-4,4′-diazastilbene and two Zn(II)-Dpa (2,2′-dipicolylamine) units; this chemosensor sequence-selectively binds to a (i, i + 1) bis-phosphorylated peptide and displays a dual-emission fluorescence change.

Chemical Communications (Cambridge, United Kingdom) published new progress about Affinity. 24484-93-3 belongs to class pyridine-derivatives, name is Methyl 4-chloropicolinate, and the molecular formula is C7H6ClNO2, COA of Formula: C7H6ClNO2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Yao, Jianwen published the artcileDesign, synthesis and biological activities of sorafenib derivatives as antitumor agents, Recommanded Product: Methyl 4-chloropicolinate, the main research area is sorafenib derivative preparation antitumor antiangiogenesis activity.

A series of novel sorafenib derivatives was designed and synthesized in high yields using various substituted anilines, and their antiproliferative activities against HCT116, PC-3 and MDA-MB-231 cell lines were also evaluated and described. All compounds exhibited potent antiproliferative activity against HCT116 and PC-3 cells with IC50 = 2.8-52.0 and 2.2-45.6 μM; compounds I [R = Et, cyclopropyl] demonstrated competitive antiproliferative activities to sorafenib against all three cancer cell lines; the cytotoxicity of compound I [R = cyclohexyl] is more potent than that of sorafenib. Some compounds were chosen for further evaluation of the anti-angiogenesis activity, and showed the inhibition of sprout formation from aortic ring ex vivo. The structures of all the newly synthesized compounds were determined by 1H NMR, 13C NMR and HRMS.

Bioorganic & Medicinal Chemistry Letters published new progress about Angiogenesis. 24484-93-3 belongs to class pyridine-derivatives, name is Methyl 4-chloropicolinate, and the molecular formula is C7H6ClNO2, Recommanded Product: Methyl 4-chloropicolinate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Ghiazza, Clement published the artcileDeaminative chlorination of aminoheterocycles, HPLC of Formula: 24484-93-3, the main research area is chloro heterocycle selective preparation; aminoheterocycle deaminative chlorination.

Herein we present a simple methodol. that enabled the NH2 groups in aminoheterocycles to be conceived as masked modification handles. With the aid of a simple pyrylium reagent and a cheap chloride source, C(sp2)-NH2 could be converted into C(sp2)-Cl bonds. The method was characterized by its wide functional group tolerance and substrate scope, allowing the modification of different classes of heteroaromatic motifs (five- and six-membered heterocycles), bearing numerous sensitive motifs. The facile conversion of NH2 into Cl in a late-stage fashion enabled practitioners to apply Sandmeyer- and Vilsmeier-type transforms without the burden of explosive and unsafe diazonium salts, stoichiometric transition metals or highly oxidizing and unselective chlorinating agents.

Nature Chemistry published new progress about Chemoselectivity. 24484-93-3 belongs to class pyridine-derivatives, name is Methyl 4-chloropicolinate, and the molecular formula is C7H6ClNO2, HPLC of Formula: 24484-93-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Qin, Mingze published the artcileDesign and synthesis of novel 2-(4-(2-(dimethylamino)ethyl)-4H-1,2,4-triazol-3-yl)pyridines as potential antitumor agents, SDS of cas: 24484-93-3, the main research area is triazolylpyridine dimethylaminoethyl preparation antitumor agent; 4-(2-(Dimethylamino)ethyl)-4H-1,2,4-triazole; Antitumor activity; Synthesis.

New 2-(4-(2-(dimethylamino)ethyl)-4H-1,2,4-triazol-3-yl)pyridine derivatives were synthesized and evaluated for their in vitro cytotoxicity against five cancer cell lines namely MKN-45, H460, HT-29, A549, and U87MG, as well as the normal cell line WI-38. Nearly all the compounds exhibited superior potency to sorafenib with a better selectivity towards the MKN-45, H460, and HT-29 cell lines. In addition, the enzymic screening result demonstrated that the optimized compounds possessed potent Raf kinase inhibition as well as favorable enzyme selectivity. The most promising compound, I, showed high levels of cytotoxicity against MKN-45, H460, and HT-29 cells with IC50 values of 51, 72, and 130 nM, resp., which are 45.5, 30.4, and 27.8 folds higher than the corresponding IC50 values for sorafenib against these cell lines. Structure-activity relationships revealed that the dimethylaminoethyl group was crucial for high activity.

European Journal of Medicinal Chemistry published new progress about Antitumor agents. 24484-93-3 belongs to class pyridine-derivatives, name is Methyl 4-chloropicolinate, and the molecular formula is C7H6ClNO2, SDS of cas: 24484-93-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

El-Damasy, Ashraf Kareem published the artcileDesign and synthesis of new potent anticancer benzothiazole amides and ureas featuring pyridylamide moiety and possessing dual B-RafV600E and C-Raf kinase inhibitory activities, Name: Methyl 4-chloropicolinate, the main research area is benzothiazole amide preparation Raf kinase inhibitory anticancer activity; urea benzothiazole preparation Raf kinase inhibitory anticancer activity; Amide; Anticancer activity; B-Raf(V600E); Benzothiazole; C-Raf; Pyridylamide; Urea.

A new series of benzothiazole amide and urea derivatives tethered with the privileged pyridylamide moiety by ether linkage at the 6-position of benzothiazole (22 final compounds) has been designed and synthesized as potent anticancer sorafenib analogs. A selected group of twelve derivatives was appraised for its antiproliferative activity over a panel of 60 human cancer cell lines at a single dose concentration of 10 μM at National Cancer Institute (NCI, USA). Some compounds exhibited promising growth inhibitions and thus were further tested in advanced 5-dose testing assay to determine their GI50 values. The cellular based assay results revealed that 3,5-bis-trifluoromethylphenyl urea derivative I is the best derivative with superior potency and efficacy compared to sorafenib as well as notable extended spectrum activity covering 57 human cancer cell lines. Kinase screening of compound I showed its kinase inhibitory effect against both B-RafV600E and C-Raf. Moreover, the most potent derivatives in cells were investigated for their RAF inhibitory activities, and the results were rationalized with the mol. docking study. Profiling of CYP450 and hERG channel inhibitory effects for the active compounds revealed their low possibilities to exhibit undesirable drug-drug interactions and cardiac side effects.

European Journal of Medicinal Chemistry published new progress about Antitumor agents. 24484-93-3 belongs to class pyridine-derivatives, name is Methyl 4-chloropicolinate, and the molecular formula is C7H6ClNO2, Name: Methyl 4-chloropicolinate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Zhong, Lili published the artcileSynthesis of deuterium-enriched sorafenib derivatives and evaluation of their biological activities, Application In Synthesis of 24484-93-3, the main research area is sorafenib deuterium anticancer agent cervical carcinoma; Antitumor activities; Deuterium substitution; Pharmacokinetics; Sorafenib.

Deuterium substitution has been widely known that can improve the pharmacokinetic profiles due to isotope effect. Herein, a series of deuterated sorafenib derivatives have been synthesized and characterized by 1H NMR, 13C NMR and MS. Their antitumor activities were evaluated in vitro against human hepatoma cell line HepG2 and human cervical carcinoma cell line HeLa. The LogP values were detected by high-performance liquid chromatog. Subsequently, the metabolic stability and pharmacokinetics study were assessed in vitro and in vivo.

Molecular Diversity published new progress about Antitumor agents. 24484-93-3 belongs to class pyridine-derivatives, name is Methyl 4-chloropicolinate, and the molecular formula is C7H6ClNO2, Application In Synthesis of 24484-93-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Qin, Mingze published the artcileDiscovery of novel diaryl urea derivatives bearing a triazole moiety as potential antitumor agents, Recommanded Product: Methyl 4-chloropicolinate, the main research area is urea triazole antitumor neoplasm; Antitumor activity; Diaryl ureas; Organic synthesis; Structure-activity relationship.

Herein, the authors report a novel series of diaryl urea derivatives bearing a triazole moiety, from which potent antitumor agents have been identified. With a modified triazole, most compounds showed high level activity in both cellular and enzymic assays, accompanied with a suitable ClogD7.4 value. The most active compound, I, effectively suppressed proliferation of HT-29, H460 and MDA-MB-231 cancer cells, with IC50 values of 0.90, 0.85 and 1.54 μM, resp. Compound I also exhibited significant inhibition of tyrosine kinases including c-Kit, RET and FLT3. Furthermore, compound I could obviously induce apoptosis of HT-29 cells in a concentration-dependent manner. The study of structure-activity relationships also revealed that a hydrophilic tail at the 4-position of the triazole was crucial for high activity of the compound

European Journal of Medicinal Chemistry published new progress about Antitumor agents. 24484-93-3 belongs to class pyridine-derivatives, name is Methyl 4-chloropicolinate, and the molecular formula is C7H6ClNO2, Recommanded Product: Methyl 4-chloropicolinate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Yang, Jie published the artcileThree water-soluble acylhydrazone tetranuclear transition metal complexes: Crystal structures, DNA/BSA interactions and cytotoxicity studies, Computed Properties of 24484-93-3, the main research area is transition metal acetylpyridinechloropyridinecarbonylhydrazone complex preparation DNA BSA binding anticancer; crystal structure transition metal acetylpyridinechloropyridinecarbonylhydrazone complex; Acylhydrazone; CT-DNA/BSA interaction; Cytotoxic activity; Transition metal complex.

2-Acetylpyridine-4-chloropyridine-2-carbonylhydrazone (C13H11ClN4O, HL) and its three water-soluble tetranuclear complexes [Cu4(NO3)2(L)4]·(NO3)2 (1), [Co4(NO3)2(H2O)(C2H5OH)(L)4]·(NO3)2 (2) and [Zn4(NO3)2(H2O)(C2H5OH)(L)4]·(NO3)2 (3) were synthesized and characterized showing that 1-3 were all tetranuclear complexes. The interactions of HL, 1-3 with calf thymus DNA (CT-DNA) and bovine serum albumin (BSA) were explored using UV-visible (UV-Vis) titration, fluorescence spectroscopy, microcalorimetry and mol. docking techniques. The UV-Vis spectroscopy measurements showed that complexes 1-3 could strongly bind to CT-DNA by the intercalation mode, while HL interacted with CT-DNA through groove binding. From the fluorescence spectroscopy results, the interaction between HL, 1-3 and BSA was a static quenching procedure, in which complexes 1-3 had two binding sites near Trp residues of BSA while HL only had one. The microcalorimetric studies revealed that the interactions of HL and 1-3 to CT-DNA/BSA were all endothermic and the duration of each interaction was all less than 30 min. The in silico mol. docking illustrated intermol. interactions of 1-3 binding with DNA/BSA included hydrogen bond, halogen bond, hydrophobic and electrostatic interactions. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay indicated that complex 1 possessed better cytotoxicity against HeLa, A549, MCF7 and HCT-116 than cisplatin and could be used as an alternative anticancer drug.

Journal of Inorganic Biochemistry published new progress about Antitumor agents. 24484-93-3 belongs to class pyridine-derivatives, name is Methyl 4-chloropicolinate, and the molecular formula is C7H6ClNO2, Computed Properties of 24484-93-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Gardner, Evan J. published the artcileTris(pyrazolyl)borate Copper Hydroxide Complexes Featuring Tunable Intramolecular H-Bonding, Application In Synthesis of 24484-93-3, the main research area is crystal structure copper pyrazolylborate pendant heterocycle arm; copper pyridyl pyrimidyl pyrazolylborate preparation intramol hydrogen bonding.

A modular synthesis provides access to new tris(pyrazolyl)borate ligands XpyMeTpK that possess a single functionalized pendant pyridyl (py) or pyrimidyl (pyd) arm designed to engage in tunable intramol. H-bonding to metal-bound functionalities. To illustrate such H-bonding interactions, [XpyMeTpCu]2(μ-OH)2 (6a-6e) complexes were synthesized from the corresponding XpyMeTpCu-OAc (5a-5e) complexes. Single crystal x-ray structures of three new dinuclear [XpyMeTpCu]2(μ-OH)2 complexes reveal H-bonding between the pendant heterocycle and bridging hydroxide ligands while the donor arm engages the Cu center in an unusual monomeric DMAPMeTpCu-OH complex. Vibrational studies (IR) of each bridging hydroxide complex reveal reduced νOH frequencies that tracks with the H-bond accepting ability of the pendant arm. Reversible protonation studies that interconvert [XpyMeTpCu]2(μ-OH)2 and [XpyMeTpCu(OH2)]OTf species indicate that the acidity of the corresponding aquo ligand decreases with increasing H-bond accepting ability of the pendant arm.

Inorganic Chemistry published new progress about Crystal structure. 24484-93-3 belongs to class pyridine-derivatives, name is Methyl 4-chloropicolinate, and the molecular formula is C7H6ClNO2, Application In Synthesis of 24484-93-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem