Day: December 6, 2022

Parrino, Barbara published the artcileSynthesis of the new ring system bispyrido[4′,3′:4,5]pyrrolo[1,2-a:1′,2′-d]pyrazine and its deaza analogue, Category: pyridine-derivatives, the main research area is pyrrolopyridinecarboxylic acid preparation; bispyridopyrrolopyrazine dione preparation antineoplastic mol docking; pyridopyrrolopyrazino indole dione antineoplastic mol docking.

A series of bispyridopyrrolopyrazine diones I [R1 = R4 = H, Cl, OMe; R2 = R3 = H, OMe] and their deaza analogs pyridopyrrolopyrazinoindole diones II [R1 = R2 = H, Cl, OMe] was synthesized and evaluated for their antineoplastic activities and mol. docking studies. Among the synthesized compounds I [R1 = R2 = R4 = H; R3 = OMe] and II [R1 = R2 = H; R1 = OMe, R2 = H; R1 = H, R2 = OMe] exhibited modest activity against MCF7 (a breast cancer cell line) and/or UO-31 (a renal cancer cell line).

Molecules published new progress about Antitumor agents. 3469-63-4 belongs to class pyridine-derivatives, name is Ethyl 5-methoxy-1H-pyrrolo[2,3-c]pyridine-2-carboxylate, and the molecular formula is C11H12N2O3, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Ren, Hang published the artcileVersatile synthesis and biological evaluation of novel 3′-fluorinated purine nucleosides, Category: pyridine-derivatives, the main research area is Suzuki Stille coupling nucleoside fluororibose human aminopurine preparation antitumor; 3’-fluororibonucleoside; 6-substituted purine; anticancer; purine nucleoside; synthesis.

A unified synthetic strategy accessing novel 3′-fluorinated purine nucleoside derivatives and their biol. evaluation were achieved. Novel 3′-fluorinated analogs were constructed from a common 3′-deoxy-3′-fluororibofuranose intermediate. Employing Suzuki and Stille cross-coupling reactions, fifteen 3′-fluororibose purine nucleosides, e.g. I, and eight 3′-fluororibose 2-chloro/2-aminopurine nucleosidese, e.g. II, with various substituents at position 6 of the purine ring were efficiently synthesized. Furthermore, 3′-fluorine analogs of natural products nebularine and 6-methylpurine riboside were constructed via our convergent synthetic strategy. Synthesized nucleosides were tested against HT116 (colon cancer) and 143B (osteosarcoma cancer) tumor cell lines. We have demonstrated 3′-fluorine purine nucleoside analogs display potent tumor cell growth inhibition activity at sub- or low micromolar concentration

Beilstein Journal of Organic Chemistry published new progress about Antitumor agents. 917471-30-8 belongs to class pyridine-derivatives, name is (5-(Prop-1-yn-1-yl)pyridin-3-yl)boronic acid, and the molecular formula is C8H8BNO2, Category: pyridine-derivatives.

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

Chessari, Gianni published the artcileFragment-Based Drug Discovery Targeting Inhibitor of Apoptosis Proteins: Discovery of a Non-Alanine Lead Series with Dual Activity Against cIAP1 and XIAP, COA of Formula: C9H11ClN2, the main research area is inhibitor apoptosis protein antitumor neoplasm.

Inhibitor of apoptosis proteins (IAPs) are important regulators of apoptosis and pro-survival signaling pathways whose deregulation is often associated with tumor genesis and tumor growth. IAPs have been proposed as targets for anticancer therapy, and a number of peptidomimetic IAP antagonists have entered clin. trials. Using the fragment-based screening approach, the authors identified nonpeptidic fragments binding with millimolar affinities to both cellular inhibitor of apoptosis protein 1 (cIAP1) and X-linked inhibitor of apoptosis protein (XIAP). Structure-based hit optimization together with an anal. of protein-ligand electrostatic potential complementarity allowed us to significantly increase binding affinity of the starting hits. Subsequent optimization gave a potent nonalanine IAP antagonist I structurally distinct from all IAP antagonists previously reported. The lead compound had activity in cell-based assays and in a mouse xenograft efficacy model and represents a highly promising start point for further optimization.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 1403899-44-4 belongs to class pyridine-derivatives, name is 6-Chloro-3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-c]pyridine, and the molecular formula is C9H11ClN2, COA of Formula: C9H11ClN2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Loza-Huerta, Arlet published the artcileThallium-sensitive fluorescent assay reveals loperamide as a new inhibitor of the potassium channel Kv10.1, HPLC of Formula: 72509-76-3, the main research area is thallium loperamide potassium channel inhibitor; Electrophysiology; Kv10.1 potassium channel; Oncogenic channel; Thallium-sensitive fluorescent assay.

Ion channels have been proposed as therapeutic targets for different types of malignancies. One of the most studied ion channels in cancer is the voltage-gated potassium channel ether-a-́go-go 1 or Kv10.1. Various studies have shown that Kv10.1 expression induces the proliferation of several cancer cell lines and in vivo tumor models, while blocking or silencing inhibits proliferation. Kv10.1 is a promising target for drug discovery modulators that could be used in cancer treatment. This work aimed to screen for new Kv10.1 channel modulators using a thallium influx-based assay. Pharmacol. effects of small mols. on Kv10.1 channel activity were studied using a thallium-based fluorescent assay and patch-clamp electrophysiol. recordings, both performed in HEK293 stably expressing the human Kv10.1 potassium channel. In thallium-sensitive fluorescent assays, we found that the small mols. loperamide and amitriptyline exert a potent inhibition on the activity of the oncogenic potassium channel Kv10.1. These results were confirmed by electrophysiol. recordings, which showed that loperamide and amitriptyline decreased the amplitude of Kv10.1 currents in a dose-dependent manner. Both drugs could be promising tools for further studies. Thallium-sensitive fluorescent assay represents a reliable methodol. tool for the primary screening of different mols. with potential activity on Kv10.1 channels or other K+ channels.

Pharmacological Reports published new progress about Antitumor agents. 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, HPLC of Formula: 72509-76-3.

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

Abebe, Felagot A. published the artcileDevelopment of a Rapid In Vitro Screening Assay Using Metabolic Inhibitors to Detect Highly Selective Anticancer Agents, Application of 2-Methoxynicotinaldehyde, the main research area is antitumor drug screening assay metabolic inhibitor.

Traditional long exposure (24-72 h) cell viability assays for identification of potential drug compounds can fail to identify compounds that are: (a) biol. active but not toxic and (b) inactive without the addition of a synergistic additive. Herein, we report the development of a rapid (1-2 h) compound screening technique using a com. available cell viability kit (CellTiter-Glo) that has led to the detection of compounds that were not identified as active agents using traditional cytotoxicity screening methods. These compounds, in combination with metabolic inhibitor 2-deoxyglucose, display selectivity toward a pancreatic cancer cell line. An evaluation of 11 mammalian cell lines against 30 novel compounds and two metabolic inhibitors is reported. The inclusion of metabolic inhibitors during an initial screening process, and not simply during mechanistic investigations of a previously identified hit compound, provides a rapid and sensitive tool for identifying drug candidates potentially overlooked by other methods.

ACS Omega published new progress about Antitumor agents. 71255-09-9 belongs to class pyridine-derivatives, name is 2-Methoxynicotinaldehyde, and the molecular formula is C7H7NO2, Application of 2-Methoxynicotinaldehyde.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Zhao, Lifeng published the artcileNovel small molecules as apoptosis inducers: Synthesis, preliminary structure-activity relationships, and in vitro biological evaluation, COA of Formula: C6H7ClN2, the main research area is small mol apoptosis inducer preparation structure activity relationship bioactivity.

Inducing apoptosis is a promising therapeutic approach to overcome cancer. In this study, 30 compounds were synthesized and evaluated for their antiproliferative activity against three tumor cell lines in vitro: A875, H460 and Hela cancer cells by the MTT assay. The most potent compound discovered by our group inhibited the proliferation of A875 cells with an IC50 value of 98 nM. Flow cytometry anal. and morphol. anal. suggested that said compound had potential anticancer efficacy via G2/M cell cycle arrest. The SAR anal. was also performed.

Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 133627-45-9 belongs to class pyridine-derivatives, name is 2-Chloro-4-methylpyridin-3-amine, and the molecular formula is C6H7ClN2, COA of Formula: C6H7ClN2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Wang, Senlin published the artcileThe antitumor activity of 4,4′-bipyridinium amphiphiles, Safety of 1,1-Di-n-octyl-4,4-bipyridinium Dibromide, the main research area is alveolar basal carcinoma cell bipyridinium amphiphile antitumor SAR.

A series of 4,4′-bipyridinium amphiphiles, compounds I [n = 8-16] were synthesized and their anticancer activities were further evaluated. MTT assay showed that the cytotoxicity first increased and then decreased with the growth of carbon chains (8-16 C) at both ends of bipyridyl. Specifically, compounds with saturated carbon chains consisting of 13 carbons at both ends of bipyridyl displayed the best cell inhibitory activity with IC50 values in the low-micromolar range, which were even superior to that of cisplatin, against all the tested human cancer cells and cisplatin-resistant A549 cancer cells in vitro. In addition, compound I [n = 13] could evidently arrest the G2/M phase of the cell cycle in a dose-dependent manner. Moreover, this study demonstrates the potent performance of compound I [n = 13] in cell growth inhibition and apoptosis induction via a conceivable approach of membrane damage.

RSC Advances published new progress about Antitumor agents. 36437-30-6 belongs to class pyridine-derivatives, name is 1,1-Di-n-octyl-4,4-bipyridinium Dibromide, and the molecular formula is C26H42Br2N2, Safety of 1,1-Di-n-octyl-4,4-bipyridinium Dibromide.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Ohmi, Masashi published the artcileIdentification of a novel 2-pyridyl-benzensulfonamide derivative, RQ-00203078, as a selective and orally active TRPM8 antagonist, Safety of 2-Chloro-3-fluoro-5-(trifluoromethyl)pyridine, the main research area is pyridylbenzensulfonamide derivative RQ00203078 preparation TRPM8 antagonist cold allodynia; structure activity TRPM8 antagonist pyridylbenzensulfonamide derivative RQ00203078; Cold allodynia; RQ-00203078; Sulfonamide; TRPM8 antagonist; Wet-dog shakes.

A novel series of 2-pyridyl-benzensulfonamide derivatives have been identified as selective and orally active TRPM8 antagonists via high throughput screening (HTS). Exploration of the structure-activity relationships of compound (I) has led to the identification of RQ-00203078 (compound 36) as a highly selective, potent and orally available TRPM8 antagonist. RQ-00203078 demonstrated excellent in vivo activity in a dose dependent manner with an ED50 value of 0.65 mg/kg in the icilin-induced wet-dog shakes model in rats after oral administration and may become an important pharmacol. tool for fully assessing the potential therapeutic use of the targets activated by cold stimulation.

Bioorganic & Medicinal Chemistry Letters published new progress about Allodynia (cold). 72600-67-0 belongs to class pyridine-derivatives, name is 2-Chloro-3-fluoro-5-(trifluoromethyl)pyridine, and the molecular formula is C6H2ClF4N, Safety of 2-Chloro-3-fluoro-5-(trifluoromethyl)pyridine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem