Results 21 to 30 of about 7,519 (213)

NAromatic-Substituted Indazole Derivatives as Brain-Penetrant and Orally Bioavailable JNK3 Inhibitors

open access: yes, 2021
An indazole/aza-indazole scaffold was developed as a novel chemotype for JNK3 inhibition. Extensive structure activity relationship (SAR) studies utilizing various in vitro and in vivo assays led to potent and highly selective JNK3 inhibitors with good ...
Jae Cheon Ryu   +7 more
core   +2 more sources

Cobalt‐Catalyzed C─N Bond Formation via Metal‐Hydride Hydrogen Atom Transfer (MHAT)

open access: yesAngewandte Chemie, EarlyView.
Cobalt‐catalyzed metal‐hydride hydrogen atom transfer (Co‐MHAT) converts simple alkenes into C─N bonds under mild, near‐neutral conditions. A shared Co─H‐initiated radical/organocobalt intermediate is channeled into radical trapping, radical‐polar crossover, or radical ligand transfer, unifying hydroamination, hydroazidation, hydroamidation, and remote
Arman Khosravi, Ming‐Yu Ngai
wiley   +2 more sources

Synthesis of Large‐ and Medium‐Sized Heterobiaryl Atropisomeric Rings and Atropopeptides by Catalytic Intramolecular SNAr

open access: yesAngewandte Chemie, EarlyView.
Catalytic, intramolecular N‐heterocycle arylation by nucleophilic aromatic substitution (SNAr) is now available for synthesis of highly strained macrocycles and medium‐sized heterobiaryl atropisomeric rings, including atropopeptides. Key to the approach is the ability to generate a strong base catalytically, taking advantage of base‐embedding ...
Alireza Abbasi Kejani   +7 more
wiley   +2 more sources

Synthesis of indazolo[5,4-b][1,6]naphthyridine and indazolo[6,7-b][1,6]naphthyridine derivatives

open access: yesHeterocyclic Communications, 2019
A simple method for the synthesis of the title compounds by an efficient in-situ reduction and cyclization reactions of aromatic aldehydes, tert-butyl 2,4-dioxopiperidine-1-carboxylate and 5-nitro-1H-indazole or 6-nitro-1H-indazole was developed.
Chen Dong-Mei   +5 more
doaj   +1 more source

Synthesis and Cytotoxic Activity of Combretastatin A-4 and 2,3-Diphenyl-2H-indazole Hybrids

open access: yesPharmaceuticals, 2021
Cancer is the second leading cause of death, after cardiovascular diseases. Different strategies have been developed to treat cancer; however, chemotherapy with cytotoxic agents is still the most widely used treatment approach.
Jaime Pérez-Villanueva   +11 more
doaj   +1 more source

Tris[2-(2H-indazol-2-yl)ethyl]amine

open access: yesActa Crystallographica Section E, 2012
The title tertiary amine, C27H27N7, a potential tripodal ligand for coordination chemistry, crystallizes with the central N atom located on a threefold axis of a trigonal cell. The gauche conformation of the N(amime)—CH2—CH2—
Saúl Ovalle   +4 more
doaj   +1 more source

Indazole-Based Covalent Inhibitors To Target Drug-Resistant Epidermal Growth Factor Receptor

open access: yes, 2017
The specific targeting of oncogenic mutant epidermal growth factor receptor (EGFR) is a breakthrough in targeted cancer therapy and marks a drastic change in the treatment of non-small cell lung cancer (NSCLC).
Carsten Schultz-Fademrecht (1533556)   +32 more
core   +1 more source

Anticonvulsant action of indazole

open access: yesEpilepsy Research, 2013
Here we report that indazole is characterized as a potential anticonvulsant, inhibiting pentylenetetrazole-, electroshock- and strychnine-induced convulsions in mice (ED50's: 39.9, 43.2 and 82.4 mg/kg, respectively) but not bicuculline- and picrotoxin-induced convulsions.
Nobuko, Matsumura   +5 more
openaire   +2 more sources

New 1H-Benzo[f]indazole-4,9-diones Conjugated with C-Protected Amino Acids and Other Derivatives: Synthesis and in Vitro Antiproliferative Evaluation

open access: yesMolecules, 2015
1H-Benzo[f]indazole-4,9-dione derivatives conjugated with C-protected amino acids (glycine, l-alanine, l-phenylalanine and l-glutamic acid) 6a–l were prepared by chemically modifying the prenyl substituent of 3-methyl-7-(4-methylpent-3-enyl)-1H-benzo[f ...
Aurora Molinari   +7 more
doaj   +1 more source

Design, synthesis and biological evaluation of novel 1H-1,2,4-triazole, benzothiazole and indazole-based derivatives as potent FGFR1 inhibitors viafragment-based virtual screening

open access: yesJournal of Enzyme Inhibition and Medicinal Chemistry, 2020
Fibroblast growth-factor receptor (FGFR) is a potential target for cancer therapy. We designed three novel series of FGFR1 inhibitors bearing indazole, benzothiazole, and 1H-1,2,4-triazole scaffold via fragment-based virtual screening.
Jian Liu   +10 more
doaj   +1 more source

Home - About - Disclaimer - Privacy