14251-82-2Relevant academic research and scientific papers
Synthesis and biological evaluation of 1-benzyl-N-(2-(phenylamino)pyridin-3-yl)-1H-1,2,3-triazole-4-carboxamides as antimitotic agents
Prasad, Budaganaboyina,Lakshma Nayak,Srikanth,Baig, Mirza Feroz,Subba Reddy,Babu, Korrapati Suresh,Kamal, Ahmed
, p. 535 - 548 (2018/11/26)
A library of 1-benzyl-N-(2-(phenylamino)pyridin-3-yl)-1H-1,2,3-triazole-4-carboxamides (7a–al) have been designed, synthesized and screened for their anti-proliferative activity against some selected human cancer cell lines namely DU-145, A-549, MCF-7 and HeLa. Most of them have shown promising cytotoxicity against lung cancer cell line (A549), amongst them 7f was found to be the most potent anti-proliferative congener. Furthermore, 7f exhibited comparable tubulin polymerization inhibition (IC50 value 2.04 μM) to the standard E7010 (IC50 value 2.15 μM). Moreover, flow cytometric analysis revealed that this compound induced apoptosis via cell cycle arrest at G2/M phase in A549 cells. Induction of apoptosis was further observed by examining the mitochondrial membrane potential and was also confirmed by Hoechst staining as well as Annexin V-FITC assays. Furthermore, molecular docking studies indicated that compound 7f binds to the colchicine binding site of the β-tubulin. Thus, 7f exhibits anti-proliferative properties by inhibiting the tubulin polymerization through the binding at the colchicine active site and by induction of apoptosis.
The Elimination of an Alkoxy Group in the Photo-Graebe-Ullmann Conversion of 1-(2,5-Dialkoxyphenyl)triazolopyridines into Carbolines, and the Preparation of α-, γ- and δ-Carboline Quinones
Mehta, Lina K.,Parrick, John,Payne, Fereshteh
, p. 1261 - 1268 (2007/10/02)
Photochemical decomposition of 1-(2,5-dialkoxyphenyl)triazolopyridines 7a, 21 and 33 resulted in elimination of an alkoxy group to give the alkoxycarbolines 9a and 35 in addition to the expected dialkoxycarbolines.The carbolines having either a methoxy and an isopropoxy substituent 22, 34a and 34b or two methoxy groups 41 were oxidised with ceric ammonium nitrate to yield the α-, γ- or δ-carboline p-quinones.
Nitro, amino and aroylamino-N-phenylpyridinamines in a process for preparing pyrido[1,4]benzodiazepines
-
, (2008/06/13)
Nitro, amino and aroylamino-N-phenylpyridinamines as chemical intermediates and/or having antidepressant activity having the formula STR1 wherein R3 is nitro, amino or aroylamino, and Q is hydrogen, --NR1 R2 or halogen are disclosed in a process for preparing pyrido[1,4]benzodiazepines.
Synthesis and analgesic activity of 1,3-dihydro-3-(substituted phenyl)imidazo[4,5-6]pyridin-2-ones and 3-(substituted phenyl)-1,2,3-triazolo[4,5-b]pyridines
Clark,Pessolano,Shen,Jacobus,Jones,Lotti,Flataker
, p. 965 - 978 (2007/10/05)
In a study of nonsteroidal antiinflammatory and analgesic agents, a series of 1,3-dihydro-3-(substituted phenyl)imidazo[4,5-b]pyridin-2-ones and 3-(substituted phenyl)triazolo[4,5-b]pyridines was prepared. Many of the imidazolones were alkylated on the free nitrogen. In a modified Randall-Selitto analgesic assay, the pain thresholds of both the inflamed and normal foot were elevated. This is not commonly observed with nonsteroidal antiinflammatory agents. The most active compounds were 1,3-dihydro-3-[3,4-(methylenedioxy)phenyl]imidazo[4,5-b]pyridin-2-one (I-15) and its N-allyl (I-21) and N-isopropyl (I-121) derivatives. In the triazole series the 3-(2-fluoro- and 2,4-difluorophenyl)triazolo[4,5-b]pyridines (T-1 and T-8) were the best. The imidazole compounds were somewhat superior in analgesic activity to codeine and d-propoxyphene without showing any narcotic characteristics. Some of the compounds also possessed activity against carrageenan-induced foot edema in the rat, so these compounds represent a new class of nonnarcotic analgesic antiinflammatories, capable of producing a greater degree of analgesia than that obtainable with other nonsteroidal antiinflammatory agents.
3-Phenyl,3H 1,2,3 triazolo[4,5-b]pyridines
-
, (2008/06/13)
3H-1,2,3-Triazolo[4,5-b]pyridines substituted in the 3-position have utility as analgesic, anti-inflammatory and anti-pyretic agents. They are prepared by diazotization of a 3-amino-2-(substitute) aminopyridine.
