938182-54-8Relevant articles and documents
A new synthetic approach for pyrazolo[1,5-a]pyrazine-4(5H)-one derivatives and their antiproliferative effects on lung adenocarcinoma cell line
Uygun, Meltem Tan,Amudi, Karina,Tura?l?, ?rem Do?an,Menges, Nurettin
, (2021/01/11)
Abstract: Starting from the 3,5-dimethyl pyrazole ring and acetophenone derivatives, five different N-propargylated C-3 substituted pyrazoles were obtained. These derivatives were reacted with different amine derivatives using Cs2CO3 in methanol and 11 different pyrazolo [1,5-a] pyrazine-4(5H)-one derivatives were obtained, which are not found in the literature. The cytotoxic effects of these derivatives in the A549 cell line were investigated. The 160?μM concentration of two derivatives was found to increase cell death rate to 50%, and two derivatives increased cell death rate by up to 40%. The structure–activity relationship (SAR) study revealed an amide group with a long alkyl chain and benzene ring with a p-CF3 group could be important for efficiency. With theoretical ADMET studies of pyrazolopyrazine derivatives, pharmacokinetic phases were predicted to be suitable. Graphic abstract: [Figure not available: see fulltext.].
Design, synthesis and biological evaluation of novel pyrazolochalcones as potential modulators of PI3K/Akt/mTOR pathway and inducers of apoptosis in breast cancer cells
Shaik, Anver Basha,Rao, Garikapati Koteswara,Kumar, G. Bharath,Patel, Nibeditha,Reddy, Vangala Santhosh,Khan, Irfan,Routhu, Sunitha Rani,Kumar, C. Ganesh,Veena, Immadi,Chandra Shekar, Kunta,Barkume, Madan,Jadhav, Shailesh,Juvekar, Aarti,Kode, Jyoti,Pal-Bhadra, Manika,Kamal, Ahmed
, p. 305 - 324 (2017/08/14)
Cancer has been established as the “Emperor of all maladies”. In recent years, medicinal chemistry has focused on identifying novel anti-cancer compounds; though discovery of these compounds appears to be a herculean task. In present study, we synthesized
