882223-89-4Relevant academic research and scientific papers
Vilsmeier reagent-mediated synthesis of 6-[(formyloxy)methyl]-pyrazolopyrimidines via a one-pot multiple tandem reaction
Lu, Shi-Han,Liu, Po-Lin,Wong, Fung Fuh
, p. 47098 - 47107 (2015)
A new Vilsmeier reagent-mediated one-pot reaction using 5-(2-chloroacetylamino)pyrazoles as the starting material was developed for the efficient synthesis of 6-[(formyloxy)methyl]-1H-pyrazolo[3,4-d]pyrimidine. This new multiple tandem reaction, involving
Synthesis, in vitro anticancer activity and in silico studies of certain pyrazole-based derivatives as potential inhibitors of cyclin dependent kinases (CDKs)
George, Riham F.,Georgey, Hanan H.,Hassan, Ghaneya S.,Mahmoud, Walaa R.,Mohammed, Esraa Z.,Omar, Farghaly A.
, (2021/09/24)
New diphenyl-1H-pyrazoles were synthesized and screened for CDK2 inhibition where 8d, 9b, 9c, and 9e exhibited promising activity (IC50 = 51.21, 41.36, 29.31, and 40.54 nM respectively) compared to R-Roscovitine (IC50 = 43.25 nM). Furthermore, preliminary anti-proliferative activity screening of some selected compounds on 60 cancer cell lines was performed at the (NCI/USA). Compounds 8a-c displayed promising growth inhibitory activity (mean %GI; 73.74, 94.32 and 74.19, respectively). Additionally, they were further selected by the NCI for five-dose assay, exhibiting pronounced activity against almost the full panel (GI50 ranges; 0.181–5.19, 1.07–4.12 and 1.07–4.82 μM, respectively) and (Full panel GI50 (MG-MID); 2.838, 2.306 and 2.770 μM, respectively). Screening the synthesized compounds 8a-c for inhibition of CDK isoforms revealed that compound 8a exhibited nearly equal inhibition to all the tested CDK isoforms, while compound 8b inhibits CDK4/D1 preferentially than the other isoforms and compound 8c inhibits CDK1, CDK2 and CDK4 more than CDK7. Flow cytometry cell cycle assay of 8a-c on Non-small cell lung carcinoma (NSCL HOP-92) cell line revealed S phase arrest by 8a and G1/S phase arrest by 8b and 8c. Apoptotic induction in HOP-92 cell line was also observed upon treatment with compounds 8a-c. Docking to CDK2 ATP binding site revealed similar interactions as the co-crystallized ligand R-Roscovitine (PDB code; 3ddq). These findings present compounds 8a-c as promising anti-proliferative agents.
Novel aminopyrazole tagged hydrazones as anti-tubercular agents: Synthesis and molecular docking studies
Padmini, Thatavarthi,Bhikshapathi, Darna,Suresh, Kandagatla,Kulkarni, Ravindra,Kamal, Bigala Raj
, p. 344 - 351 (2021/03/08)
Background: Pyrazole derivatives have been reported to possess numerous pharmacological activities viz., anti-inflammatory, antipsychotic, etc. Our group has disclosed that pyrazole benzamides display potent antibacterial and anti-tubercular activities. O
