Novel 1<i>H</i>-Pyrazole-3-carboxamide Derivatives: Synthesis, Anticancer Evaluation and Identification of Their DNA-Binding Interaction

Abstract

And it demonstrated more than 50% decrease of the emission intensity of the ethidium bromide-calf thymus DNA (EB-CT-DNA) complex in fluorescence spectra, suggesting that pym-5 could strongly affect the DNA conformation. Furthermore, pym-5 showed the cleavage activity upon the supercoiled plasmid pBR322 DNA in the pBR322 DNA cleavage assay. Our study suggests that DNA may serve as a potential target to these pyrazole derivatives.

Discovery of 4-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-N-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-1H-pyrazole-3-carboxamide (FN-1501), an FLT3- and CDK-Kinase Inhibitor with Potentially High Efficiency against Acute Myelocytic Leukemia

“…In our previous studies, 40 a series of pyrazole-3-carboxamide compounds were synthesized. Recently, it has been identified that compound 26 inhibits FLT3 and CDK2 with IC 50 's of 42.6 nM and 318 nM, respectively.…”

“…In fact, the activation of the FLT3 downstream signal-transduction pathway is an extremely important process in promoting cell proliferation and requires the cooperation of CDKs. Therefore, inhibitors of FLT3 and CDKs can arrest antimitotic signaling pathways and the cell cycle simultaneously, which may exert synergistic effects to increase antileukemic efficiencies. ,, We have reported a series of compounds with moderate CDK2 activities. − Among these compounds, 26 (Figure ) has a certain inhibitory activity against CDK2 (IC 50 : 318.21 nM) and FLT3 (IC 50 : 42.60 nM) and shows moderate activity in MV4-11 (IC 50 : 0.45 μM). Starting from 26 , our group has explored the biological properties of variously substituted 1- H -pyrazole-3-carboxamide derivatives with the aim to find new active compounds and pharmacophores that are potent FLT3 and CDK inhibitors.…”

Dinuclear Nickel(II) and Copper(II) Complexes of 8‐Quinoline‐1H‐pyrazole‐3‐carboxamide: Crystal Structure, Magnetic Properties, and DFT Calculations

“…[1][2][3][4][5][7][8][9][10][11][12][13][14][15][18][19][20][21][23][24][25][26]28,31,32] A very facile method to generate a polydentate ligand with a pending pyrazolate function is the condensation of the commercially available 1H-pyrazole-3-carboxylic acid with suitable amines but remarkably, no such ligands have been reported so far, although this method was used to generate a big number of pharmaceutically active organic molecules. [36][37][38][39][40][41][42] Herein we report on the new pyrazole-based amide ligand, 8-quinoline-1H-pyrazole-3-carboxamide (H 2 qpyzc) that was synthesised in one step from 1H-pyrazole-3-carboxylic acid and 8aminoquinoline in high yield, using a novel and facile synthetic method with no need for further purification. The ligand has been reacted with Cu(OAc) 2 • H 2 O and Ni(OAc) 2 .…”

“…A very facile method to generate a polydentate ligand with a pending pyrazolate function is the condensation of the commercially available 1 H ‐pyrazole‐3‐carboxylic acid with suitable amines but remarkably, no such ligands have been reported so far, although this method was used to generate a big number of pharmaceutically active organic molecules [36–42] …”

Amberlite IR-120H Catalyzed Synthesis of 1,3-Diphenylpyrazolechromenoquinolin-6-one Compounds and Their Biological Evaluation

“…At present, DNA is the most essential target for the design and discovery of drugs in pharmaceutical field and many of the drug molecules currently in clinical trials are because of DNA response to their binding ability and the topological changes in DNA effective to the anticancer, anti-bacterial and therapeutic agents, the DNA binding is in different ways such as intercalation, groove binding and alkylation [3,4]. The translation and transcription process are associated with many enzymes one such is topoisomerase I that involves in many aspects of chromatin topology and DNA metabolism.…”