Design, microwave-mediated synthesis and biological evaluation of novel 4-aryl(alkyl)amino-3-nitroquinoline and 2,4-diaryl(dialkyl)amino-3-nitroquinolines as anticancer agents

Unanticipated Cleavage of 2-Nitrophenyl-Substituted N-Formyl Pyrazolines under Bechamp Conditions: Unveiling the Synthesis of 2-Aryl Quinolines and Their Mechanistic Exploration via DFT Studies

“…NMR and HRMS images were outsourced and recorded at SAIF, Panjab University, Chandigarh, and IIT Ropar, Punjab, respectively, in using CDCl 3 /dimethyl sulfoxide (DMSO) -d 6 as solvent on 400 MHz ( 1 H) and 100 MHz ( 13 C) Bruker Avance NMR spectrometers. 26…”

N-Alkyl-1,5-dideoxy-1,5-imino-l-fucitols as fucosidase inhibitors: Synthesis, molecular modelling and activity against cancer cell lines

“…After docking iso-6FNJ to the fucosidase, an RMSD value of 0.391 Å between the co-crystallized structure and the docked structure indicated that the adopted docking procedure was reliable. [74].…”

Imine/amide–imidazole conjugates derived from 5-amino-4-cyano- N 1-substituted benzyl imidazole: Microwave-assisted synthesis and anticancer activity via selective topoisomerase-II-α inhibition

“…Briefly 2,3-diaminomaleonitrile was treated with CH(OEt) 3 Microwave (MW) assisted organic synthesis [23][24][25][26] is swiftly advancing and is now accepted as a valuable tool to overcome some of the bottlenecks in the drug discovery process and has enhanced the rapid generation of libraries of compounds in lesser time, high yields, proficient and speedy dielectric heating of the reaction mixture in a conserved vessel to temperatures even higher than the boiling point of the solvent. 6,27 In order to determine the optimum reaction conditions for the synthesis of imine-imidazole hybrids (ARK-4-11), a representative reaction of 3 (1 equiv) was carried out with 4-hydroxybenzaldehyde (1 equiv) under various MW reaction conditions. The results are summarized in Table 1.…”

“…3 The scope of molecular hybridization can be clearly exemplified through the US-FDA approved estramustine and successful ongoing of other hybrid molecules that are currently in different phases of clinical trials such as CUDC-101, CBLC-137, PLX3397, E-3810, and CUDC-907. 2 In continuation of our previous efforts towards anticancer drug discovery [4][5][6][7][8][9] and development, 10 we thought of designing hybrid pharmacophores derived from imine-imidazoles and imineamides ( Fig. 1) in which one of the aromatic rings of stilbenes 11,12 / imines (1) or benzamides (2) was substituted with imidazole scaffold, that is, 5-amino-4-cynao-N1-substituted benzyl imidazole (3).…”