Nitrogen Containing Heterocycles as Anticancer Agents: A Medicinal Chemistry Perspective

Abstract

Cancer is one of the major healthcare challenges across the globe. Several anticancer drugs are available on the market but they either lack specificity or have poor safety, severe side effects, and suffer from resistance. So, there is a dire need to develop safer and target-specific anticancer drugs. More than 85% of all physiologically active pharmaceuticals are heterocycles or contain at least one heteroatom. Nitrogen heterocycles constituting the most common heterocyclic framework. In this study, we have compiled the FDA approved heterocyclic drugs with nitrogen atoms and their pharmacological properties. Moreover, we have reported nitrogen containing heterocycles, including pyrimidine, quinolone, carbazole, pyridine, imidazole, benzimidazole, triazole, β-lactam, indole, pyrazole, quinazoline, quinoxaline, isatin, pyrrolo-benzodiazepines, and pyrido[2,3-d]pyrimidines, which are used in the treatment of different types of cancer, concurrently covering the biochemical mechanisms of action and cellular targets.

Antioxidant activity of novel nitrogen scaffold with docking investigation and correlation of DFT stimulation

“…20 Moreover, pyridines are important building blocks in pharmaceuticals due to their analgesic, anti-inammatory, antitumor, and antiviral properties. 21 Likewise, the O-containing heterocycles display a variety of pharmacological properties, including antibacterial, anti-HIV, anti-malaria, anti-cancer, anti-tubercular, and diabetic properties. [22][23][24][25][26] The iso-oxazolines exhibit antibacterial, antifungal, anticancer, and anti-inammatory properties.…”

NRF2 Activation by Nitrogen Heterocycles: A Review

“…The applications of nitrogen heterocycles in drug design and development have been reviewed by [ 2 ]. Many of them have been found to possess anticancer activities and good physicochemical properties [ 3 ]. Thus, the presence of an N -based heterocyclic moiety may improve the adsorption, distribution, metabolism and excretion (ADME) and toxicological properties of drug molecules.…”

New 1,3,4-thiadiazoles as potential anticancer agents: pro-apoptotic, cell cycle arrest, molecular modelling, and ADMET profile

“…The KBr wafer approach was used to record IR-spectra using a Pye Unicam SP1200 spectrophotometer (Pye Unicam Ltd., Cambridge, UK). 1 H-NMR spectra were obtained on a Bruker Avance (III) utilizing a Varian-Gemini 400 MHz and an internal standard of tetramethyl silane (chemical shis in scale d ppm ), whereas 13 C-NMR spectra were obtained at 100 MHz. In deuterated dimethyl sulfoxide, TMS was used as an internal standard (DMSO-d 6 ).…”