The anticancer therapeutic potential of pyrimidine–sulfonamide hybrids

Abstract

Cancer as a devastating malignancy, seriously threatens human life and health, but most chemotherapeutics have long been criticized for unsatisfactory therapeutic efficacy due to drug resistance and severe off-target toxicity. Pyrimidines, including fused pyrimidines, are privileged scaffolds for various biological cancer targets and are the most important class of metalloenzyme carbonic anhydrase inhibitors. Pyrimidine–sulfonamide hybrids can act on different targets in cancer cells simultaneously and possess potent activity against various cancers, revealing that hybridization of pyrimidine with sulfonamide is a promising approach to generate novel effective anticancer candidates. This review aims to summarize the recent progress of pyrimidine–sulfonamide hybrids with anticancer potential, covering papers published from 2020 to present, to facilitate further rational design of more effective candidates.

Explore new quinoxaline pharmacophore tethered sulfonamide fragments as in vitro α‐glucosidase, α‐amylase, and acetylcholinesterase inhibitors with ADMET and molecular modeling simulation

“…Sulfonamides have gained considerable attention from organic chemists due to their broad spectrum of biological activities, encompassing anticonvulsant (Fayed et al, 2021), antimicrobial Ragab, Elsisi, et al, 2022), antidiabetic (Khair-ul-Bariyah et al, 2024, carbonic anhydrase (Tawfik et al, 2024), anticancer activities (Zhang et al, 2024) as EGFR (Eldeeb et al, 2022) and VEGFR-2 inhibitors (Ismail et al, 2023), and antiviral activity targeting RNA polymerase and spike glycoprotein for COVID-19 (El-Kalyoubi et al, 2022), as well as anti-inflammatory properties (Ragab, Eldehna, et al, 2023), and so forth.…”