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"Retraction:Synthesis

  • Ali Bahadur*
  • , Shahid Iqbal
  • , Saiqa Muneer
  • , Hashem O. Alsaab
  • , Nasser S. Awwad
  • , Hala A. Ibrahium
  • *Corresponding author for this work

Research output: Journal PublicationArticlepeer-review

Abstract

The sulfonamide-based thiadiazole derivatives (STDs) with different hydrophobic/hydrophilic substitutions were synthesized to investigate their potentials in carbonic anhydrase inhibition (CAI). The CAI activity of the STDs (4a-4h) and the mechanism of the inhibition kinetics were determined. STD 4f contained both methoxy and Cl groups at benzene ring in STD 4f showed the lowest IC50 value. The molecular docking study confirmed that STDs bind strongly with the active sites of the target protein PDBID 1V9E. With the help of Lineweaver-Burk plots, inhibition kinetics of PDBIR 1V9E protein with STDs were determined. Cytotoxicity was checked against human keratinocyte cell lines and the anticancer properties were determined against MCF-7 cell lines. The electrochemical method was used to investigate the binding study with DNA and CA enzymes. Anticancer studies showed that STDs have weak bonding ability to DNA and strong binding ability with CA. It is concluded that anticancer activity is through CAI rather than by DNA binding.

Original languageEnglish
Article number128520
JournalBioorganic and Medicinal Chemistry Letters
Volume57
DOIs
Publication statusPublished - 1 Feb 2022
Externally publishedYes

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

  1. SDG 3 - Good Health and Well-being
    SDG 3 Good Health and Well-being

Free Keywords

  • Anticancer studies
  • Carbonic anhydrase
  • Inhibition evaluations
  • Sulfonamides
  • Thiadiazole

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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