Sulfonamides and sulfonylated derivatives as anticancer agents

Angela Casini, Andrea Scozzafava, Antonio Mastrolorenzo, Claudiu T. Supuran

Research output: Contribution to journalArticleAcademicpeer-review

269 Citations (Scopus)


The sulfonamides constitute an important class of drugs, with several types of pharmacological agents possessing antibacterial, anti-carbonic anhydrase, diuretic, hypoglycemic and antithyroid activity among others. A host of structurally novel sulfonamide derivatives have recently been reported to show substantial antitumor activity in vitro and/or in vivo. Although they have a common chemical motif of aromatic/heterocyclic sulfonamide, there are a variety of mechanisms of their antitumor action, such as carbonic anhydrase inhibition, cell cycle arrest in the G1 phase, disruption of microtubule assembly, functional suppression of the transcriptional activator NF-Y, and angiogenesis (matrix metalloproteinase, MMP) inhibition among others. Some of these compounds selected via elaborate preclinical screenings or obtained based on computer-aided drug design, are currently being evaluated in clinical trials. This review summarizes recent classes of sulfonamides and related sulfonyl derivatives disclosed ultimately as effective tumor cell growth inhibitors, or for the treatment of different types of cancer.
Original languageEnglish
Pages (from-to)55-75
Number of pages21
JournalCurrent cancer drug targets
Issue number1
Publication statusPublished - 1-Dec-2002
Externally publishedYes


  • 1 (3,4 dichlorophenyl) 3 (2,3 dihydrobenzofuran 5 ylsulfonyl)urea
  • 5 chlorosulfaquinoxaline
  • acetazolamide
  • amprenavir
  • antineoplastic agent
  • beta tubulin
  • carbonate dehydratase
  • coumarin derivative
  • er 34410
  • estrone 3 sulfamate
  • estrone sulfate
  • furosemide
  • heterocyclic compound
  • indisulam
  • matrix metalloproteinase
  • matrix metalloproteinase inhibitor
  • n [2 [(4 hydroxyphenyl)amino] 3 pyridinyl] 4 methoxybenzenesulfonamide
  • neutrophil collagenase
  • nuclear factor Y
  • sulfathiazole
  • sulfonamide
  • sulfonylurea derivative
  • sulofenur
  • tamoxifen derivative
  • torasemide
  • transcription factor
  • unclassified drug
  • angiogenesis
  • animal cell
  • antibacterial activity
  • antineoplastic activity
  • cancer chemotherapy
  • cancer classification
  • cell cycle G1 phase
  • clinical trial
  • computer aided design
  • diuresis
  • drug classification
  • drug design
  • drug efficacy
  • drug mechanism
  • drug structure
  • enzyme inhibition
  • growth inhibition
  • human
  • human cell
  • hypoglycemia
  • microtubule assembly
  • microtubule organizing center
  • nonhuman
  • review
  • structure analysis
  • thyroid function
  • transcription regulation
  • tumor growth

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