“…A series of metabolic studies suggested that the release of p-chloroaniline from sulofenur was the major cause of the dose-limiting haemolytic anaemia and methaemoglobinaemia observed [64]. Therefore, many analogs were further synthesized with the clear intent to minimize the potential for these troublesome side effects, resulting in the discovery of LY295501.…”
Section: Sulfonylureas With Antitumor Propertiesmentioning
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.
“…A series of metabolic studies suggested that the release of p-chloroaniline from sulofenur was the major cause of the dose-limiting haemolytic anaemia and methaemoglobinaemia observed [64]. Therefore, many analogs were further synthesized with the clear intent to minimize the potential for these troublesome side effects, resulting in the discovery of LY295501.…”
Section: Sulfonylureas With Antitumor Propertiesmentioning
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.
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