Here, we explored the benzothiopyranoindole scaffold to develop antiproliferative agents with a polypharmacological profile targeting both G-quadruplex (G4)-structures and Topoisomerase (Topo) I enzyme. In a preliminary optimization phase, compound was selected from an in-house collection as a suitable lead for the rational development of a small library of analogs (-). When assayed in NIH's NCI-60 Human Cancer Cell Line In Vitro Screen Program, compound and its demethylated analogue showed significant antiproliferative/cytotoxic activity.
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January 2025
Introduction: Obesity is one of the biggest modern health issues worldwide. Owing to the failure of both behavioral and pharmacological measures, the surgical approach has been established as the main conduct to follow, with bariatric surgery being one of the most effective and safe procedures. One of the bases for the optimal analgesic strategy is the use of adjuvants during the perioperative period.
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