Drug intelligence / Profile preview

aspirin-sulfonamide hybrid 3k

Development stage
Preclinical
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
01

Overview

Aspirin-sulfonamide hybrid 3k is a novel small molecule compound designed as a structural modification of aspirin, incorporating a sulfonamide moiety with a bromothiophene group. This hybrid was synthesized to enhance the anticancer efficacy of aspirin. In preclinical studies, it demonstrated potent cytotoxicity against human non-small-cell lung cancer (A549) cells, with an IC50 of 36 μM—over 33-fold more potent than parent aspirin. Mechanistic investigations revealed that hybrid 3k induces apoptosis and causes cell cycle arrest at the G0/G1 phase in A549 cells. Molecular docking and biochemical assays indicate that its anticancer activity is likely mediated by inhibition of cyclooxygenase-2 (COX-2). The compound represents an effort to expand the antitumor potential of traditional NSAIDs through rational drug design[1][2].

Other names
hybrid 3khybrid3khybrid-3k
02

Targets

PTGS2 (Prostaglandin-Endoperoxide Synthase 2)

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