Repositioning Established Compounds for Oncological Applications
Our drug repurposing initiative systematically evaluates public-domain, off-patent, and investigational compounds for previously uncharacterized or underexplored anticancer activity using validated in vitro assay platforms.
Why Drug Repurposing?
Drug repurposing — the identification of new therapeutic applications for existing pharmacological agents — represents a scientifically compelling and resource-efficient research strategy. Established compounds possess well-characterized pharmacological profiles, known safety data, and in many cases, existing manufacturing infrastructure, making them attractive candidates for repositioning into new therapeutic contexts.
In the oncology context, numerous public-domain compounds originally developed for non-oncological indications have demonstrated unexpected anticancer activity in preclinical studies. Our research program systematically investigates these candidates using rigorous in vitro methodology to characterize their antiproliferative activity, selectivity profiles, and potential mechanisms of action.
Evaluation Methodology
Literature Review & Candidate Selection
Systematic review of published literature to identify compounds with reported or hypothesized anticancer activity. Candidate selection is guided by mechanistic rationale, structural features, and availability of pharmacological data.
Primary Cytotoxicity Screening
Initial evaluation of antiproliferative activity across the full cell line panel using MTT or SRB assay at a fixed concentration range. Compounds demonstrating ≥50% growth inhibition at ≤100 μM advance to dose-response evaluation.
IC₅₀ Determination & Selectivity
Full dose-response analysis for active compounds with IC₅₀ determination by non-linear regression. Selectivity index calculation using non-malignant reference cell lines to assess therapeutic window.
Mechanistic Investigation
Active compounds with favorable selectivity profiles advance to mechanistic studies including apoptosis analysis, cell cycle assessment, and target-specific pathway interrogation by Western blot.
Therapeutic Classes Evaluated for Anticancer Repositioning
Antifungal Agents
Azole-class antifungals and polyene macrolides have demonstrated antiproliferative activity in multiple cancer cell line models, potentially through disruption of ergosterol-independent membrane targets and inhibition of CYP enzymes involved in steroid biosynthesis.
Antidiabetic Agents
Biguanide compounds, particularly metformin, have been extensively studied for anticancer activity. Our program evaluates metformin and structurally related compounds for antiproliferative effects and potential synergistic interactions with established cytotoxic agents.
Antiparasitic Agents
Several antiparasitic compounds, including benzimidazole anthelmintics and aminoquinolines, have demonstrated significant anticancer activity in vitro. We evaluate these compounds for cytotoxic activity and investigate potential mechanisms involving tubulin disruption and mitochondrial targeting.
Anti-inflammatory Agents
NSAIDs and corticosteroids with documented effects on inflammatory signaling pathways relevant to cancer biology are evaluated for direct antiproliferative activity and modulation of cancer cell survival signaling.
Cardiovascular Agents
Cardiac glycosides and certain antihypertensive agents have demonstrated anticancer activity through mechanisms including Na+/K+-ATPase inhibition and HIF-1α pathway modulation. We systematically evaluate these compound classes across our cell line panel.