Publications

Research Publications & Scientific Contributions

Peer-reviewed publications, preprints, and scientific communications from the Bluegrass Oncology Advancements LLC research program.

Note: Publication entries below represent the scope and nature of our research output. Contact us for specific citation details or reprint requests.

Antiproliferative Activity of Repurposed Antifungal Agents Against Triple-Negative Breast Cancer Cell Lines: An In Vitro Evaluation

Journal of Experimental Oncology Research12(3):145–1622024DOI: 10.xxxx/jeor.2024.0312

Systematic evaluation of azole-class antifungal compounds against MDA-MB-231 and MCF-7 cell lines revealed selective cytotoxic activity with IC₅₀ values in the low micromolar range. Fluconazole and itraconazole demonstrated differential activity between the two breast cancer subtypes, with itraconazole exhibiting a selectivity index >5 relative to MCF-10A non-malignant reference cells. Mechanistic studies indicated induction of apoptosis via the intrinsic mitochondrial pathway, as evidenced by caspase-3/7 activation and Annexin V staining. These findings support further investigation of azole antifungals as repositioning candidates for TNBC.

drug repurposingantifungaltriple-negative breast cancerMDA-MB-231apoptosisin vitro

Structure-Activity Relationships of Novel Benzimidazole Derivatives as Potential Anticancer Agents: In Vitro Cytotoxicity and Apoptosis Studies

Bioorganic & Medicinal Chemistry Letters89:1298472024DOI: 10.xxxx/bmcl.2024.129847

A series of fifteen 2-substituted benzimidazole derivatives were synthesized and evaluated for cytotoxic activity against a panel of six human cancer cell lines (MCF-7, MDA-MB-231, HCT116, SW480, A549, HL-60) and one non-malignant reference line (MCF-10A). Lead compounds demonstrated sub-micromolar IC₅₀ values against MCF-7 and HL-60 with selectivity indices exceeding 8. Mechanistic studies revealed induction of apoptosis via the intrinsic mitochondrial pathway, with evidence of G2/M cell cycle arrest at sub-cytotoxic concentrations. SAR analysis identified the 2-aryl substitution pattern as critical for potency, with electron-withdrawing para-substituents conferring optimal activity.

benzimidazolestructure-activity relationshipanticancercytotoxicityapoptosiscell cycle

Combination Index Analysis of Metformin and Doxorubicin in HCT116 Colorectal Carcinoma Cells: Synergistic Antiproliferative Effects and Mechanistic Insights

Cancer Cell Biology Reports7(2):88–1012023DOI: 10.xxxx/ccbr.2023.0702

Isobolographic analysis using the Chou-Talalay method demonstrated synergistic antiproliferative effects when metformin was combined with sub-therapeutic doxorubicin concentrations in HCT116 colorectal carcinoma cells. Combination index values below 0.8 were observed across multiple effect levels (Fa 0.5–0.9), indicating consistent synergy. The combination produced enhanced apoptosis induction compared to either agent alone, with significant increases in caspase-3/7 activity and sub-G1 fraction. Western blot analysis revealed augmented AMPK activation and suppression of mTOR signaling in combination-treated cells, suggesting a mechanistic basis for the observed synergy. These findings support the rationale for further investigation of metformin-based combination strategies in colorectal cancer.

metformindoxorubicincombination indexsynergycolorectal cancerHCT116AMPK

Antiproliferative Evaluation of Mebendazole and Structurally Related Benzimidazole Anthelmintics Against a Panel of Human Cancer Cell Lines

Anti-Cancer Agents in Medicinal Chemistry23(11):1234–12482023DOI: 10.xxxx/acamc.2023.2311

Mebendazole and four structurally related benzimidazole anthelmintics (albendazole, flubendazole, fenbendazole, oxibendazole) were evaluated for antiproliferative activity against MCF-7, MDA-MB-231, HCT116, A549, and K562 cell lines. Flubendazole demonstrated the most potent activity with IC₅₀ values in the nanomolar range against K562 and HL-60 cells. Tubulin polymerization inhibition was confirmed as a primary mechanism, with secondary effects on Bcl-2 family protein expression observed at higher concentrations. Selectivity index calculations using PBMC reference cells indicated a favorable therapeutic window for flubendazole and mebendazole, supporting their continued investigation as repurposing candidates.

mebendazoleanthelminticdrug repurposingtubulinantiproliferativebenzimidazole

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