Retrospective Benchmarking of Previously Modeled Coumarin–Pyrimidine Structures Against MDA-MB-231/MCF-10A Cellular Activity

This study retrospectively evaluates agreement between target-level molecular-modeling rankings from a previously published coumarin–pyrimidine library and an available cellular dataset for 14 experimentally evaluated compounds with documented structure assignments. Laboratory-reported MDA-MB-231 and MCF-10A IC50 values from multi-concentration MTT testing were compared with published AutoDock Vina scores using rank-based analyses. Compound 5e had the lowest laboratory-reported MDA-MB-231 IC50 (12.4 ± 0.2 µM; n = 2) and the largest descriptive selectivity index (7.75); this ratio is specific to the MDA-MB-231/MCF-10A comparison and is not interpreted as evidence of general tumor selectivity. Docking rankings showed weak correspondence with cellular potency, and no docking–phenotype association remained statistically significant after Benjamini–Hochberg adjustment. No basic 2D descriptor showed a compelling adjusted association. Complete 1H/13C NMR and validated HRMS documentation, quantitative purity measurements, and the complete full-series MTT raw export are not available; structure-dependent and potency claims are therefore interpreted cautiously. Overall, the analysis demonstrates limited cross-endpoint transferability between target-level docking rankings and whole-cell activity in the MDA-MB-231/MCF-10A dataset, without establishing a validated structure–activity relationship, generalized TNBC activity, apoptosis induction, a BCL-2 mechanism, or translational efficacy.

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Publication Details

Journal
Biology
Published
2026-11-04
DOI
https://doi.org/10.3390/biology15211999
Primary Topic
Computational Drug Discovery Methods
Type
article
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article

Retrospective Benchmarking of Previously Modeled Coumarin–Pyrimidine Structures Against MDA-MB-231/MCF-10A Cellular Activity

Marcin Gackowski, Łukasz Szeleszczuk, Piotr Kośliński, Veda B. Hacholli et al.
Biology
Computational Drug Discovery Methods
article

Retrospective Benchmarking of Previously Modeled Coumarin–Pyrimidine Structures Against MDA-MB-231/MCF-10A Cellular Activity

Marcin Gackowski, Łukasz Szeleszczuk, Piotr Kośliński, Veda B. Hacholli, Abhishek Kumar
article en

Abstract

This study retrospectively evaluates agreement between target-level molecular-modeling rankings from a previously published coumarin–pyrimidine library and an available cellular dataset for 14 experimentally evaluated compounds with documented structure assignments. Laboratory-reported MDA-MB-231 and MCF-10A IC50 values from multi-concentration MTT testing were compared with published AutoDock Vina scores using rank-based analyses. Compound 5e had the lowest laboratory-reported MDA-MB-231 IC50 (12.4 ± 0.2 µM; n = 2) and the largest descriptive selectivity index (7.75); this ratio is specific to the MDA-MB-231/MCF-10A comparison and is not interpreted as evidence of general tumor selectivity. Docking rankings showed weak correspondence with cellular potency, and no docking–phenotype association remained statistically significant after Benjamini–Hochberg adjustment. No basic 2D descriptor showed a compelling adjusted association. Complete 1H/13C NMR and validated HRMS documentation, quantitative purity measurements, and the complete full-series MTT raw export are not available; structure-dependent and potency claims are therefore interpreted cautiously. Overall, the analysis demonstrates limited cross-endpoint transferability between target-level docking rankings and whole-cell activity in the MDA-MB-231/MCF-10A dataset, without establishing a validated structure–activity relationship, generalized TNBC activity, apoptosis induction, a BCL-2 mechanism, or translational efficacy.

BiologyVol. 15(21)
Nitte University (IN), Medical University of Warsaw (PL), Nicolaus Copernicus University (PL)
Openalex Percentile: Top 16%
Computational Drug Discovery Methods
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