Journal of Medicinal Chemistry

OCT 23, 2026 · JOURNAL ARTICLE

Evaluation and an Exploratory Human Study of 99mTc-Labeled PSMA-Targeting Agents with Reduced Renal Uptake via Proline Incorporation

Journal of Medicinal Chemistry

Abstract Excessive renal uptake of prostate-specific membrane antigen (PSMA)-targeted radiopharmaceuticals remains a major challenge in prostate cancer (PCa) detection and therapy.

OCT 22, 2026 · JOURNAL ARTICLE

Design and Biological Evaluation of a Potent Dual PARP and BRD4 Inhibitor for Tumor Therapy via Disrupting HRR and BRD4-cJUN-CCL2 Axis

Journal of Medicinal Chemistry

Abstract Inducing homologous recombination repair (HRR) deficiency is an attractive strategy to expand the therapeutic scope of PARP inhibitors. Since BRD4 inhibition impairs HRR f

OCT 22, 2026 · JOURNAL ARTICLE

Imidazo[1,2- a ]pyrazine Derivatives as Dual A2A/A2B Adenosine Receptor Antagonists Enhancing Anti-PD-1 Antibody Therapy in Colorectal Cancer

Journal of Medicinal Chemistry

Abstract Adenosine signaling through A2A and A2B adenosine receptors (ARs) suppresses antitumor immunity and promotes tumor progression, limiting immune checkpoint blockade in micr

OCT 20, 2026 · JOURNAL ARTICLE

Design, Synthesis, and Biological Evaluation of Novel Benzimidazole Derivatives as Dual PI3K/HDAC8 Inhibitors with Potent Anti-Cervical Cancer Activity In Vivo

Journal of Medicinal Chemistry

Abstract The dual inhibition of phosphatidylinositol 3-kinase (PI3K) and histone deacetylase 8 (HDAC8) has emerged as a promising strategy for cervical cancer (CC) therapy. We synt

OCT 19, 2026 · JOURNAL ARTICLE

Evaluation of Cytotoxic Potential of Water-Soluble Photosensitive Pincer-Copper Complexes

Journal of Medicinal Chemistry

Abstract Herein, the synthesis and characterization of four new water-soluble pincer-copper complexes of the type (R2NNN)CuCl2 (R = C6H5, p-OMe-C6H4, p-Me-C6H4, and p-F-C6H4) based

OCT 19, 2026 · JOURNAL ARTICLE

FGFR3 Selectivity in Drug Discovery: Biological Rationale, Design Strategies, and Therapeutic Potential

Journal of Medicinal Chemistry

Abstract Fibroblast growth factor receptor 3 (FGFR3) gain-of-function alterations drive a spectrum of conditions, including cancers and skeletal dysplasias, making FGFR3 an attract

OCT 17, 2026 · JOURNAL ARTICLE

Dual Peptide Modification via Isopeptide Bonding and Lipidation Boosts Antifungal Activity

Journal of Medicinal Chemistry

Abstract The rapid rise in drug-resistant infectious diseases urgently demands new therapeutic strategies, particularly against fungi. Antimicrobial peptides (AMPs) are key effecto

OCT 12, 2026 · JOURNAL ARTICLE

Developing a Ferric(III) Agent for Targeted Inhibition of Growth and Metastasis of Triple-Negative Breast Cancer Based on Human Serum Albumin by Chemodynamic Therapy-Driven Synergistic Therapy

Journal of Medicinal Chemistry

Abstract Triple-negative breast cancer (TNBC) remains challenging due to its aggressiveness and the lack of targeted therapies. In this study, we proposed designing a ferric (Fe) a