2. Academic Validation
  3. Anticancer Activity of Region B Capsaicin Analogs

Anticancer Activity of Region B Capsaicin Analogs

  • J Med Chem. 2023 Apr 13;66(7):4294-4323. doi: 10.1021/acs.jmedchem.2c01594.
Kathleen C Brown 1,  Kushal J Modi 1,  Reagan S Light 1,  Ashley J Cox 1,  Timothy E Long 2,  Rama S Gadepalli 3,  John M Rimoldi 3,  Sarah L Miles 1,  Gary Rankin 1,  Monica Valentovic 1,  Krista L Denning 4,  Maria T Tirona 5,  Paul T Finch 6,  Joshua A Hess 6,  Piyali Dasgupta 1
Affiliations

Affiliations

  • 1 Department of Biomedical Sciences, Toxicology Research Cluster, Joan C. Edwards School of Medicine, Marshall University, 1700 Third Avenue, Huntington, West Virginia 25755, United States.
  • 2 Department of Pharmaceutical Sciences and Research, Marshall University School of Pharmacy, 1538 Charleston Ave, Huntington, West Virginia 25701, United States.
  • 3 Department of Biomolecular Sciences, School of Pharmacy, Thad Cochran Research Center, University of Mississippi, University Avenue, University, Mississippi 38677, United States.
  • 4 Department of Pathology, Joan C. Edwards School of Medicine, Marshall University, 1400 Hal Greer Boulevard, Huntington, West Virginia 25755, United States.
  • 5 Department of Hematology-Oncology, Edwards Cancer Center, Joan C. Edwards School of Medicine, Marshall University, 1400 Hal Greer Boulevard, Huntington, West Virginia 25755, United States.
  • 6 Department of Oncology, Edwards Cancer Center, Joan C. Edwards School of Medicine, Marshall University, 1400 Hal Greer Boulevard, Huntington, West Virginia 25755, United States.
PMID: 37000154 DOI: 10.1021/acs.jmedchem.2c01594
Abstract

The heterocyclic vanilloid compound capsaicin is responsible for the spicy and pungent flavor of chili peppers. Several convergent studies have shown that capsaicin suppresses the growth of multiple human cancers. Apart from capsaicin, natural and synthetic capsaicin-like compounds display growth suppressive activity in human cancers. The pharmacophore of capsaicin is comprised of three regions, namely region A (the aromatic ring), region B (the amide bond), and region C (the side chain). The present manuscript describes the isolation and synthesis of capsaicin analogs which have structural modifications in region B of the molecule. Furthermore, the pharmacokinetic properties, Anticancer activity of region B capsaicin analogs, as well as the signaling pathways (underlying the growth-inhibitory effects of region B capsaicin analogs) have also been described. The discovery of novel, second-generation region B capsaicin analogs may foster the hope of innovative nutrition-based combination therapies in human cancers.

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