Details

Autor(en) / Beteiligte

• Richbart, Stephen D
• Friedman, Jamie R
• Brown, Kathleen C
• Gadepalli, Rama S
• Miles, Sarah L
• Rimoldi, John M
• Rankin, Gary O
• Valentovic, Monica A
• Tirona, Maria T
• Finch, Paul T
• Hess, Joshua A
• Dasgupta, Piyali

Titel

Nonpungent N‑AVAM Capsaicin Analogues and Cancer Therapy

Ist Teil von

• Journal of medicinal chemistry, 2021-02, Vol.64 (3), p.1346-1361

Ort / Verlag

United States: American Chemical Society

Erscheinungsjahr

2021

Link zum Volltext

Quelle

MEDLINE

Beschreibungen/Notizen

• Capsaicin displays robust growth-inhibitory activity in multiple human cancers. However, the feasibility of capsaicin as a clinically relevant anticancer drug is hampered by its adverse side effects. This concern has led to extensive research focused on the isolation and synthesis of second-generation nonpungent capsaicin analogues with potent antineoplastic activity. A major class of nonpungent capsaicin-like compounds belongs to the N-acyl-vanillylamide (N-AVAM) derivatives of capsaicin (hereafter referred as N-AVAM capsaicin analogues). This perspective discusses the isolation of N-AVAM capsaicin analogues from natural sources as well as their synthesis by chemical and enzymatic methods. The perspective describes the pharmacokinetic properties and anticancer activity of N-AVAM capsaicin analogues. The signaling pathways underlying the growth-inhibitory effects of N-AVAM capsaicin analogues have also been highlighted. It is hoped that the insights obtained in this perspective will facilitate the synthesis of a second generation of N-AVAM capsaicin analogues with improved stability and growth-suppressive activity in human cancer.