Semisynthesis of Forsyshiyanine A and a Derivative with Significant Anti-Pancreatic Cancer Activity

  • J Nat Prod. 2025 Nov 28;88(11):2781-2788. doi: 10.1021/acs.jnatprod.5c01178.
Saad Y Rfaish  1 ,  Antonio Fernández  1 ,  María C Ramos  2 ,  Thomas A Mackenzie  2 ,  José Justicia  1 ,  Rachid Chahboun  1
Affiliations
  • 1. Departamento de Química Orgánica, Facultad de Ciencias, Instituto de Biotecnología, Universidad de Granada, 18071 Granada, Spain.
  • 2. Fundación MEDINA, Av. Conocimiento 34, Health Sciences Technology Park, 18016 Granada, Spain.
PMID: 41183481 DOI: 10.1021/acs.jnatprod.5c01178
Abstract

Forsyshiyanine A (8), a trinorditerpene alkaloid isolated from Forsythia suspensa exhibiting in vitro anti-inflammatory and Antiviral activities, has been synthesized for the first time from trans-communic acid (12a) and labdane cupressic acid (13). Furthermore, a series of derivatives were efficiently prepared and screened for cytotoxic activities against five human tumoral cell lines. Derivative 25 showed cytotoxicity (IC50 = 6.5 μM) against the Mia PaCa-2 pancreatic Cancer cell line, making it an interesting candidate for future structure-activity relationship (SAR) investigations.

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