Work

Structural Modification of Sesquiterpene Lactones via Michael Addition: Improved Bioactivity and Pharmacokinetics

Year: 2026

Type: article

Abstract: Sesquiterpene lactones (SLs) are privileged medicinal scaffolds, offering potent bioactivities driven by their reactive α-methylene-γ-lactone motif. This review highlights the literature published up to the first half of 2026, detailing the synthetic methodologies utilized to optimize SLs via Michael addition. We critically evaluate how these structural transformations translate into biological and pharmacokinetic improvements. Specifically, the resulting Michael adducts achieve significantly enhanced solubility in aqueous media and highly refined drug-target interactions. Addressing a clear literature gap unaddressed since earlier foundational reviews, this focus review highlights the literature published up to the first half of 2026. By explicitly correlating synthetic strategies with pharmacological outcomes, such as enhanced efficacy and target specificity, this review provides medicinal chemists with a robust framework to accelerate the development of next-generation SL-based therapeutics.

Source: International Journal of Molecular Sciences

DOI: 10.3390/ijms27167374

Authors: Min Woo Ha, Jayun Kang, Sumi Lee, Seung-Mann Paek

Institutions: Jeju Research Institute, Jeju National University, Jeonbuk National University, Gyeongsang National University

Language: English

Topic: Sesquiterpenes and Asteraceae Studies

Subfield: Cancer Research

Field: Biochemistry, Genetics and Molecular Biology

Domain: Life Sciences

Open Access status: gold

Estimated APC paid: $3,499

Funder: Ministry of Education