Related Experiment Video
Updated: Mar 26, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Structure-activity & structure-toxicity relationship study of salinomycin diastereoisomers and their benzoylated
Wenxuan Zhang1, Jun Wu2, Bo Li1
1State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100050, China. ws@imm.ac.cn.
Abstract:
Salinomycin diastereoisomers and their benzoylated derivatives were synthesized and evaluated for both antiproliferative activity and neurotoxicity in vitro. The results indicated that the stereoscopic configurations of the spiro C17 and C21 atoms as well as the benzoyl groups of O-20 on the rigid B/C/D spiro-ketal structures are crucial for biological activity and neural toxicity. In general, there are some positive correlations between the antiproliferative activity and neurotoxicity in these salinomycin derivatives, indicating possibly similar mechanisms of action.
Related Concept Videos
Structure-Activity Relationships and Drug Design
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence...
Adrenergic Agonists: Chemistry and Structure-Activity Relationship
Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
Separation of...
Directing and Steric Effects in Disubstituted Benzene Derivatives
Preparation and Reactions of Sulfides
Nucleophilic Aromatic Substitution of Aryldiazonium Salts: Aromatic SN1
In the Sandmeyer reaction, for example, the diazonio group is replaced by a chloro, bromo,...
Electrophilic Aromatic Substitution: Sulfonation of Benzene

