Ferrocene-based Drug Molecules in Medicinal Chemistry: Comprehensive Insights into their Chemistry, Pharmacology, and Emerging Therapeutic Applications.

Authors

Ramling D Mali, Somnath Bhinge

Published in

Mini reviews in medicinal chemistry. Jul 02, 2026. Epub Jul 02, 2026.

Abstract

Ferrocene, which was a milestone organometallic compound discovered in 1951, remains of interest in medicinal chemistry due to its exceptional stability, redox activity, and ease of functionalization, etc. A variety of pharmacological activities were observed for the Ferrocene derivatives, and several reviews have appeared highlighting the increasing applications of Ferrocene in bio-organometallic chemistry. Novel ferrocene-conjugates of betulin, artemisinin, steroids, and alkaloids were reported, which showed enhanced biological potential. Notably, ferroquine is still in Phase IIb clinical trials, and a number of ferrocene-based anticancer agents demonstrate activity against multidrug resistance. Ferrocene, thus, is an ideal scaffold for next-generation therapeutics with unique structural and redox properties that will overcome current limitations of drug scaffolds.
The methodology consists of a thorough literature survey of chemistry, structural modifications, pharmacological activities, pharmacokinetics, toxicity, and future prospects of compounds involving ferrocene. Recent developments on anticancer, antimalarial, antibacterial, and antiinflammatory applications with detailed Structure Activity Relationship (SAR) were highlighted.
The results show that drug lipophilicity, cellular uptake, and redox activity are improved by the integration of ferrocene, which results in improved efficacy and resistance-overcoming ability. The main pharmaceutical results to date are the preparation of a successful antimalarial drug called ferroquine and a number of ferrocene derivatives with strong anticancer activity. Pharmacokinetic analysis shows good absorption, distribution, and metabolic stability, and the toxicity studies highlight the need for redox tuning to reduce side effects. New approaches such as prodrug design, targeting with nanoparticles, PEGylation, and targeted conjugates help overcome issues of solubility, selectivity, and safety.
Ferrocene-based drug molecules are versatile and promising metallopharmaceuticals. It is hoped that ongoing interdisciplinary research and innovative delivery methods will further extend their clinical utility, especially in the treatment of multidrug resistance and their use in central nervous system and metabolic diseases.
Ferrocene-based drug molecules exhibit remarkable potential in medicinal chemistry with respect to their stability, redox activity, and structural versatility. Their inclusion makes them more lipophilic, increases their uptake into cells, and improves their activity, especially in the fields of anticancer and antimalarial activity, as reflected in the discovery of Ferroquine as a milestone in the clinical field. The targeted delivery and prodrug approaches also further enhance safety and pharmacokinetic properties. In conclusion, ferrocene can be used as a good scaffold in the design of second-generation drugs that can overcome drug resistance.

PMID:
42405407
Bibliographic data and abstract were imported from PubMed on 06 Jul 2026.

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