Anti-inflammatory effects of butadiene Diels–Alder adducts to some 1-dehydroglucocorticoids in rats

Sharifzadeh, Mohammad; Ramazani, Farid; Shamsa, Fazel

doi:10.1016/j.ejps.2003.12.008

Cited by 2 publications

(1 citation statement)

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“…The derivatives of androgens, estrogens, and glucocorticoids have been continuously developed in order to increase potency and reduce side effects . Ferrocene [Fe(C 2 H 5 )] is an organometallic and multielectron transfer compound, which can be used as a precursor for the preparation of organometallic complexes, gasoline additives to prevent “knocking” in motors, anion and cation sensors, − DNA biosensors, and mediators of electron transfer between active sites of oxidoreductases enzyme . It is also used as catalysts for the oxidative organic synthesis, molecular chemistry, water treatment, and photolytic chemistry. , Several pharmacological activities of ferrocene derivatives have been reported.…”

Section: Introductionmentioning

confidence: 99%

Novel Ferrocenic Steroidal Drug Derivatives and Their Bioactivities

Manosroi¹,

Rueanto²,

Boonpisuttinant³

et al. 2010

J. Med. Chem.

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Seven novel ferrocenic derivatives, compounds 1-7, were synthesized from steroidal drugs by Aldol condensation reaction. The derivatives were purified by chromatography, and their structures were determined on the basis of HR-ESI-MS and two-dimensional NMR spectroscopy. The purity of all derivatives was more than 95%. Compounds 1-5 demonstrated anti-proliferative activity on HeLa cell line by SRB assay more than their parent compounds. All seven derivatives showed anti-oxidative activities evaluated by DPPH scavenging and metal ion chelating, while their parent compounds gave no activity. Compound 1 indicated the most potent anti-proliferative activity similar to doxorubicin, with the GI(50) at 0.223 +/- 0.014 microg/mL. Compounds 6 and 7 demonstrated similar potent in vivo anti-inflammatory to their parent compounds (prednisolone and hydrocortisone) at 80.99 +/- 13.5 and 68.24 +/- 10.4% edema inhibition, respectively. This study has suggested that the novel compound 1 was the most potential derivative that can be further developed for cancer treatment.

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