1. Synthesis and antimitotic activity of novel 2-methoxyestradiol analogs—Part II
- Author
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Pemmaraju N. Rao, James W. Cessac, Jamshed H. Shah, Arthur D. Hanson, and James W. Boyd
- Subjects
Models, Molecular ,Stereochemistry ,medicine.medical_treatment ,Clinical Biochemistry ,Molecular Conformation ,Antimitotic Agents ,Biochemistry ,Ovarian hormone ,Steroid ,Structure-Activity Relationship ,chemistry.chemical_compound ,Endocrinology ,Biosynthesis ,Cell Line, Tumor ,medicine ,Humans ,2-Methoxyestradiol ,Computational analysis ,Molecular Biology ,Cells, Cultured ,Cell Proliferation ,Pharmacology ,Estradiol ,Organic Chemistry ,Biological activity ,Methylation ,Tubulin Modulators ,chemistry ,medicine.drug - Abstract
The syntheses and antimitotic activity of several novel 18a-homo-analogs of 2-methoxyestradiol are described. Structural modifications of the parent 2-methoxy-18a-homoestradiol include introduction of unsaturation in the D-ring and methylation of the 17-OH. Of seven analogs synthesized, one has demonstrated superior biological activities compared to 2-methoxyestradiol. The relationship between biological activity and the conformational preference of the 13-ethyl group as determined by computational analysis is discussed.
- Published
- 2008