Antihormonal potential of selected D-homo and D-seco estratriene derivatives

• Published in: Steroids Vol. 97; pp. 45 - 53
• Main Authors: Jovanović-Šanta, Suzana S., Petri, Edward T., Klisurić, Olivera R., Szécsi, Mihály, Kovačević, Radmila, Petrović, Julijana A.
• Format: Journal Article
• Language: English
• Published: NEW YORK Elsevier Inc 01.05.2015; Elsevier
• Subjects: 16,17-Seco-estratriene derivatives; Animals; Antiestrogens; Aromatase - metabolism; Biochemistry & Molecular Biology; Crystallography, X-Ray; D-homo-estratriene derivatives; Dose-Response Relationship, Drug; Endocrinology & Metabolism; Enzyme Inhibitors - chemical synthesis; Enzyme Inhibitors - chemistry; Enzyme Inhibitors - pharmacology; Estrenes - chemical synthesis; Estrenes - chemistry; Estrenes - pharmacology; Estrogens - biosynthesis; Female; Homosteroids - chemical synthesis; Homosteroids - chemistry; Homosteroids - pharmacology; Hormone Antagonists - chemical synthesis; Hormone Antagonists - chemistry; Hormone Antagonists - pharmacology; Life Sciences & Biomedicine; Models, Molecular; Molecular Conformation; Molecular docking studies; Rats; Rats, Wistar; Science & Technology; Secosteroids - chemical synthesis; Secosteroids - chemistry; Secosteroids - pharmacology; Stereoisomerism; Steroid 17-alpha-Hydroxylase - antagonists & inhibitors; Steroid 17-alpha-Hydroxylase - metabolism; Steroidogenesis enzymes inhibitors and activators; Structure-Activity Relationship; X-ray (XRD); Molecular docking studies; Steroidogenesis enzymes inhibitors and activators; 16,17-Seco-estratriene derivatives; Antiestrogens; D-homo-estratriene derivatives; X-ray (XRD); BREAST-CANCER; PLATFORM; BIOLOGICAL-ACTIVITY; RECEPTOR; AROMATASE INHIBITORS; 17-ALPHA-HYDROXYLASE/C-17,C-20-LYASE

•New D-homo and 16,17-seco-estratriene compounds were synthesised and characterized.•Docking studies were performed for protein targets of steroidal anti-cancer drugs.•Estrogen and antiestrogen activity of the new compounds was determined.•X-ray structural analysis of a new compound was performed.•S...