Synthesis and aromatase inhibitory activity of some new 16E-arylidenosteroids |
| |
| Institution: | 1. University Institute of Pharmaceutical Sciences, Sector-14, Panjab University, Chandigarh 160 014, India;2. Pharmaceutical and Medicinal Chemistry, Saarland University, Helmholtz Institute for Pharmaceutical Research Saarland (HIPS), Campus C2.3, D-66123 Saarbrücken, Germany;1. Natl Inst Mat Phys, Atomistilor 405A, Magurele, Ilfov, 077125, Romania;2. University of Bucharest, Faculty of Physics, Atomi?tilor 405, 077125 M?gurele-Ilfov, Romania;1. Department of Animal Production, School of Agriculture, Faculty of Agriculture, Forestry & Natural Environment, Aristotle University of Thessaloniki, Thessaloniki, Greece;2. Department of Molecular Biology and Genetics, Democritus University of Thrace, Alexandroupolis 68100, Greece;3. Department of Zoology, School of Biology, Aristotle University of Thessaloniki, Thessaloniki 54124, Greece;1. Department of Physics, Ocean University of China, Qingdao, 266100, China;2. College of Mathematics and Physics, Qingdao University of Science and Technology, Qingdao, 266061, China;1. School of Physics and Electronic Engineering, Sichuan Normal University, Chengdu 610101, China;2. School of Optoelectronic Information, University of Electronic Science and Technology, Chengdu 610054, China |
| |
| Abstract: | A new series of 16E-arylidene androstene derivatives has been synthesized and evaluated for aromatase inhibitory activity. The impact of various aryl substituents at 16 position of the steroid skeleton on aromatase inhibitory activity has been observed. The 16E-arylidenosteroids 6, 10 and 11 exhibited significant inhibition of the aromatase enzyme. 16-(4-Pyridylmethylene)-4-androstene-3,17-dione (6, IC50: 5.2 μM) and 16-(benzo-1,3]dioxol-5-ylmethylene)androsta-1,4-diene-3,17-dione (11, IC50: 6.4 μM) were found to be approximately five times more potent in comparison to aminoglutethimide. |
| |
| Keywords: | |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
