| abstract |
Galeterone and its C-3 analogs are of substantial interest because of their multi-target anticancer activities, including AR and Mnk degrading activities. Provided are novel procedures for gram-scale, high-yield synthesis of C-3 analogs of galeterone, including 3β-(1 H -imidazole-1-yl)-17-(1 H -benzimidazole-1-yl)-androsta-5,16-diene (galeterone 3β-imidazole) and 3β-(pyridine-4-ylmethoxy)-17-(1 H -benzimidazol-1-yl)androsta-5,16-diene (galeterone 3β-pyridine methoxylate). |