1236153-23-3

Upstream product

• 13105-72-1 2-(N-methyl-N-prop-2-yn-1-ylamino)ethanol 
• 134414-14-5 11beta-(4-hydroxyphenyl)-estra-4,9-diene-3,17-dione 
• 17878-42-1 4-((trimethylsilyl)oxy)phenyl magnesium bromide 
• 17878-44-3 (4-bromophenoxy)trimethylsilane 

Downstream Products

• 1236153-24-4 (8S,9R,11S,13S,14S)-11-(4-(2-([2-propynyl]methylamino)ethoxy)phenyl)-7,8,9,11,12,13,14,15,16,17-decahydro-13-methyl-17-oxo-6H-cyclopenta[a]phenanthren-3-yl acetate 
• 1236153-25-5 (8S,9R,11S,13S,14S,17S)-11-(4-(2-([2-propynyl]methylamino)ethoxy)phenyl)-7,8,9,11,12,13,14,15,16,17-decahydro-13-methyl-6H-cyclopenta[a]phenanthrene-3,17-diol 

Relevant academic research and scientific papers

Synthesis and preliminary evaluation steroidal antiestrogen-geldanamycin conjugates

Three novel steroidal antiestrogen-geldanamycin conjugates were prepared using a convergent strategy. The antiestrogenic component utilized the 11β-(4-functionalized-oxyphenyl) estradiol scaffold, while the geldanamycin component was derived by replacement of the 17-methoxy group with an appropriately functionalized amine. Ligation was achieved in high yield using azide alkyne cyclization reactions. Evaluation of the products against two breast cancer cell lines indicated that the conjugates retained significant antiproliferative activity.

STEROIDAL ANTI-HORMONE HYBRIDS

Disclosed are novel compounds and compositions for inhibition of androgen and estrogen receptor signaling, methods for inhibiting androgen signaling, methods for inhibiting estrogen signaling, methods for inhibiting the interaction between a co-regulatory protein and an androgen or estrogen receptor, and methods for treating cancer.