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. Author manuscript; available in PMC: 2012 Dec 7.
Published in final edited form as: ChemMedChem. 2010 Jul 5;5(7):979–985. doi: 10.1002/cmdc.201000146

Figure 2.

Figure 2

C-terminal protection of the HIF-1α pentapeptide provides improved degradation of the ER by PROTACs linked at any position on estradiol. A. O-17 (2 and 2*) and C-16 (13 and 14) derivatives of E2-based PROTACs with the benzyl protected HIF-1α pentapeptide (2 and 13) are more effective in degrading the endogenous ER than benzyl deprotected PROTACs (2* and 14). B. A similar pattern was observed for the C-7 derivative of E2-based PROTAC, as the benzyl protected compounds (13 and 24) showed greater ER degradation than the deprotected compound (14).