. Author manuscript; available in PMC: 2022 May 3.

Published in final edited form as: Angew Chem Int Ed Engl. 2021 Mar 26;60(19):10547–10551. doi: 10.1002/anie.202015422

Table 1:

Replacement of the isopropyl group, IC₅₀ determined using fluorescence polarization (FP) assay. Compounds were incubated with Hsp90α/β and FITC-GDA in triplicate, and ± SD was measured.


Compound	R group	IC₅₀ Hsp90α (μM)^(a)	IC₅₀ Hsp90β (μM)^(a)
4	Cl	4.69 ± 0.27	>100
5	Br	2.73 ± 0.19	>100
6	I	>100	>100
7	CF₃	7.90 ± 1.18	>100
8		2.62 ± 0.08	>100
9		0.65 ± 0.04	12.92 ± 1.92
10		>50	>50
11		>25	>50
12		4.87 ± 0.29	>100