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. Author manuscript; available in PMC: 2017 Aug 21.
Published in final edited form as: J Med Chem. 2015 Apr 17;58(9):3794–3805. doi: 10.1021/jm501984f

Table 2.

SAR of the merged tricyclic indole derivatives for binding to Mcl-1 and Bcl-xL

graphic file with name nihms883364u3.jpg
compd Z n R Ar Mcl-1 Ki (µM)
Bcl-xL		 Bcl-2
16 S 1 H 1-naphthyl 3.0 9.0
17 CH2 1 H 1-naphthyl 4.0 >20
18 0 1 H 1-naphthyl 1.6 12.7
19 S 2 H 1-naphthyl 0.12 >20 3.1
20 CH2 2 H 1-naphthyl 0.31 >20 7.3
21 0 2 H 1-naphthyl 0.11 1.9 5.7
22 S02 2 H 1-naphthyl 0.088 >20
23 SCH2 2 H 1-naphthyl 0.17 7.4 9.9
24 SOCH2 2 H 1-naphthyl 0.074 >20 16.0
25 S02CH2 2 H 1-naphthyl 0.061 >20 11.7
26 S 2 H 1 -(5,6,7,8-tetrahy dronaphthyl) 0.150 3.0 3.7
27 S 2 H 1-(4-Cl-naphthyl) 0.200 4.7 1.1
28 S 2 H 2-(5,6,7,8-tetrahydronaphthyl) 0.410 >20 4.4
29 S 2 H 3-Me4-a-phenyl 0.210 >20 6.3
30 S 2 H 3,5-di-Me4-Cl-phenyl-phenyl 0.071 >20 2.3
31 CH2 2 H 3,5-di-Me4-Cl-phenyl-phenyl 0.110 7.8
32 0 2 H 3,5-di-Me4-Cl-phenyl-phenyl 0.065
33 SCH2 2 H 3,5-di-Me4-Cl-phenyl-phenyl 0.040 >20 3.7
34 CH2 2 CI 3,5-di-Me4-Cl-phenyl-phenyl 0.003 5.2 0.77
35 0 2 CI 3,5-di-Me4-Cl-phenyl-phenyl 0.009 >20 1.3