Table 2 Structure-activity relationship and affinity probe synthesis of indole analog.

From: Nicotinamide phosphoribosyltransferase is a molecular target of potent anticancer agents identified from phenotype-based drug screening

Compound

R1

R2

R5′

RMG-I GI50 (nM)

ES-2 GI50 (nM)

K542

View full size image

1.8

>1000

K543

View full size image

82

>1000

K541

0.7

>1000

K216

View full size image

<1

>1000

K270

>300

>1000

K336

View full size image

>1000

>1000

K209

View full size image

6.1

>1000

Ind-tag

N.T.a

N.T.a

  1. aNot Tested.