Table 2.
Structure-Activity Relationship (SAR) of DC-S303 and its derivatives.
No. | R1 | R2 | R3 | Inhibition Ratio at 100 μM/% | IC50 (μM) |
---|---|---|---|---|---|
DC-S303 | ![]() |
![]() (A) |
![]() |
99 | 1.1 |
DC-S304 | ![]() |
44 | |||
DC-S305 | ![]() |
−5 | |||
DC-S306 | ![]() |
94 | 20 | ||
DC-S307 | ![]() |
8 | |||
DC-S308 | ![]() |
7 | |||
DC-S309 | ![]() |
−5 | |||
DC-S310 | ![]() |
−6 | |||
DC-S311 | ![]() |
97 | 13 | ||
DC-S312 | ![]() |
−3 | |||
DC-S313 | ![]() |
−6 | |||
DC-S314 | ![]() |
![]() (B) |
![]() |
77 | 46 |
DC-S315 | ![]() |
46 | |||
DC-S316 | ![]() |
37 | |||
DC-S317 | ![]() |
29 | |||
DC-S318 | ![]() |
17 | |||
DC-S319 | ![]() |
14 | |||
DC-S320 | ![]() |
11 | |||
DC-S321 | ![]() |
9 | |||
DC-S334 | ![]() |
![]() (C) |
![]() |
96 | 9.9 |
DC-S335 | ![]() |
12 | IC50 (μM) | ||
DC-S336 | ![]() |
49 | 1.1 | ||
DC-S337 | ![]() |
1 | |||
DC-S338 | ![]() |
1 | |||
DC-S339 | ![]() |
−6 | 20 | ||
DC-S340 | ![]() |
−6 | |||
DC-S341 | ![]() |
−10 | |||
DC-S342 | ![]() |
−13 | |||
DC-S343 | ![]() |
![]() (D) |
![]() |
1 | |
DC-S344 | ![]() |
32 | 13 | ||
DC-S345 | ![]() |
29 | |||
DC-S346 | ![]() |
21 | |||
DC-S347 | ![]() |
10 | |||
DC-S348 | ![]() |
−11 | |||
DC-S349 | ![]() |
−1 | |||
DC-S350 | ![]() |
6 | |||
DC-S351 | ![]() |
96 | 3.4 | ||
DC-S352 | ![]() |
39 | |||
DC-S353 | ![]() |
35 | |||
DC-S354 | ![]() |
35 | |||
DC-S355 | ![]() |
20 | |||
DC-S356 | ![]() |
17 | |||
DC-S357 | ![]() |
13 | |||
DC-S358 | ![]() |
6 | |||
DC-S359 | ![]() |
5 | |||
DC-S360 | ![]() |
4 | |||
DC-S361 | ![]() |
−1 | |||
DC-S362 | ![]() |
−4 | |||
DC-S363 | ![]() |
−15 | |||
DC-S364 | ![]() |
54 | 3.7 | ||
DC-S365 | ![]() |
![]() (E) |
![]() |
10 | |
DC-S366 | ![]() |
9 | |||
DC-S367 | ![]() |
−1 |