Table 1.
Biological activity of novel DHA and ART hybrid and dimer derivatives against metastatic melanoma cancer cell lines RPMI7951.[a]
|
Entry |
Type |
Compound |
CC50±SD[b] C3PV |
IC50±SD[c] RPMI7951 |
|---|---|---|---|---|
|
1 |
– |
1 |
>300.0±14.85 |
3.62±0.99 |
|
2 |
– |
2 |
0.68±0.19 |
0.91±0.45 |
|
3 |
– |
3 |
1.68±0.44 |
1.08±0.56 |
|
4 |
DHA Hybrid |
5[d] |
1.76±0.31 |
0.33±0.08 |
|
5 |
ART Hybrid |
6[d] |
>300.0±10.71 |
8.34±3.06 |
|
6 |
ART Hybrid |
7[d] |
132±12.58 |
0.09±0.03 |
|
7 |
ART DIMER |
8[d] |
6.10±3.74 |
0.49±0.05 |
|
8 |
DHA Hybrid |
7‐β |
1.14±0.45 |
0.2±0.01 |
|
9 |
DHA Hybrid |
12‐β |
38.15±2.56 |
0.4±0.03 |
|
10 |
ART Hybrid |
13‐α |
3.39±0.05 |
1.7±0.03 |
|
11 |
ART Hybrid |
14‐α |
6.38±1.5 |
1.3±0.07 |
|
12 |
ART Hybrid |
15‐α |
55.25±7.33 |
2.5±0.05 |
|
13 |
DHA Hybrid |
16‐α |
8.14±0.85 |
4.6±0.03 |
|
14 |
DHA DIMER |
17‐α,α |
0.25±0.03 |
0.07±0.01 |
|
15 |
DHA DIMER |
18‐α,α |
8.0±0.1 |
10.75±1.6 |
|
16 |
DHA DIMER |
19‐β,β |
5.7±0.79 |
3.6±0.95 |
|
17 |
ART DIMER |
20‐α,α |
228.0±1.5 |
2.45±0.05 |
|
18 |
ART DIMER |
21‐α,α |
>300.0±7.56 |
1.76±0.03 |
|
19 |
ART DIMER |
22‐α,α |
>300.0±9.78 |
0.05±0.02 |
|
20 |
– |
Paclitaxel |
78.88±0.79 |
0.013±0.10 |
[a]All experiments were conducted in triplicate. [b]CC50±SD (half‐maximal cytotoxic concentration±standard deviation) values for all compounds are expressed in micromolar units. [c]IC50±SD (half‐maximal inhibitory concentration±standard deviation) values for all compounds are expressed in micromolar units. [d]Antimelanoma and cytotoxicity data from ref. 12.