Table 2.
Antiproliferative activity of conjugates 5–7 and free PTX in αvβ3‐expressing human renal cell carcinoma 786‐O cells after 96 h treatment, in the presence (or absence) of elastase from human leukocytes.
| IC50 [nm][a] | ||
|---|---|---|
| Added elastase | ||
| Structure | NO | YES |
| Paclitaxel (PTX) (12) | 35.8±16.7 | 29.5±7.6 |
| cyclo(DKP‐RGD)‐NPV‐PTX (5) | >5000 | 19.6±4.1 |
| cyclo(DKP‐RGD)‐NPv‐PTX (6) | >5000 | >5000 |
| cyclo(DKP‐RGD)‐unc‐PTX (7) | >5000 | >5000 |
[a] IC50 values were determined as the concentration of compound required for 50 % inhibition of cell viability in presence or absence of 50 nm elastase (ELANE, 324681, Millipore). Samples were measured in triplicate.