Table 3.
Cytostatic activity of peptide/drug conjugates on MCF-7 and MDA-MB-231.
| Conjugate | IC50 ±SD (µM) a | |
|---|---|---|
| MCF-7 | MDA-MB-231 | |
| Dabcyl-AMBA-Arg-Arg-Arg-Arg-Lys(DauSuc) | 10.3 ± 5.0 | 10.1 ± 6.0 |
| Dabcyl-PABA- Arg-Arg-Arg-Arg-Lys(DauSuc) | 17.7 ± 1.2 | 14.3 ± 1.1 |
| Dabcyl-NAPH- Arg-Arg-Arg-Arg-Lys(DauSuc) | 15.0 ± 4.2 | 16.6 ± 0.5 |
| Dabcyl-Trp-Arg-Arg-Arg-Arg-Lys(DauSuc) b | 26.4 ± 4.2 | 18.0 ± 6.7 |
| DauSuc-Arg8 b | 14.4 ± 0.2 | 19.5 ± 0.4 |
| Dabcyl-AMBA-Arg-Arg-Arg-Arg-Lys(MTX) | 11.8 ± 6.9 | 19.2 ± 7.1 |
| Dabcyl-PABA- Arg-Arg-Arg-Arg-Lys(MTX) | 18.6 ± 3.3 | 16.8 ± 4.7 |
| Dabcyl-NAPH- Arg-Arg-Arg-Arg-Lys(MTX) | 14.8 ± 2.5 | 16.9 ± 2.8 |
| Dabcyl-AMBA-Arg-Arg-Arg-Arg-Lys(GFLG-E5-MTX) | 8.0 ± 2.4 | 16.3 ±0.7 |
| Dabcyl-Trp-Arg-Arg-Arg-Arg-Lys(MTX) b | 36.9 ± 3.0 | 7.4 ± 2.2 |
| MTX-Arg8 c | >100 | >100 |
| DauSuc d | 24.5 ± 7.1 | >100 |
| MTX c | 0.8 ± 0.3 | >100 |
a The cells were incubated with the compound for 3 h, and subsequently cultured in serum containing medium for 3 days.The IC50 values were determined by MTT assay as described in the text. Standard deviation values (SD) are also presented. b From the literature [33], c From the literature [6] and d From the literature [32].