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. 2018 Apr 4;14:756–771. doi: 10.3762/bjoc.14.64

Table 2.

In vitro cytostatic effects of GnRH-III bioconjugates on HT-29 human colon cancer and MCF-7 human breast cancer cell line.

code [8Lys(Dau=Aoa)]–GnRH-III compound MCF-7 IC50 [µM] HT-29 IC50 [µM]

K1 [6L-Asp] 3.2 ± 0.1 1.5 ± 0.5
1 [6D-Asp] 13.0 ± 0.5 8.9 ± 1.3
2 [6D-Glu] 6.8 ± 1.0 10.1 ± 1.4
3 [6D-Trp] n.d.a n.d.a
K2 [4Lys(Bu),6L-Asp] 2.7 ± 0.1 1.9 ± 0.7
4 [4Lys(Bu),6D-Asp] 6.2 ± 0.2 9.3 ± 1.1
5 [4Lys(Bu),6D-Glu] 7.0 ± 1.2 13.7 ± 2.6
6 [4Lys(Bu),6D-Trp] n.d.a n.d.a

an.d. - no data (compound 3 and 6 precipitated in medium at concentrations higher than 20 µM – no dose response). All values represent mean ± SE.