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. Author manuscript; available in PMC: 2016 Mar 12.
Published in final edited form as: J Med Chem. 2015 Feb 18;58(5):2406–2416. doi: 10.1021/jm5019115

Table 1.

Cytotoxicities (IC50, nM) of Paclitaxel, Taxoid 3, Conjugates 1 and 4 against BR+ and BR− Cell Lines (Incubation at 37 °C for 48 h)

Entry Compound MX-1a ID8b L1210FRc L1210d WI38e
1f paclitaxel 7.23 ± 0.68 14.36 ± 1.81 38.7 ± 17.7 77.1 ± 12.8 61.4 ± 12.7
2f Taxoid 3 4.13 ± 2.59 0.17 ± 0.14 4.18 ± 1.8 7.05 ± 1.38 5.23 ± 0.27

3f 1 21.2 ± 4.6 6.62 ± 0.86 14.7 ± 4.0 593 ± 123 709 ± 55
4f 4 15.4 ± 4.2 4.32 ± 1.58 13.4 ± 6.8 481 ± 34 670 ± 89
a

human breast carcinoma cell line (BR+);

b

murine ovarian carcinoma cell line (BR+);

c

murine lymphocytic leukemia cell line (BR+);

d

murine lymphocytic leukemia cell line (BR−);

e

Human lung fibroblast cell line (BR−);

f

Cells were incubated with a drug or conjugate at 37 °C for 48 h.