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. Author manuscript; available in PMC: 2009 Aug 29.
Published in final edited form as: J Med Chem. 2008 May 9;51(11):3203–3221. doi: 10.1021/jm800086e

Table 5.

Cytotoxicity of second-generation taxoids with modifications at C1O (IC50 nM)a

graphic file with name nihms102336t1.jpg
Taxoid R LCC6-WTb LCC6-MDRc R/S
Paclitaxel -- 3.1 346 112
6a Bz 1.8 4.8 2.7
6b graphic file with name nihms102336t2.jpg 2.1 5.8 2.7
6c graphic file with name nihms102336t3.jpg 2.8 5.1 1.8
6d graphic file with name nihms102336t4.jpg 3.8 4.7 1.2
6e graphic file with name nihms102336t5.jpg 2.1 5.7 2.7
6f graphic file with name nihms102336t6.jpg 5.3 15.2 2.9
6g graphic file with name nihms102336t7.jpg 6.3 15.2 2.4
6h Cbz 1.8 16.7 9.3
6i graphic file with name nihms102336t8.jpg 2.3 13.8 6.0
6j graphic file with name nihms102336t9.jpg 2.1 20.3 9.7
6k graphic file with name nihms102336t10.jpg 1.4 38.4 27.4
6l graphic file with name nihms102336t11.jpg 5.1 31.2 6.1
6m graphic file with name nihms102336t12.jpg 1.5 5.0 3.3
6n graphic file with name nihms102336t13.jpg 3.7 6.7 1.8
6o graphic file with name nihms102336t14.jpg 1.7 4.9 2.9
a

Concentration of compound which inhibits 50% (IC50, nM) of the growth of human tumor cell line after 72 h drug exposure.

b

LCC6-WT: human breast carcinoma cell line (Pgp−).

c

LCC6-MDR: mdrl transduced cell line (Pgp+).

d

Resistance factor = (IC50 for drug resistant cell line, R)/(IC50 for drug-sensitive cell line, S).