Absolute and relative activities of 4' -iodo-4'-deoxydoxorubicin against human colo-rectal tumors, as evaluated by a short-term in vitro assay.
A short-term antimetabolic assay based on the interference with 3H-thymidine and 3H-uridine incorporation after 3 hours of in vitro treatment was used to compare the cytotoxicity of a new halogenated anthracycline, 4'-Iodo-4'-deoxydoxorubicin (IDX), with that of its parent compound Doxorubicin (DX) against 44 human colorectal carcinomas. IDX had a marked dose-dependent effect, with frequencies of activity consistently greater than those of DX at all concentrations. The minimal dose of IDX required to induce a significant antimetabolic effect obtained by extrapolation from the dose-effect plots for each drug was 1/10 that of DX (2.3 micrograms/ml vs 23 micrograms/ml). When the relative activities of the two drugs on the same tumor specimen were determined, there was 71% to 86% overall agreement, depending on the concentration used. Lack of agreement was always attributed to sensitivity to IDX and resistance to the parent compound.
Villa
R
R
Oncologia Sperimentale C, Istituto Nazionale per lo Studio e la Cura dei Tumori, Milano, Italy.
Zaffaroni
N
N
Giuliani
F C
FC
Colella
G
G
Sanfilippo
O
O
Silvestrini
R
R
D015179:Colorectal Neoplasms / Q000188:drug therapy / Q000473:pathology*; D004305:Dose-Response Relationship, Drug; D004317:Doxorubicin / Q000031:analogs & derivatives* / Q000494:pharmacology; D004351:Drug Resistance; D006801:Humans; D014407:Tumor Cells, Cultured / Q000187:drug effects
C053044:4'-deoxy-4'-iododoxorubicin; D004317:Doxorubicin