Antitumour Prescreening

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In vivo testing of tetraorganotin compounds showed that they are inactive, whereas organotin halides and their complexes with amines and other ligands exhibit borderline activities against P388 and L1210 leukaemia.9 14 The in vivo pre-screenings against these two cancers used initially by the National Cancer Institute (NCI), USA, were later replaced by in vitro pre-screenings against

Table 22.1 ID50 values (ng/ml) of oncology drugs: doxorubicin (DOX), cisplatin (CPT), 5-fluorouracil (5-FU), methotrexate (MTX) and etoposide (ETO) against seven cancer cell lines of human origin, MCF-7, EVSA-T (mammary cancers), WIDR (colon cancer), IGROV (ovarian cancer), M19 MEL (melanoma), A498 (renal cancer) and H226 (non-small-cell lung cancer)

Drug

Drug

Table 22.1 ID50 values (ng/ml) of oncology drugs: doxorubicin (DOX), cisplatin (CPT), 5-fluorouracil (5-FU), methotrexate (MTX) and etoposide (ETO) against seven cancer cell lines of human origin, MCF-7, EVSA-T (mammary cancers), WIDR (colon cancer), IGROV (ovarian cancer), M19 MEL (melanoma), A498 (renal cancer) and H226 (non-small-cell lung cancer)

Cell line

DOX

CPT

5-FU

MTX

ETO

MCF-7

10

699

750

18

2594

EVSA-T

8

422

475

5

317

WIDR

11

967

225

<3

150

IGROV

60

169

297

7

580

M19 MEL

16

558

442

23

505

A498

90

2253

143

37

1314

H226

199

3269

340

2287

3934

a panel of human tumour cell lines.15 27 This was also the procedure used when organotin compounds were tested by the Rotterdam Cancer Institute. The seven human tumour cell lines comprising the panel were: MCF-7 and EVSA-T (two mammary cancers), WIDR (a colon cancer), IGROV (an ovarian cancer), M19 MEL (a melanoma), A498 (a renal cancer) and H226 (a non-small-cell lung cancer).

In Table 22.1, ID50 (the mass of material required to inhibit the growth of a particular cell line by 50%) values of some well-known oncology drugs are presented; ID50 values sometimes show some variation due to the circumstances of the test but these provide a reliable guide of cytotoxicity and a benchmark for comparison with test compounds. Normally, compounds were dissolved in ethanol solution containing 1 mg of compound in 200 ml and diluted to appropriate concentrations in the screen. Trial compounds that were found to be insoluble in ethanol were dissolved in dimethyl sulphoxide (DMSO).

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