Antitumour Screening of Organotin Derivatives of Biologically Relevant Substrates

A strategy for developing improved anti-cancer drugs is one where biologically active species are coordinated to the tin centre so that, for example, the metabolic pathway of the original drug is altered resulting in greater therapeutic benefit. In this context, diorganotin (of type 1) and triorganotin steroidcarbox-ylates (of type 3) were studied (Table 22.4).64 66

Triorganotin steroidcarboxylates are more potent than dimeric distannox-anes and possess high in vitro cytotoxicities, but their water solubility still remains a drawback,67 which could possibly affect their in vivo properties owing to low bioavailability.

Table 22.4 Typical ID50 values (ng/ml) of three selected organotin steroidcarboxylates

Table 22.4 Typical ID50 values (ng/ml) of three selected organotin steroidcarboxylates

Cell line

Compound

MCF-7

EVSA-T

WIDR

IGROV M19 MEL

A498

H226

1, R = n-Bu

160

60

390

160 120

220

420

3, R = Ph

16

<3

19

18 51

65

61

3, R = n-Bu

16

<3

15

<3 51

138

76

CPT

699

422

967

169 558

2253

3269

DOX

10

8

11

60 16

90

199

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