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[Studies on the antitumor activity of organotin compounds].

Organotin compounds were found to obviously inhibit the activity of phospholipid/Ca(2+)-dependent protein kinase (PKC) in rat brain tissue and the proliferation of tumor cell lines in vitro. The results showed that a correlation exists between the effects on PKC and anti-proliferative and antitumor activities. The structure-activity relationship was shown to be as follows: (1) R, the organic group determines the biological activity; (2) electronegativity of the halogen can affect the activity. The organotin compounds inhibit tumor cells by its [SnR2]2+, and inhibit G1-->S phases of HL-60 cell cycle. The IC50 of [SnPh2F2], [SnPh2(CysOS)].H2O and [SnPh2Cl2.phen(CH3)2] are respectively 25, 15 and 20 mumol.L-1 on PKC, 0.5, 4.0 and 0.3 mumol.L-1 on HL-60 cells, 2.7, 9 and 1.5 mumol.L-1 on BEL-7402 cells, 2.2, 15 and 5.0 mumol.L-1 on KB cells. But no induction of differentiation of leukemic cell lines HL-60 and K562 was observed.