[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.
Peng
J
J
Department of Biochemical Pharmacology, School of Pharmacy, Beijing Medical University.
Su
H D
HD
D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D001921:Brain / Q000378:metabolism; D002455:Cell Division / Q000187:drug effects; D006801:Humans; D004915:Leukemia, Erythroblastic, Acute / Q000473:pathology; D015473:Leukemia, Promyelocytic, Acute / Q000473:pathology; D008113:Liver Neoplasms / Q000473:pathology; D008297:Male; D009947:Organotin Compounds / Q000494:pharmacology*; D011493:Protein Kinase C / Q000378:metabolism; D051381:Rats; D017208:Rats, Wistar; D014407:Tumor Cells, Cultured / Q000187:drug effects
D000970:Antineoplastic Agents; D009947:Organotin Compounds; D011493:Protein Kinase C