Biological Activity of Organo Silicon Compounds—Study on Cancer Chemotherapeutic Activity—

Abstract

Fifty organo silicon compounds were screened as to their antitumor effect by using several animal transplantable tumors such as Ehrlich carcinoma (EHC), Sarcoma-180 (S-180), Lewis lung carcinoma (LLC), B-16 melanoma (B-16 M), L-1210 and P-388 leukemia. Among these compounds, 2-(2-trimethylsilylethyl)thioethylamine (SDK-12A) was found to be effective by oral administration on solid tumors of EHC, S-180, LLC and B-16M, but SDK-12 A was found to be ineffective on L-1210 and P-388 leukemia. The effect on EHC, S-180 and B-16 M was superior to that of 5-FU administered intraper-itoneally and the effect on LLC was equivalent to that of 5-FU. SDK-12 A was found to be low toxic and after the oral administration of 1/5 LD50/day to mice for 10 days, any toxic symptoms were not observed. This compound showed an inhibitory effect on the metastasis of both of B-16 M and LLC. Furthermore, SDK-12 A showed activation of the delayed type hypersensitivity response of mice bearing B-16 M. From these findings, it may be suggested that SDK-12 A is a unique drug possessing a dual effect for inhibition of the tumor growth and activation of the delayed type cellular immunity. © 1990, The Chemical Society of Japan. All rights reserved.