SYNTHESIS AND PROPERTIES OF POLY[3,3'-(1, 3-DIOXO-1,3-DIGERMOXANEDIYL)BISPROPANOIC ACID] (GE-132) AND RELATED-COMPOUNDS AS BIOACTIVE ORGANOGERMANIUM COMPOUND

There has been considerable interest in recent years in the synthesis of bioactive organogermanium compounds. Previously, we observed that y [3,3'-(1,3-dioxo-1,3-digermoxanediyl)bispropanoic acid] (Ge-132) has a unique chemical structure and shows various physiological activities. Therefore, we synthesized the number of Ge-132 relates compounds (pol y (1,3-dioxodigermoxanes) and bis (1,3-dithioxodigermathianes), germat ranes and thiagermatranes, 4,5-dihydro-5-germafuran-2(3H)-ones and 4,5 -dihydro-5-germathiophen-2(3H)-ones, and 3-(trialkylgermyl)propanoic a cids). We also clarified and the, chemical proparties of these compoun ds which were found to exhibit more or less active than Ge-132. Ge-132 and related compounds showed the following pharmacological activities . 1) Antitumor activities against certain tumor being animals. 2) Anti viral activities in virus-infected animals. These two activities were considered to be based on BRM activities such as activation of macroph ase increase of NK activity and increase of humoral immunity. These BR M activities are considered to be based by interferon-gamma (IFN) indu ction, because the formation of IFN gamma m-RNA by Ge-132 and related compounds in confirmed by means of PCR method. 3) Regulation of Ca2+ m etabolism. 4) Alleviation of concerous pain and osteocope. 5) A protec tive effect against free radicals. 6) Inhibitory activity of the forma tion of advanced glycation end products (AGE) in tissue, which is acce lerated in diabetes mellitus. Although more sophisticated molecular bi ological studies remain to be conducted, we believe that a new type of therapeutic agents may be derived from these oraganogermanium derivat ives.