SYNTHESIS, CHARACTERIZATION, AND ANTI-HUMAN-IMMUNODEFICIENCY-VIRUS ACTIVITY OF WATER-SOLUBLE SALTS OF POLYOXOTUNGSTATE ANIONS WITH COVALENTLY ATTACHED ORGANIC GROUPS

The cesium and tetramethylammonium (TMA) salts of polyoxotungstate anions with covalently attached organosilyl groups of formula [(RSi)2O]SiW11O39(4-), where R = CH2CH2COCH3, (CH2)3CN, and CH = CH2 (1-R, cesium salt, unless otherwise noted) have been prepared, purified, and spectroscopically characterized. The water solubility (25-degrees-C) of these 10 new compounds ranges from 0.14 mM to 2.16 mM. All appear to be stable in aqueous media over a period of several hours as assessed by H-1 NMR. The activities (EC50) of the new compounds against human immunodeficiency virus in primary human lymphocytes range from 3.3-mu-M to 39.0-mu-M. Their toxicities (IC50) are all greater than 100-mu-M. The inhibition constants of the new compounds against purified virion-derived HIV-1 reverse transcriptase are in the 1-10-mu-M range.