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Substituted Schiff bases of l-amino-3-hydroxyguanidine (SB-HAG) were tested for the first time against noninfected T4 lymphocytes (CEM-6 cells) and the same cell line infected by HIV-1 in vitro. Twenty-one of 23 compounds at micromolar levels did not inhibit the growth of the noninfected T4 cells, suggesting minimal cytotoxicity. The antiviral effects of these compounds in a micromolar concentration range have been shown to be nonsignificant (

Combretastatins and their synthetic analogues, having structural features resembling that of colchicine, also have similar modes of action. In this report we have correlated the cytotoxicity of combretastatins against the murine leukemic cell line L1210 with physicochemical parameters such as the summation of the Hansch-Fujita pi constant, which was used as an index of lipophilicity of the substituent groups on ring A (sigma pi a) and ring B (sigma pi b), the vector summation of the group dipole moments of ring A (sigma mu a) and ring B (sigma mu b), the nature of the linker chain between ring A and ring B (Bt-L), indicator parameters (NOH)a and (NOH)b, which represent the number of hydroxyl groups on ring A and ring B, respectively, and the summation of pi values of the substituents on the linker (sigma pi L). Cytotoxicity correlated well with (sigma pi b), (NOH)a, (Bt-L), and (sigma mu b), and the dependency on (sigma pi b) was found to be parabolic.

In the search for new brain imaging agents for the use with single photon emission computed tomography (SPECT), quantitative structure activity relationship (QSAR) analysis of the correlations between initial brain uptake and physicochemical parameters like lipophilicity, log P, molecular weight, log MW and log U/D (undissociated/dissociated), of the 99mTc-DADT (diaminedithiol) complexes and 99mTc-PAO (propyleneamineoxime) complexes have been analyzed. High correlations are found for both the 99mTc-DADT complexes (r = 0.94) and for the 99mTc-PAO complexes (r = 0.83) which are significant at 99.9 and 99.5 percentile level, respectively. These results will help the further design of better ligands for 99mTc in brain imaging.