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General procedure for the synthesis ofN-{1-[(3-thioxo-5,6-dihydroimidazo[2,1-c][1,2,4]thiadiazol-7-lythio)-thiocarbonyl]2-imidazolidene}arylsulfonamides (2a-z). 6,7-Dihydro-5H-imidazo[2,1-c][1,2,4]thiadiazole-3-thione (1) (0.5 g, 3.14 mmol) was dissolved in pyridine (10 mL). The resulting solution was cooled to 0 °C and a corresponding sulfonyl chloride (1.89 mmol) was added. The reaction mixture was stirred for 12 h at room temperature. Then, water was added (15 mL) and the solution was concentrated under reduced pressure to half of its initial volume. The oily product 2 thus obtained was purified by either crystallization or column chromatography (see Supplementary material).
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33746529243
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note
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50 = molar concentration of the compound leading to 50% net cell death). Furthermore, a mean graph midpoint (MG_MID) is calculated for each of the mentioned parameters, giving an averaged activity parameter over cell lines. Selectivity of a compound with respect to one or more cell lines of the screen is characterized by a high deviation of the particular cell line parameter compared to the MG_MID value.
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