Table 3. Early ADMET Data on Two Representative Lectin-Targeted Conjugates (22 and 30) and Ciprofloxacin (3): All Compounds Were Metabolically Stable in Human Plasma and Microsomal Fractions. Cytotoxicity was reduced compared to ciprofloxacina.
metabolic
stability |
|
|||||
---|---|---|---|---|---|---|
t1/2 [min] | CLMIC [μL/min/mg protein] |
plasma protein binding [%] | cytotoxicity @ 100 μM [% inhibition] |
|||
compound | human plasma | MLM | HLM | human plasma | HEK293 | A549 |
22 | >150 | 10 | 10 | 69 ± 7 | 8 ± 4 | 5 ± 22 |
30 | >150 | 10 | 15 | 75 ± 10 | 11 ± 12 | –9 ± 15 |
3 | >150 | n.d. | n.d. | 33 ± 2 | 48 ± 5 | 18 ± 11 |
Data is presented as mean and standard deviation from at least two independent experiments (exception: one experiment for CLMIC data). MLM, mouse liver microsomes; HLM, human liver microsomes; n.d., not determined.