reported a clear trend on chlorination of the southern phenyl ring of a series of halogenated indole derivatives as RORγt inverse agonists to treat autoimmune disorders ( Fig. 5A ). 16 Dichlorinated derivative 21c (IC 50 = 28 nM) was more active than chloro-fluoro derivative 21b (IC 50 = 199 nM), which in turn was more active than difluorinated compound 21a (IC 50 = 445 nM).
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Which halogen to choose? Comparing the effects of chlorine and fluorine as bioisosteric substituents in drug design.
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Wang and co-workers from Minnesota presented 6-arylthio-3-hydroxypyrimidine-2,4-dione inhibitors 52 of human cytomegalovirus which showed an interesting trend in activity and toxicity ( Fig. 17B ). 65 Although the chlorinated compounds were in general better inhibitors they were also more cytotoxic than their fluorinated analogues, as demonstrated in a Hel299 cell viability assay.
This increase in metabolic stability of the chlorinated compounds was found to be close to being statistically significant with a t -test p -value of 0.06.