19116-90-6Relevant articles and documents
N-Acyl arylsulfonamides as novel, reversible inhibitors of human steroid sulfatase
Lehr, Philipp,Billich, Andreas,Wolff, Barbara,Nussbaumer, Peter
, p. 1235 - 1238 (2007/10/03)
Steroid sulfatase (STS) is an attractive target for a range of oestrogen- and androgen-dependent diseases. In search of novel chemotypes of STS inhibitors, we had previously identified nortropinyl-arylsulfonylureas 1; however, while these compounds were good inhibitors of purified STS (lowest Ki = 76 nM), they showed only weak inhibition of STS activity in cells (lowest IC50 around 2 μM). Extended structure-activity relationship studies involving modification of the phenylacetyl side chain and replacement of the nortropine element by simpler scaffolds led to the discovery of N-acyl arylsulfonamides, more specifically N-(Boc-piperidine-4-carbonyl)- benzenesulfonamides, as STS inhibitors, some of which exhibit improved cellular potency (best IC50 = 270 nM).
Herbicidal aryl triazolinones
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, (2008/06/13)
Herbicidal aryl triazolinones include the compounds of the formula STR1 where X is preferably halogen such as fluorine, Y is preferably halogen such as chlorine, R1 is preferably methyl, R2 is preferably CHF2, R3 is preferably CH(CH3), and STR2 is --NH2 or the residue of a primary or secondary amine or of a sulfonamide.