ABSTRACT
We herein describe a new synthesis of N-(7-indazolyl)benzenesulfonamide derivatives. These compounds were evaluated for their antiproliferative activities toward L1210 murine leukemia cells. One of them, 4-methoxy-N-(3-chloro-7-indazolyl)benzenesulfonamide, was identified as the most potent with an IC(50) of 0.44 microM.
Subject(s)
Cell Cycle/drug effects , Indazoles/chemistry , Indazoles/pharmacology , Sulfonamides/chemistry , Sulfonamides/pharmacology , Animals , Cell Line, Tumor , Humans , Indazoles/chemical synthesis , Leukemia/pathology , Mice , Molecular Structure , Structure-Activity Relationship , Sulfonamides/chemical synthesisABSTRACT
The synthesis of a new series of alpha- and beta-adrenergic blocking agents 14 is described. The affinity and selectivity of these compounds for alpha, beta 1 and beta 2-adrenoceptors were studied in comparison with those of WB-4101 and propranolol. The derivatives 14cx and 14dx are more potent beta 1-blockers than propranolol.
Subject(s)
Adrenergic alpha-Antagonists/chemical synthesis , Adrenergic beta-Antagonists/chemical synthesis , Dioxins/chemical synthesis , Adrenergic alpha-Antagonists/pharmacology , Adrenergic beta-1 Receptor Antagonists , Adrenergic beta-2 Receptor Antagonists , Adrenergic beta-Antagonists/pharmacology , Animals , Dioxanes/pharmacology , Dioxins/pharmacology , Guinea Pigs , Heart Atria/drug effects , In Vitro Techniques , Male , Propranolol/pharmacology , Rats , Stereoisomerism , Trachea/drug effects , Vas Deferens/drug effectsABSTRACT
The four stereoisomers of compound 1 were synthesized from 2,3-dihydro-1, 4-benzodioxin and evaluated as alpha- and beta-adrenergic antagonists. Enantiomer 1-b [2R, 2'S] (Figure 1) is the best beta 1-blocking agent. Furthermore all compounds showed a alpha-blocking activity.