Use of certain amides as probes for detection of antitubulin activity and residence monitoring.

摘要

This invention relates to methods for screening compounds for antitubulin activity, resistance monitoring and quantifying tubulin using certain amides that inhibit the growth of eukaryotic cells as probes in binding assays, said amides having the structural formula wherein A is cycloalkyl, alkyl, haloalkyl, alkylthio, haloalkylthio, alkenyl, haloalkenyl, alkynyl, haloalkynyl, alkoxy, haloalkoxy, or phenyl, pyridyl, furyl, thienyl, isoxazolyl, oxazolyl, pyrrolyl, isothiazolyl, thiazolyl, pyrazolyl, imidazolyl, pyrimidinyl, quinolyl, isoquinolyl, naphthyl, pyridazinyl, pyrazinyl, benzothienyl, indolyl, benzofuranyl or benzyl, all optionally substituted in an acceptable manner with up to 4 substituents; R<1> and R<2> are each independently a hydrogen atom, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl or haloalkynyl, provided that both R<1> and R<2> are not a hydrogen atom; and X, Y and Z are each independently a hydrogen atom, halo, cyano, thiocyano, isothiocyano or alkylsulfonyloxy, provided that at least one of X, Y and Z is not a hydrogen atom; or the optical enantiomers thereof.