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

• Main Author: DAVID HAMILTON YOUNG
• Format: Patent
• Language: English
• Published: 12.05.1998
• Edition: 6
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; BEER; BIOCHEMISTRY; CHEMISTRY; COMPOSITIONS OR TEST PAPERS THEREFOR; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL ORENZYMOLOGICAL PROCESSES; ENZYMOLOGY; INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIRCHEMICAL OR PHYSICAL PROPERTIES; MEASURING; MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEICACIDS OR MICROORGANISMS; METALLURGY; MICROBIOLOGY; MUTATION OR GENETIC ENGINEERING; ORGANIC CHEMISTRY; PHYSICS; PROCESSES OF PREPARING SUCH COMPOSITIONS; SPIRITS; TESTING; VINEGAR; WINE

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 and R are each independently a hydrogen atom, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl or haloalkynyl, provided that both R and R 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.