Use of certain amides as probes for detection of antitubulin activity and resistance monitoring
US6500405B1 · kind B1 · utility
Assignee
Inventor
Key dates
| Filing date | Nov 4, 1999 |
| Grant date | Dec 31, 2002 |
| Priority date | — |
| Expiry date | Nov 4, 2019 |
Classification
- Technology area (CPC G)Physics
- CPC primaryG01N33/68
- WIPO fieldMeasurement
- WIPO sectorInstruments
Abstract
This invention relates to methods for screening compounds for antitubulin activity, evaluation of cells for sensitivity to antitubulin drugs, 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 whereinA 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;R1 and R2 are each independently a hydrogen atom, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl or haloalkynyl, provided that both R1 and R2 are not a hydrogen atom; andX, 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; orthe optical enantiomers thereof.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.