MODULATORS OF MULTI-DRUG RESISTANCES

• Main Authors: MJALLI, ADNAN M.M, SARSHAR, SEPEHR
• Format: Patent
• Language: English; French
• Published: 25.10.1998
• Edition: 6
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The present invention relates to imidazole derivatives having formula 1 (see fig. I) wherein: R1 is selected from the group consisting of: mono-,di-,and tri-substituted phenyl or thienyl, the substituents are selected from the group consisting of: (i) substituted C1-6 alkyl, substituted C2-6 alkyloxy, wherein the substituents are selected from the group consisting of hydrogen or C1-6 alkoxy; (ii) C1-11 CO2R5, trans- CH=CHCO2R5, wherein R5 is C1-11 alkyl, or phenyl C1-11 alkyl; R2 and R3 are mono-, di, and tri-substituted phenyl wherein the substituents are independently selected from: (i) halo; (ii) C1-6 alkyl-amino, or di(C1-6 alkyl)amino, and R4 is hydrogen. These compounds are useful for restoring the sensitivity of multidrug resistant cells to cancer chemotherapeutic agents.