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Methods and compositions utilizing quinazolinones

  • US 6,562,831 B1
  • Filed: 11/28/2000
  • Issued: 05/13/2003
  • Est. Priority Date: 10/27/1999
  • Status: Expired due to Fees
First Claim
Patent Images

1. A method of screening for compounds that bind to KSP kinesin comprising the steps of:

  • (a) combining a KSP kinesin with a labeled compound, wherein said compound is chosen from the group consisting of;

    embedded image

    wherein;

    R1 is chosen from hydrogen, alkyl, aryl, alkylaryl, heteroaryl, alkylheteroaryl, substituted alkyl, substituted aryl, substituted alkylaryl, substituted heteroaryl, and substituted alkylheteroaryl;

    R2 and R2

    are independently chosen from hydrogen, alkyl, oxaalkyl, aryl, alkylaryl, heteroaryl, alkylheteroaryl, substituted alkyl, substituted aryl, substituted alkylaryl, substituted heteroaryl, and substituted alkylheteroaryl;

    or R2 and R2

    taken together form a 3- to 7-membered ring;

    R3 is chosen from hydrogen, alkyl, aryl, alkylaryl, heteroaryl, alkylheteroaryl, substituted alkyl, substituted aryl, substituted alkylaryl, substituted heteroaryl, substituted alkylheteroaryl, oxaalkyl, oxaalkylaryl, substituted oxaalkylaryl, R15O— and

    R15

    NH—

    ;

    R3′

    is chosen from hydrogen, alkyl, aryl, alkylaryl, heteroaryl, alkylheteroaryl, substituted alkyl, substituted aryl, substituted alkylaryl, substituted heteroaryl, substituted alkylheteroaryl and R15

    NH—

    ;

    R3″

    is chosen from alkyl, aryl, alkylaryl, heteroaryl, alkylheteroaryl, substituted alkyl, substituted aryl, substituted alkylaryl, substituted heteroaryl, and substituted alkylheteroaryl;

    R4 is chosen from hydrogen, alkyl, aryl, alkylaryl, heteroaryl, alkylheteroaryl, substituted alkyl, substituted aryl, substituted alkylaryl, substituted heteroaryl, substituted alkylheteroaryl, and R16-alkylene-;

    R5, R6, R7 and R8 are independently chosen from hydrogen, alkyl, alkoxy, halogen, fluoroalkyl, nitro, dialkylamino, alkylsulfonyl, alkylsulfonamido, sulfonamidoalkyl, sulfonamidoaryl, alkylthio, carboxyalkyl, carboxamido, aminocarbonyl, aryl and heteroaryl;

    R15 is chosen from hydrogen, alkyl, aryl, alkylaryl, heteroaryl, alkylheteroaryl, substituted alkyl, substituted aryl, substituted alkylaryl, substituted heteroaryl, and substituted alkylheteroaryl;

    R16 is chosen from alkoxy, amino, alkylamino, dialkylamino, N-heterocyclyl and substituted N-heterocyclyl;

    under conditions suitable for said compound to bind to said KSP kinesin;

    (b) adding a candidate agent under conditions suitable for said agent to bind to said KSP kinesin, thereby displacing at least a portion of said compound that had been bound to said KSP kinesin; and

    (c) determining the binding of said agent to said KSP by monitoring the amount of said compound either bound to said KSP or displaced therefrom.

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