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Estrogenic compounds as anti-mitotic agents

  • US 5,661,143 A
  • Filed: 12/12/1995
  • Issued: 08/26/1997
  • Est. Priority Date: 08/06/1993
  • Status: Expired due to Term
First Claim
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1. A method for treating a mammalian disease characterized by undesirable cell mitosis, said method comprising administering to a mammal a compound of the formula below, said compound being administered in an amount sufficient to inhibit tubulin polymerization or depolymerization:

  • ##STR4## wherein;

    I. Ra -Ro are defined as follows;

    A) each Ra, Rb, Rc, Rd, Re, Rf, Ri, Rj, Rk, RL, Rm, Ro, independently is --R1, --OR1, --OCOR1, --SR1, --F, --NHR2, --Br, or --I; and

    Rg is --R1, --OR1, --OCOR1, --SR1, --F, --NHR2, --Br, --I, or --C.tbd.CH;

    orB) each Ra, Rb, Rc, Rf, Rk, RL Ro, independently is --R1, --OR1, --OCOR1, --SR1, --F, --NHR2, --Br, or --I; and

    each Rd, Re, Ri, Rj, Rm, independently is ═

    O, --R1, --OR1, --OCOR1, --SR1, --F, NHR2, --Br or --I; and

    Rg is ═

    O, --R1, --OR1, --OCOR1, --SR1, --F, --NHR2, --Br, --I, or --C.tbd.CH; and

    II. Z'"'"' is defined as follows;

    ##STR5## and III. Z" is defined as follows;

    Z" is Y, where Y is ##STR6## where n is 0-6;

    IV. provided that when each Rb, Rc, Rd, Re, Ri, Rj, Rk, RL, Rm and Ro is H;

    Rf is --CH3 ;

    Rg is --OH;

    Z'"'"' is >

    CHOH; and

    Z" is >

    CH2 ;

    then Ra is not --H; and

    V. provided that when each Rb, Rc, Rd, Re, Ri, Rj, Rk, RL, Rm and Ro is H;

    Rf is --CH3 ;

    Rg is OH;

    Z'"'"' is >

    COH; and

    Z" is >

    CH2 ;

    then Ra is not OCH3 ;

    where, in each formula set forth above, each R1 and R2 independently is --H, or an alkyl, alkenyl or alkynl group of up to 6 carbons.

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