The invention is based on the discovery that certain 3-oxoacetamideindolyl compounds
have potent anticancer and anti-angiogenic activity. The 3-oxoacetamideindolyl
compounds are of the following formula.
##STR1##
In this formula, each R1 is independently isoxazolyl, thiazolyl, isothiazolyl,
1,3,4-thiadiazolyl, 1,3-benzothiazolyl, quinolyl, isoquinolyl, thionaphthenyl,
or benzofuranyl, each being optionally substituted with 1-6 independent R5;
or when taken together with R2 and the nitrogen atom to which they are
attached form a 5-8 membered ring comprising C, N, S, or O atoms wherein any atom
is optionally substituted with an independent R5. Each R2 is
independently H, C1-C10 alkyl, or aryl, each being optionally substituted with
1-4 independent R5; or when taken together with R1 and the
nitrogen atom to which they are attached form a 5-8 membered ring comprising C,
N, S, or O atoms wherein any atom is optionally substituted with an independent
R5. Each R3 is independently C3-C10 cycloalkyl, C4-C10 cycloalkenyl,
isoxazolyl, furanyl, thiophenyl, thiazolyl, imidazolyl, pyridyl, or heterocyclyl,
each being optionally substituted with 1-4 independent R5. Each R4
is independently H, NO2, halo, CN, R7, OR7,
CO2R7, SR7, NR7R7, C(O)R7,
C(O)NR7R7, OC(O)R7, S(O)2R7,
S(O)2NR7R7, NR7C(O)NR7R7,
NR7C(O)R7, NR7(COOR7), NR7S(O)2NR7R7,
NR7S(O)2R7, or S(O)2OR7.
