A novel hydroxyfuroic acid compound as an insulin receptor activator structure and activity relationship of a prenylindole moiety to insulin receptor activation

Table 1 Relative insulin receptor activation potentials of hydroxyfuroic acid compounds with various prenylindole moiety.

Compound	Side Chain	Study 1^a	% activation^b	Study 2^a	% activation^b
D-410637	(CH₂)₂CH₂OH	18.9
D-410638	(CH₂)₃CH₂OH	31.3
D-410639	(CH₂)₄CH₂OH	5590	89.4	1181	72.3
D-410641	(CH₂)₄CH₃			792.7	48.6
D-410642	(CH₂)₃CH(CH₂OH)₂			659.3	40.4
D-410643	(CH₂)₄COOH			799	48.9
D-410644	(CH₂)₂COOH			357.3	21.9
Insulin - 10 nM		6250		1632.5

^a Data in these columns are cpm, representing phosphoryl incorporation by tyrosine kinase activities. Study 1 and 2 are separate experiments each with a 10 nM insulin and a 100 μM D-410639 control for internal reference. The test concentration for hydroxyfuroic acid compounds was 100 μM. See Materials and Methods for detail.
^b Percentage of tyrosine kinase activities as compared to that offered by 10 nM insulin stimulation, presented at the bottom row.

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