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Wijngaarden 51 and research group have synthesized a series of 2-phenylpyrrole
Mannich bases and screened in pharmacological models for antipsychotic activity
and extrapyramidal effects. They made structure modification of 5-(4-
flourophenyl)-2-[4-(2-methoxyphenyl)-I-piperazinyl] methyl pyrrole, the prototype
of new class of sodium independent atypical dopamine D-2 anganosits and
resulted in 2-[4-(7-benzofuranyl)-I-piperazinyl] methyl-5-(flouro phenyl) pyrrole,
which was an even more potent and selective D-2 anganosits than the parent
compound. They found excellent oral activity in the apomorphine induced
climbing behavior and the conditioned avoidance response tests and the absence
of catalepsy make this compound particularly promising as a potential
antipsychotic with low propensity to induce acute extrapyramidal side effect.
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Demetri 52 has suggest, GIST is the most common mesenchymal cancer of the
gastrointestinal tract. Activating mutations in KIT are common in GIST, and
imatinib, which also inhibits KIT, was found to be the first RTK inhibitors to show
efficacy in this cancer, dramatically improving disease outcome 43 . However,
resistance to imatinib resulting from subsequent mutations in KIT has emerged.