Gastrin receptor antagonist

Gastrin receptor antagonists and gastrin-releasing peptide antagonists have now been developed for experimental use. but it is not yet clear if either will be useful clinically. See BOMBESIN RECEPTOR ANTAGONISTS) CHOLECYSTOKININ RECEPTOR ANTAGONISTS. 

Table 3.7 CCKa/Gastrin Receptor Antagonists That Have Been Evaluated in the Clinic... 

B8. Beauchamp, R. D., Townsend, C. M., Singh, P., Glass, E. J., and Thompson, J. C., Proglumide, a gastrin receptor antagonist inhibits growth of colon cancer and enhances survival in mice. Ann. Surg. 202, 303-309 (1985). 

H10. Hoosein, N. M., Kiener, P. A., Curry, R. C., Rovati, L. C., McGilbra, D. K., and Brattain, M. G., Antiproliferative effects of gastrin receptor antagonists and antibodies to gastrin on human colon carcinoma cell lines. Cancer Res. 48, 7179-7183 (1988). 

In an approach to the gastrin receptor antagonist (+)-AG-041, the Iwabuchi group has prepared the nitrogen-substituted spirocycle 153 by means of an oxidative intermolecular aza-spiro-annulation (Scheme 38) [82], Accordingly, indole 151 was treated with dirhodium catalyst 152 in the presence of PHl(OAc)2 and MgO to afford spirocycle 153 in 70% yield and 96% ee. The deuterium labeling was necessary for successful implementation of the spirocyclization. 

Emura, T. Esaki, T. Tachihana, K. Shimizu M. Efficient asymmetric synthesis of novel gastrin receptor antagonist AG-041R via highly stereoselective alkylation of oxindole enolates. J. Org. Chem. 2006, 71, 8559-8564. 

Hoosein NM, Kiener PA, Curry RC (1988) Antiproliferative effects of gastrin receptor antagonists and antibodies to gastrin on human colon carcinoma cell lines. Cancer Res 48 7179-7183... 

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