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Activity of Bis-Carbamoyloxymethyl Derivatives of Pyrroles and Pyrrolizines against Human Tumor Xenografts in Nude Mice¹

Department of Medicinal Chemistry, School of Pharmacy, State University of New York at Buffalo, Buffalo, New York 14260

The activities of the pyrrolizines, Compounds I and II, and the pyrroles, Compounds IV and V, are reported in nude mouse-grown HT-29 human adenocarcinoma of the colon, DO 1 human oat carcinoma of the lung, and CL 1 human duct cell carcinoma of the breast (coded as CX-1, LX-1, and MX-1, respectively, by the National Cancer Institute). Compounds II and IV were active against all three experimental tumors; both compounds produced significant tumor regression in the human breast tumor xenograft and Compound IV caused tumor regression in the human lung tumor xenograft.

¹ This investigation was supported by USPHS Grant CA-22935, awarded by the National Cancer Institute, Department of Health and Human Services. This is Paper 9 of the series entitled "Vinylogous Carbinolamine Tumor Inhibitors." For Paper 8 in this series, see Ref. 1.

Received 6/26/81. Accepted 3/ 2/82.