FERROCENYL POLYAMINES AS AGENTS FOR CHEMOIMMUNOTHERAPY OF CANCER

A series of ferrocenyl polyamines, compounds intended to bind to the tumor cell surface nucleic acid and elicit an immune response, was synthesized and screened for antitumor activity. Target ferrocenyl polyamines 1a,b, 2, and 3, bearing 2-, 3-, and 4-amino groups, respectively, were readily obtained in yields of 31-58% from their corresponding ferrocenyl polyamides (5a-d) by reduction with diborane in THF; lithium aluminum hydride was not an effective reducing agent in this case. Although the target compounds failed to prolong the life of mice with P-388 lymphocytic leukemia, three of the intermediate amides (5b-d) did exhibit low but significant activity (T/C=123, 132, and 120%, respectively). © 1978, American Chemical Society. All rights reserved.