Camptothecin analogs with bulky, hydrophobic substituents at the 7-position via a Grignard reaction

…, RM Wadkins, D Bearss, DD Von Hoff, MC Wani…

Index: Manikumar, Govindarajan; Wadkins, Randy M.; Bearss, David; Von Hoff, Daniel D.; Wani, Mansukhlal C.; Wall, Monroe E. Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 21 p. 5377 - 5381

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Citation Number: 8

Abstract

By developing a new synthetic procedure for introduction of side chains onto the camptothecin ring system, we were able to achieve the preparation of a number of analogs bearing bulky, hydrophobic groups directly attached to the 7-position. These include 7-tert- butylcamptothecin, 7-benzylcamptothecin and the corresponding 10, 11- methylenedioxycamptothecins. This method involves the reaction of an appropriate ...