Author/Authors :
Michael R. Peel، نويسنده , , Mark W. Milstead، نويسنده , , Daniel D. Sternbach، نويسنده , , Jeffrey M. Besterman، نويسنده , , Peter Leitner، نويسنده , , Bradley Morton، نويسنده , , Monroe E. Wall and، نويسنده , , Mansukh C. Wani، نويسنده ,
Abstract :
A camptothecin derivative has been prepared wherein the A-ring is fused to an oxazole ring. The compound was prepared via a Friedlander condensation involving benzoxazole 8 and tricyclic ketone 9. This derivative displays potent topoisomerase I inhibition (IC50 150 nM) when assayed in the ‘cleavable complex’ assay.