Synthesis, topoisomerase I inhibitory activity, and in vivo evaluation of 11-azacamptothecin analogs

…, SS Nanthakumar, D Croom, DL Emerson…

Index: Uehling, David E.; Nanthakumar, Suganthini S.; Croom, Dallas; Emerson, David L.; Leitner, Peter P.; et al. Journal of Medicinal Chemistry, 1995 , vol. 38, # 7 p. 1106 - 1118

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Citation Number: 50

Abstract

A series of analogs based on a novel template, ll-aza-(20S)-camptothecin, were obtained from total synthesis and tested as potential anticancer drugs in the topoisomerase I enzyme cleavable complex assay. The parent compound 1 l-aza-(20S)-camptothecin (8) was derived from a Friedlander condensation between the known aminopyridine derivative 3-(3- amino-4-picoly1idene) ptoluidine and optically active tricyclic ketone 7. Compound 8 had ...