Camptothecin-20-PEG ester transport forms: the effect of spacer groups on antitumor activity

RB Greenwald, A Pendri, CD Conover, C Lee…

Index: Greenwald, Richard B.; Pendri, Annapurna; Conover, Charles D.; Lee, Chyi; Choe, Yun H.; Gilbert, Carl; Martinez, Anthony; Xia, Jing; Wu, Dechun; Hsue, Mei-mann Bioorganic and Medicinal Chemistry, 1998 , vol. 6, # 5 p. 551 - 562

Full Text: HTML

Citation Number: 117

Abstract

An improved synthesis of the hindered PEG-camptothecin diester transport form has been achieved using the Mukaiyama reagent. We have also assessed the effect of changing the electronic configuration of the (d-position of PEG-camptothecin transport forms on the rates of hydrolysis of the pro-moiety, and attempted to correlate these differences to efficacy in two animal models. In addition to the simple substitution of N for O, other synthetic ...