Synthesis of topoisomerase inhibitor type anticancer drugs linked gold nanoparticles

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2008
Pekçağlıyan, Gönül
This study presents studies on camptothecin (CPT), a potent antitumor agent in order to improve its stability and solubility without reducing its activity. The work describes the modification of camptothecin at 20-OH position a new strategy to overcome the stability and solubility problems of the free drug. Camptothecin is conneted to linker that could be processed to a terminal thiol group and this thiol group was connected to gold surface, to obtain CPT-gold nanoparticles. In the first part of the study; undecenol was chosen as the starting material and reacted with azobisisobutylonitrile to obtain S-11-hydroxyundecyl ethanethioate. 11-hydroxyundecyl ethanethioate was reacted with NaOMe to synthesize the target linker 11, 11’-disulfanediyldiundecan. After synthesis of the target linker, the 20- OH functional group of CPT was replaced with this linker to obtain 20- (11, 11’-disulfanediyldiundecan) - captothecin. The second part of the study, gold nanoparticles were synthesized by using HAuCl4 solution and the camptothecin derivative containing thiol group at 20-OH position was connected to the gold surface.

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Citation Formats
G. Pekçağlıyan, “Synthesis of topoisomerase inhibitor type anticancer drugs linked gold nanoparticles,” M.S. - Master of Science, Middle East Technical University, 2008.