Cui, Xinxin; Du, Kunda; Yuan, Xiaoyin; Xiao, Wen; Tao, Yayu; Xu, Defeng; Hu, Hang published the artcile< A comparative study of the in vitro antitumor effect of mannose-doxorubicin conjugates with different linkers>, Synthetic Route of 5505-63-5, the main research area is doxorubicin mannose conjugate antitumor agent drug delivery system; conjugate; doxorubicin; mannose.
In this work, five Man-DOX conjugates with different linkers were developed for targeted DOX delivery. The five Man-DOX conjugates with different linkers were characterized by 1H NMR, HRMS, HPLC, UV-vis, and fluorescence spectroscopy. Man-Suc-DOX, Man-TDG-DOX, and Man-DG-DOX can self-assemble into near-spherical nanoparticles with hydrodynamic diameters of 150-200 nm and neg. ζ potentials in deionized water, whereas Man-SS-DOX and Man-SeSe-DOX are hardly dispersed in deionized water. The self-assembly behaviors of Man-Suc-DOX, Man-TDG-DOX, and Man-DG-DOX were studied by dissipative particle dynamics simulation and the results show that Man-Suc-DOX, Man-TDG-DOX, and Man-DG-DOX all self-assemble into spherical particles with Man and linkers on the surfaces and DOX in the interiors. The in vitro drug release study shows that Man-Suc-DOX, Man-TDG-DOX, and Man-DG-DOX exhibit limited drug release, while Man-SS-DOX and Man-SeSe-DOX exhibit glutathione-responsive drug release. The cellular uptake study shows that Man-DG-DOX exhibits the highest cellular uptake amount on HepG2 cells. Finally, Man-DG-DOX exhibits the best in vitro antitumor effect against HepG2 cells among the five Man-DOX conjugates with different linkers. Although the in vitro antitumor activity of Man-DG-DOX is still lower than free DOX, Man-DG-DOX shows significant selectivity toward HepG2 cells. Man-DG-DOX might achieve selective DOX delivery for mannose receptor overexpressed tumors.
Drug Development Research published new progress about Antitumor agents. 5505-63-5 belongs to class alcohols-buliding-blocks, and the molecular formula is C6H14ClNO5, Synthetic Route of 5505-63-5.
Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts