@article{4d68e1efc3be452b9104e0b2d2b7cd47,
title = "Anti-AIDS agents 88. Anti-HIV conjugates of betulin and betulinic acid with AZT prepared via click chemistry",
abstract = "In the present study, a new strategy to link AZT with betulin/betulinic acid (BA) by click chemistry was designed and achieved. This conjugation via a triazole linkage offers a new direction for the modification of anti-HIV triterpenes. Click chemistry provides an easy and productive way for linking two molecules, even when one of them is a large natural product. Among the newly synthesized conjugates, compounds 15 and 16 showed potent anti-HIV activity with EC 50 values of 0.067 and 0.10 μM, respectively, which are comparable to that of AZT (EC 50: 0.10 μM) in the same assay.",
author = "Bori, {Ibrahim D.} and Hung, {Hsin Yi} and Keduo Qian and Chen, {Chin Ho} and Morris-Natschke, {Susan L.} and Lee, {Kuo Hsiung}",
note = "Funding Information: This investigation was supported by Grant AI-077417 from the National Institute of Allergy and Infectious Diseases (NIAID) awarded to K.-H.L. This study was also supported in part by the Taiwan Department of Health Clinical Trial and Research Center of Excellence (DOH100-TD-B-111-004). Efficient purification of all the synthetic BA analogs was performed with a Grace Reveleris{\textregistered} flash chromatography system equipped with RevealX(TM) detection allowing for multisignal (UV/ELSD) collection to low mg quantities. Reveleris{\textregistered} Navigator method optimizer and Grace Reveleris{\textregistered} flash silica cartridges were employed for high quality separations. ",
year = "2012",
month = apr,
day = "11",
doi = "10.1016/j.tetlet.2012.02.022",
language = "English",
volume = "53",
pages = "1987--1989",
journal = "Tetrahedron Letters",
issn = "0040-4039",
publisher = "Elsevier Limited",
number = "15",
}