Synthesis of a Terminal Amino‐Modified Nucleolin Aptamer and Its Paclitaxel Conjugate

Aptamer‐drug conjugate has been developed as a potential class of targeted therapeutics, which using aptamer as tumor recognition elements could targeted deliver the conjugated chemically toxic drug to tumor site. One of the keys to the success of aptamer‐drug conjugate is terminal modification of aptamer to facilitate the conjugation with drugs. Herein, a novel terminal amino‐modified nucleolin aptamer which using solketal as raw material was developed. Moreover, its paclitaxel conjugate wherein the aptamer coupled with paclitaxel derivatives by amidation was also conducted. The easily available raw materials, stable structure, together with its simplicity of operation, gives it the potential for use on an industrial scale. Aptamer‐drug conjugate has been developed as a potential class of targeted therapeutics, which using aptamer as tumor recognition elements could targeted deliver the conjugated chemically toxic drug to tumor site. One of the keys to the success of aptamer‐drug conjugate is terminal modification of aptamer to facilitate the conjugation with drugs. Herein, a novel terminal amino‐modified nucleolin aptamer which using solketal as raw material was developed. Moreover, its paclitaxel conjugate wherein the aptamer coupled with paclitaxel derivatives by amidation was also conducted. The easily available raw materials, stable structure, together with its simplicity of operation, gives it the potential for use on an industrial scale.