An easy microwave-assisted synthesis of C8-alkynyl adenine pyranonucleosides as novel cytotoxic antitumor agents

作者：Dimopoulou Athina; Manta Stella; Parmenopoulou Vanessa; Kollatos Nikolaos; Christidou Ourania; Triantakonstanti Virginia V; Schols Dominique; Komiotis Dimitri^*

来源：Frontiers in Chemistry, 2015, 3: 21.

DOI：10.3389/fchem.2015.00021

• Sonogashira coupling reaction
• 8-bromoadenine
• N-6-benzoyladenine pyranonucleosides
• microwave irradiation
• cytotoxic activity

We describe the synthesis of C8-alkynyl adenine pyranonucleosides 4, 5, and 8-phenylethynyl-adenine (II), via Sonogashira cross-coupling reaction under microwave irradiation. Compounds 4e and II were less cytostatic than 5-fluorouracil (almost an order of magnitude) against murine leukemia (L1210) and human cervix carcinoma (HeLa) cells, while the same compounds proved to be more active than 5-fluorouracil against human lymphocyte (CEM) cells.

• 出版日期2015-3-23
• 单位河北医科大学