Synthesis of 10-substituted triazolyl artemisinins possessing anticancer activity via Huisgen 1,3-dipolar cylcoaddition.
Most of the 10-substituted triazolylartemisinin synthesized via the Huisgen 1,3-dipolar cylcoaddition of diastereomeric 10-azidoartemisinin (5, 6, and 7) with various alkynes (a-h) exhibit strong growth inhibition activity, even at sub-micromolar concentrations, against various cancer cell lines such as DLD-1, U-87, Hela, SiHa, A172, and B16. In particular, 10b and 10f showed a highly strong cytotoxicity.
Cho
Sungsik
S
Department of Basic Science, Kwandong University College of Medicine, 522 Naegok, Gangneung , Gangwon 210-701, Republic of Korea.
Oh
Sangtae
S
Um
Yumi
Y
Jung
Ji-Hee
JH
Ham
Jungyeob
J
Shin
Woon-Seob
WS
Lee
Seokjoon
S
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D037621:Artemisinins / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D003500:Cyclization; D006801:Humans; D009682:Magnetic Resonance Spectroscopy
D000970:Antineoplastic Agents; D037621:Artemisinins; C031327:artemisinin