[Chemistry and antitumor activity of hainanensine analogues].
A synthetic analogue of hainanensine 2a was further modified in order to improve its antitumor activity. Six compounds 3-8, were obtained, and among these compounds 8 showed significant activity. The diastereomer (+/-)8B was resolved by (+) tartaric acid and (-)benzoyl-tartaric acid to the corresponding enantiomers (-)8B and (+)8B, respectively and their optical purities were determined by isotope dilution method as 93% and 96%. The antitumor activity of the newly obtained compounds were tested in vitro, and (-)8B was found to have an IC50 of 1.9 mol/L, eighteen times higher than the original compound 2a.
Yin
D L
DL
Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing.
Xu
C X
CX
Gao
Y S
YS
Liu
D K
DK
Wen
S Y
SY
Guo
J Y
JY
D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D006248:Harringtonines / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D007939:Leukemia L1210 / Q000188:drug therapy; D051379:Mice; D015394:Molecular Structure
D000972:Antineoplastic Agents, Phytogenic; D006248:Harringtonines; C030424:hainanensine