scholarly journals Studies on antitumor-active 2,3-dioxopiperazine derivatives. III. Synthesis and structure-antitumor activity relationship of 1-(4-aminobenzyl)-2,3-dioxopiperazine derivatives.

1981 ◽  
Vol 29 (5) ◽  
pp. 1253-1266 ◽  
Author(s):  
TAKAKO HORI ◽  
CHOSAKU YOSHIDA ◽  
SHOHACHI MURAKAMI ◽  
YASUO KIBA ◽  
RYUKO TAKENO ◽  
...  
1981 ◽  
Vol 4 (1) ◽  
pp. 58-64 ◽  
Author(s):  
MOTOKO INOMATA ◽  
FUMIKO FUKUOKA ◽  
AKIO HOSHI ◽  
KAZUO KURETANI ◽  
MINEO SANEYOSHI

1993 ◽  
Vol 46 (9) ◽  
pp. 1439-1446 ◽  
Author(s):  
MASARU KAMISHOHARA ◽  
HIROYUKI KAWAI ◽  
ATSUO ODAGAWA ◽  
TOSHIYUKI ISOE ◽  
JUN-ICHIRO MOCHIZUKI ◽  
...  

2016 ◽  
Vol 32 (6) ◽  
pp. 929-937 ◽  
Author(s):  
Hongshuang Li ◽  
Xinran Wang ◽  
Guiyun Duan ◽  
Chengcai Xia ◽  
Yuliang Xiao ◽  
...  

Author(s):  
Zhonghao Sun ◽  
Shuxian Yang ◽  
Chengfang Xu ◽  
Guoxu Ma ◽  
Li Cao ◽  
...  

(-)-Zeylenone is a promising cytotoxic agent,which is a natural product isolated from Uvaria grandiflora Roxb. Though substantial antitumor mechanism has been researched , little has focused on its enantiomer (+)-Zeylenone.This article will try to find a gram scale synthesis method of (+)-Zeylenone and explain the structure-activity relationship of this kind of compound. Total synthesis of (+)-zeylenone was completed in 13 steps with quinic acid as starting material in 8.8% overall yield. The highlight of the route was the control of the three carbon’s chirality by clever use of single step dihydroxylation under the direction of the key C-3 chirality. In addition, zeylenone derivatives were designed and synthesized and their antitumor activity were evaluated against three human cancer cell lines using the CCK8 assay. Structure-activity relationship suggested compounds with both two absolute configurations exhibited good activity. Besides, hydroxyls at C-1/2 position were crucial for the activity and esterification of C-1 hydroxyl with large groups made the activity disappeared. Hydroxyl at C-3 position was also important as proper ester substituent could increase the potency.


1996 ◽  
Vol 6 (11) ◽  
pp. 1247-1252 ◽  
Author(s):  
Pier Giovanni Baraldi ◽  
Italo Beria ◽  
Barbara Cacciari ◽  
Laura Capolongo ◽  
Paolo Cozzi ◽  
...  

Sign in / Sign up

Export Citation Format

Share Document