Structure-activity relationship of novel tallimustine derivatives: synthesis and antitumor activity

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

Synthesis, antitumor activity and preliminary structure-activity relationship of 2-aminothiazole derivatives

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

scholarly journals Concise Total Synthesis of (+)-Zeylenone with Antitumor Activity and Structure-Activity Relationship of Its Derivatives

2019 ◽  
Author(s):  
Zhonghao Sun ◽  
Shuxian Yang ◽  
Chengfang Xu ◽  
Guoxu Ma ◽  
Li Cao ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Total Synthesis ◽  
Human Cancer ◽  
Synthesis Method ◽  
Structure Activity Relationship ◽  
Single Step ◽  
Activity Relationship ◽  
Human Cancer Cell Lines ◽  
Structure Activity ◽  
Relationship Of

(-)-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.

Structure-activity relationship of novel distamycin a derivatives : synthesis and antitumor activity

1994 ◽  
Vol 4 (12) ◽  
pp. 1467-1472 ◽  
Author(s):  
Roberto D'Allessio ◽  
Cristina Geroni ◽  
Giovanni Biasoli ◽  
Enrico Pesenti ◽  
Maria Grandi ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Distamycin A ◽  
Structure Activity ◽  
Relationship Of

Structure–activity relationship of phosmidosine: importance of the 7,8-dihydro-8-oxoadenosine residue for antitumor activity

2004 ◽  
Vol 12 (19) ◽  
pp. 5193-5201 ◽  
Author(s):  
Mitsuo Sekine ◽  
Kazuhisa Okada ◽  
Kohji Seio ◽  
Hideaki Kakeya ◽  
Hiroyuki Osada ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Structure Activity ◽  
Relationship Of
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