Structure-activity relationship studies of thalidomide analogs with a taxol-like mode of action.
Bioorg Med Chem Lett
; 23(24): 6902-4, 2013 Dec 15.
Article
in En
| MEDLINE
| ID: mdl-24169233
ABSTRACT
Anti-microtubule agents such as paclitaxel and docetaxel have played an important role in the treatment of cancer for many years. Recently, a small molecule that has a taxol-like mode of action (5HPP-33) was reported. Herein, the detailed structure-activity relationship (SAR) studies of 5HPP-33 analogs that are substituted at the isoindole and phenyl rings are described. Bulky substitutions (such as di-isopropyl groups) on the phenyl ring result in the isoindole and phenyl rings being perpendicular to each other. It was found that this conformation is critical for anti-microtubule activity. These studies have provided valuable information, which will be helpful in the design of more potent analogs.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Thalidomide
/
Paclitaxel
/
Tubulin Modulators
/
Isoindoles
/
Microtubules
Limits:
Humans
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2013
Document type:
Article
Affiliation country:
United States