Synthesis and structure-activity relationship of 2-aminobenzophenone derivatives as antimitotic agents.
J Med Chem
; 45(12): 2556-62, 2002 Jun 06.
Article
em En
| MEDLINE
| ID: mdl-12036364
ABSTRACT
A new type of inhibitor of tubulin polymerization was discovered on the basis of the combretastatin molecular skeleton. The lead compounds in this series, compounds 6 and 7, strongly inhibited tubulin polymerization in vitro and significantly arrested cells at the G(2)/M phase. Compounds 6 and 7 yielded 50- to 100-fold lower IC(50) values than did combretastatin A-4 against Colo 205, NUGC3, and HA22T human cancer cell lines as well as similar or greater growth inhibitory activities than did combretastain A-4 against DLD-1, HR, MCF-7, DU145, HONE-1, and MES-SA/DX5 human cancer cell lines. Structure-activity relationship information revealed that introduction of an amino group at the ortho position of the benzophenone ring plays an integral role for increased growth inhibition.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Benzofenonas
/
Antineoplásicos
Limite:
Humans
Idioma:
En
Revista:
J Med Chem
Ano de publicação:
2002
Tipo de documento:
Article