Synthesis and mechanism of action of novel pyrimidinyl pyrazole derivatives possessing antiproliferative activity.
Bioorg Med Chem Lett
; 12(21): 3191-3, 2002 Nov 04.
Article
in En
| MEDLINE
| ID: mdl-12372531
ABSTRACT
Pyrimidinyl pyrazole derivatives 1-4, prepared as a new scaffold of an anti-tumor agent, showed antiproliferative activity against human lung cancer cell lines and inhibited tubulin polymerization. Furthermore, it was found that compound 2 bound at the colchicine site on tubulin, but the tubulin binding pattern was different from that of colchicine. Here, we describe the synthesis of the derivatives and the differences of the action mechanism on tubulin polymerization inhibition between compound 2 and colchicine.
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Collection:
01-internacional
Database:
MEDLINE
Main subject:
Pyrazoles
/
Pyrimidines
/
Antineoplastic Agents
Limits:
Humans
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2002
Document type:
Article
Affiliation country:
Japan
Country of publication:
ENGLAND
/
ESCOCIA
/
GB
/
GREAT BRITAIN
/
INGLATERRA
/
REINO UNIDO
/
SCOTLAND
/
UK
/
UNITED KINGDOM