Antiproliferative activity against MCF-7 breast cancer cells by diamino-triazaspirodiene antifolates.
Two triazaspirodienes, having similar phenoxy propyloxy side chain, were identified as potent mammalian dihydrofolate reductase inhibitors; one having a 6,5-spiro bicyclic ring system (IC(50) = 2.3 nm) and the other a 6,6-spiro bicyclic system (IC(50) = 6.9 nm). They also showed more than 50% antiproliferative activity against the MCF-7 breast cancer cells at 20 microm. This study demonstrated the potential lead of the diamino-triazaspirodienes in anticancer chemotherapeutical agents' discovery.
Ma
Xiang
X
Department of Pharmacy, Faculty of Science, National University of Singapore, Singapore, Singapore 117543. phacwk@nus.edu.sg
Woon
Renee Ser-Peng
RS
Ho
Paul Chi-Lui
PC
Chui
Wai-Keung
WK
D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology; D001372:Aza Compounds / Q000737:chemistry* / Q000494:pharmacology; D001943:Breast Neoplasms / Q000188:drug therapy*; D001643:Bridged Bicyclo Compounds / Q000737:chemistry / Q000494:pharmacology; D002417:Cattle; D045744:Cell Line, Tumor; D005260:Female; D005493:Folic Acid Antagonists / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D013141:Spiro Compounds / Q000737:chemistry* / Q000494:pharmacology; D013762:Tetrahydrofolate Dehydrogenase / Q000737:chemistry / Q000378:metabolism
D000970:Antineoplastic Agents; D001372:Aza Compounds; D001643:Bridged Bicyclo Compounds; D005493:Folic Acid Antagonists; D013141:Spiro Compounds; D013762:Tetrahydrofolate Dehydrogenase