title: Antiproliferative activity against MCF-7 breast cancer cells by diamino-triazaspirodiene antifolates.
abstract: 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.
authors.affiliation: Department of Pharmacy, Faculty of Science, National University of Singapore, Singapore, Singapore 117543. phacwk@nus.edu.sg
authors.forename: Xiang
authors.initials: X
authors.lastname: Ma
authors.forename: Renee Ser-Peng
authors.initials: RS
authors.lastname: Woon
authors.forename: Paul Chi-Lui
authors.initials: PC
authors.lastname: Ho
authors.forename: Wai-Keung
authors.initials: WK
authors.lastname: Chui
mesh_terms: 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
chemical_list: D000970:Antineoplastic Agents; D001372:Aza Compounds; D001643:Bridged Bicyclo Compounds; D005493:Folic Acid Antagonists; D013141:Spiro Compounds; D013762:Tetrahydrofolate Dehydrogenase