2,3-dibenzylbutyrolactones and 1,2,3,4-tetrahydro-2-naphthoic acid gamma-lactones: structure and activity relationship in cytotoxic activity.
Dibenzyl-g-butyrolactone and 1,2,3,4-tetrahydro-2-naphthoic acid gamma-lactone (TNL) derivatives were synthesized and evaluated for cytotoxic activity against some cancer cell lines. It was found that TNL derivatives with a shorter distance between C-4 in ring A and C'-2 in ring C were more cytotoxic, while dibenzyl-gamma-butyrolactones with a longer one were nearly inactive. In TNL series, presence of 3,4-dioxy group in ring A and 2-methoxy group in ring C was essential for the enhancement of the activity.
College of Pharmacy, Chungnam National University, Daejeon, Korea.
Yong
Y
Kim
Young-Jae
YJ
You
Nguyen-Hai
NH
Nam
Byung-Zun
BZ
Ahn
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007202:Indicators and Reagents; D007783:Lactones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D009682:Magnetic Resonance Spectroscopy; D009281:Naphthalenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013055:Spectrophotometry, Infrared; D017550:Spectroscopy, Fourier Transform Infrared; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D007202:Indicators and Reagents; D007783:Lactones; D009281:Naphthalenes