- 作者: 吳明忠 ; 林志峰 ; 井寶柱 ; 張麗娟 ; 杜采潓 ; 李芳城 ; 陳惠婷
- 作者服務機構: School of Chemistry, Kaohsiung Medical College, Kaohsiung, Taiwan, R.O.C.
- 中文摘要: (Z)-7-Sulfonyl-3-hexen-1,5-diyne containing molecules are stable at room temperature and isomerized to eneyne-allene-sulfones under alkaline conditions. These eneyne-allene-sulfones were not isolable, spontaneously cyclized to form biradical intermediates under mild conditions, and exhibited good DNA-cleaving and human tumor cell line growth inhibition properties. Further studies indicated that compounds bearing on aromatic ring at C(3) and C(4), such as 25, proved to be more active against those tumor cell lines. Removal of acetylene unit at C(1) and C(2), made the resulting compound less active. A related compound, (Z,Z)-12-(2-tetrahydropyranyl)oxy-1-phenylsulfontldodeca-4,8-diene-2,6,10-triyen (37), was synthesized. Upon treatment of triethylamine at refluxing benzene, this compound undergoes double cycloaromatization to from a naphalene adduct, which possesses excellent DNA-cleaving activity.
- 英文摘要: --
- 中文關鍵字: Sulfony1 Hexen Diyne; Eneyne; Allenesulfone; Dna; Antitumor Antibiotics
- 英文關鍵字: 磺醯己烯二炔;烯炔;丙二烯;去氧核糖核酸;抗癌抗生素