2638-15-5Relevant articles and documents
Synthesis of Psoralidin derivatives and their anticancer activity: First synthesis of Lespeflorin I1
Pahari, Pallab,Saikia, Ujwal Pratim,Das, Trinath Prasad,Damodaran, Chendil,Rohr, Jürgen
, p. 3324 - 3334 (2016/05/19)
Synthetic scheme for the preparation of a number of different derivatives of anticancer natural product Psoralidin is described. A convergent synthetic approach is followed using simple starting materials like substituted phenyl acetic esters and benzoic acids. The developed synthetic route leads us to complete the first synthesis of an analogous natural product Lespeflorin I1, a mild melanin synthesis inhibitor. Preliminary bioactivity studies of the synthesized compounds are carried out against two commonly used prostate cancer cell lines. Results show that the bioactivity of the compounds can be manipulated by the simple modification of the functional groups.
Design, synthesis, and evaluation of postulated transient intermediate and substrate analogues as inhibitors of 4-hydroxyphenylpyruvate dioxygenase
Lin, Yun-Loung,Huang, Jian-Lin,Wu, Chung-Shieh,Liu, Hung-Ge,Yang, Ding-Yah
, p. 1709 - 1713 (2007/10/03)
An epoxybenzoquinone, 4-hydroxyphenoxypropionic acid, and 2-hydroxy-3-phenyl-3-butenoic acid derivatives have been designed, synthesized, and evaluated for in vitro inhibition activity against 4-hydroxyphenylpyruvate dioxygenase (4-HPPD) from pig liver by the spectrophotometric enol-borate method. The biological data demonstrated that neither epoxybenzoquinone ester nor 2-hydroxy-3-phenyl-3-butenoic acid is an inhibitor of 4-HPPD. The most potent 4-HPPD inhibitor tested was 3-hydroxy-4-phenyl-2(5H)-furanone with an IC50 value of 0.5 μM, which may serve as a lead compound for further design of more potent 4-HPPD inhibitors.