30664-77-8Relevant academic research and scientific papers
Evaluation of inhibitory actions of flavonols and related substances on lysophospholipase D activity of serum autotaxin by a convenient assay using a chromogenic substrate
Ueda, Kaori,Yoshihara, Masanori,Nakao, Michiyasu,Tanaka, Tamotsu,Sano, Shigeki,Fukuzawa, Kenji,Tokumura, Akira
experimental part, p. 6053 - 6063 (2011/08/09)
Overproduction of lysophosphatidic acid (LPA) by lysophospholipase D/autotaxin (lysoPLD/ATX) is postulated to be involved in the promotion of cancer and atherosclerosis. A lysoPLD inhibitor may be utilized to ameliorate the LPA-related pathological condit
Synthesis and evaluation of anti-tumor activities of N4 fatty acyl amino acid derivatives of 1-β-arabinofuranosylcytosine
Liu, Boyang,Cui, Chunying,Duan, Wei,Zhao, Ming,Peng, Shiqi,Wang, Lili,Liu, Hu,Cui, Guohui
scheme or table, p. 3596 - 3600 (2009/12/04)
1-β-d-Arabinofuranosylcytosine (Ara-C, Cytarabine) is one of the drugs used for acute nonlymphocytic leukemia (ANLL). However, the bioavailability of Ara-C is relatively low due to its low lipophilicity. In order to improve the lipophilicity and bioavailability of Ara-C, a series of N4 derivatives of Ara-C, i.e., (fatty acid)-(amino acid)-Ara-C analogues, were prepared. The 15 derivatives synthesized were characterized by their melting points, optical rotations and partition coefficients. It was found that the Ara-C derivatives synthesized in this study were more lipophilic than Ara-C as determined by their partition coefficients. Their in vitro cytotoxicity and in vivo anti-tumor activity were determined and compared with that of Ara-C. It was found that the derivatives were more active than Ara-C in Hela cells, but not in HL-60 cells. The in vivo results showed that some of the derivatives were more effective than Ara-C in mice bearing S180 tumor while others showed a decreased activity in comparison with Ara-C.
Synthetic libraries of tyrosine-derived bacterial metabolites
Georgiades, Savvas N.,Clardy, Jon
supporting information; experimental part, p. 3117 - 3121 (2009/04/03)
The preparation of a collection of 131 small molecules, reminiscent of families of long chain N-acyl tyrosines, enamides and enol esters that have been isolated from heterologous expression of environmental DNA (eDNA) in Escherichia coli, is reported. The synthetic libraries of N-acyl tyrosines and their 3-keto counterparts were prepared via solid-phase routes, whereas the enamides and enol esters were synthesized in solution-phase.
