73414-58-1Relevant articles and documents
Bromo-tyrosine alkaloidal compound as well as preparation method and application thereof
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Paragraph 0045-0048, (2018/04/03)
The invention belongs to the field of a medical technology, and concretely relates to a bromo-tyrosine alkaloidal compound as well as a preparation method and application thereof. The invention provides the bromo-tyrosine alkaloidal compound as shown in a general formula I and a general formula II, the preparation method thereof, and the application thereof in preparing an antitumor drug for the first time. The bromo-tyrosine alkaloidal compound has good antineoplastic activity, the preparation method is simple and feasible, the yield is better, and the bromo-tyrosine alkaloidal compound has abroad application prospect.
Synthesis of novel purpurealidin analogs and evaluation of their effect on the cancer-relevant potassium channel KV10.1
Moreels, Lien,Bhat, Chinmay,Vorá?ová, Manuela,Peigneur, Steve,Goovaerts, Hannah,M?ki-Lohiluoma, Eero,Zahed, Farrah,Pardo, Luis A.,Yli-Kauhaluoma, Jari,Kiuru, Paula,Tytgat, Jan
, (2017/12/15)
In the search for novel anticancer drugs, the potassium channel KV10.1 has emerged as an interesting cancer target. Here, we report a new group of KV10.1 inhibitors, namely the purpurealidin analogs. These alkaloids are produced by the Verongida sponges and are known for their wide variety of bioactivities. In this study, we describe the synthesis and characterization of 27 purpurealidin analogs. Structurally, bromine substituents at the central phenyl ring and a methoxy group at the distal phenyl ring seem to enhance the activity on KV10.1. The mechanism of action of the most potent analog 5 was investigated. A shift of the activation curve to more negative potentials and an apparent inactivation was observed. Since KV10.1 inhibitors can be interesting anticancer drug lead compounds, the effect of 5 was evaluated on cancerous and non-cancerous cell lines. Compound 5 showed to be cytotoxic and appeared to induce apoptosis in all the evaluated cell lines.
The synthetic and biological studies of discorhabdins and related compounds
Wada, Yasufumi,Harayama, Yu,Kamimura, Daigo,Yoshida, Masako,Shibata, Tomoyuki,Fujiwara, Kousaku,Morimoto, Koji,Fujioka, Hiromichi,Kita, Yasuyuki
scheme or table, p. 4959 - 4976 (2011/08/06)
Various analogues of the marine alkaloids, discorhabdins, have been synthesized. The strategy contains spirocyclization with phenyliodine(iii) bis(trifluoroacetate) (PIFA), oxidative fragmentation of the β-amino alcohols with the hypervalent iodine reagent C6F 5I(OCOCF3)2, the detosylation and dehydrogenation reaction of the pyrroloiminoquinone unit in the presence of a catalytic amount of NaN3 and the bridged ether synthesis with HBr-AcOH as the key reactions. All the synthesized compounds were evaluated by in vitro MTT assay for cytotoxic activity against the human colon cancer cell line HCT-116. Furthermore, the discorhabdin A oxa analogues were also evaluated against four kinds of tumor model cells, a human colon cancer cell line (WiDr), a human prostate cancer cell line (DU-145) and murine leukemia cell lines (P388 and L1210). For the identification of the target, discorhabdin A and the discorhabdin A oxa analogue were evaluated by an HCC panel assay. In the test, discorhabdins could have a novel mode of action with the tumor cells. The Royal Society of Chemistry 2011.
