41361-60-8Relevant articles and documents
Antitumor Potential of the Isoflavonoids (+)- And (-)-2,3,9-Trimethoxypterocarpan: Mechanism-of-Action Studies
Banwell, Martin G.,Bezerra, Eveline M.,Da Costa, Roner F.,De Moraes, Manoel O.,De Oliveira, Maria Da C. F.,Diniz-Filho, Jairo,Farias, Kaio,Freire, Valder N.,Gardiner, Michael G.,Guest, Prue,Ma, Xinghua,Meira, Assuero S.,Nikahd, Maryam,Do ó Pessoa, Claudia
, p. 1274 - 1280 (2020)
Synthetically derived samples of (+)-(6aS,11aS)-2,3,9-trimethoxypterocarpan [(+)-1] and its enantiomer [(-)-1], both of which are examples of naturally occurring isoflavonoids, were evaluated, together with the corresponding racemate, as cytotoxic agents against the HL-60, HCT-116, OVCAR-8, and SF-295 tumor cell lines. As a result it was established that compound (+)-1 was particularly active with OVCAR-8 cells being the most sensitive and responding in a dose-dependent manner. A study of cell viability and drug-induced morphological changes revealed the compound causes cell death through a mechanism characteristic of apoptosis. Finally, a computational study of the interactions of compound (+)-1 and (S)-monastrol, an established, synthetically derived, potent, and cell-permeant inhibitor of mitosis, with the kinesin-type protein Eg5 revealed that both bind to this receptor in a similar manner. Significantly, compound (+)-1 binds with greater affinity, an effect attributed to the presence of the associated methoxy groups.
NOVEL COMPOUND OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS ACTIVE INGREDIENT
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Paragraph 0186-0188, (2015/05/26)
The present invention relates to a novel compound inhibiting Hsp 90 and to a pharmaceutical composition including same as an active ingredient. Compounds of formula 1 and formula 2 according to the present invention inhibit the accumulation of HIF-1α protein, which is an Hsp90 client protein, by suppressing Hsp90 expression, and effectively inhibit the activity of vascular endothelial growth factor (VEGF). Furthermore, said compounds have low cytotoxicity and can thus be used as an active ingredient for the treatment of diabetic retinopathy and arthritis.
Identification of small molecule inhibitors of the STAT3 signaling pathway: Insights into their structural features and mode of action
Kim, Kyeojin,Kim, Su-Jung,Han, Young Taek,Hong, Sung-Jun,An, Hongchan,Chang, Dong-Jo,Kim, Taewoo,Lim, Bumhee,Lee, Jeeyeon,Surh, Young-Joon,Suh, Young-Ger
, p. 5444 - 5448 (2015/11/09)
A series of novel STAT3 inhibitors consisting of Michael acceptor has been identified through assays of the focused in-house library. In addition, their mode of action and structural feature responsible for the STAT3 inhibition were investigated. In parti