54950-20-8Relevant articles and documents
An Alternate Synthesis of Deethylvincadifformine
Wenkert, Ernest,Orito, Kazuhiko,Simmons, Dana P.,Ardisson, Janick,Kunesch, Nicole,Poisson, Jacques
, p. 5006 - 5009 (1983)
A synthesis of 20-deethylvincadifformine from methyl nicotinylacetate is described.The reaction scheme involved a fast construction of the pentacyclic nucleus of the Aspidosperma alkaloids and the early incorporation of the 16-carbomethoxy group common to these bases.
NEW ANALOGS AS ANDROGEN RECEPTOR AND GLUCOCORTICOID RECEPTOR MODULATORS
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Paragraph 0276; 0277; 0278; 0279, (2019/05/16)
The present invention relates to novel dihydropyridine derivatives of formula (I): as modulators of nuclear receptors selected from androgen receptor and glucocorticoid receptor, to processes for their preparation, to pharmaceutical compositions comprising said compounds and to the use of said for manufacturing a medicament for the treatment of pathological conditions or diseases that can improve by modulation of androgen receptor and/or glucocorticoid receptor, selected from cancer, metastasizing cancers, benign prostate hyperplasia, polycystic ovary syndrome (PCOS), hair loss, hirsutism, acne, hypogonadism, muscle wasting diseases, cachexia, Cushing's syndrome, anti-psychotic drug induced weight gain, obesity, post-traumatic stress disorder and alcoholism.
Quinone-Fused Pyrazoles through 1,3-Dipolar Cycloadditions: Synthesis of Tricyclic Scaffolds and in vitro Cytotoxic Activity Evaluation on Glioblastoma Cancer Cells
Bertuzzi, Giulio,Crotti, Simone,Calandro, Pierpaolo,Bonini, Bianca Flavia,Monaco, Ilaria,Locatelli, Erica,Fochi, Mariafrancesca,Zani, Paolo,Strocchi, Elena,Mazzanti, Andrea,Chiariello, Mario,Franchini, Mauro Comes
supporting information, p. 1744 - 1750 (2018/09/11)
A novel and straightforward synthesis of highly substituted isoquinoline-5,8-dione fused tricyclic pyrazoles is reported. The key step of the synthetic sequence is a regioselective, Ag2CO3 promoted, 1,3-dipolar cycloaddition of C-heteroaryl-N-aryl nitrilimines and substituted isoquinoline-5,8-diones. The broad functional group tolerability and mild reaction conditions were found to be suitable for the preparation of a small library of compounds. These scaffolds were designed to interact with multiple biological residues, and two of them, after brief synthetic elaborations, were analyzed by molecular docking studies as potential anticancer drugs. In vitro studies confirmed the potent anticancer effects, showing promising IC50 values as low as 2.5 μm against three different glioblastoma cell lines. Their cytotoxic activity was finally positively correlated to their ability to inhibit PI3K/mTOR kinases, which are responsible for the regulation of diverse cellular processes in human cancer cells.