180976-98-1Relevant articles and documents
Synthesis and biological evaluation of 2,4-diaminopyrimidines as selective Aurora A kinase inhibitors
Qin, Wen-Wen,Sang, Chun-Yan,Zhang, Lin-Lin,Wei, Wei,Tian, Heng-Zhi,Liu, Huan-Xiang,Chen, Shi-Wu,Hui, Ling
, p. 174 - 184 (2015/03/31)
The Aurora kinases are a family of serine/threonine kinases that interact with components of the mitotic apparatus and serve as potential therapeutic targets in oncology. Here we synthesized 15 2,4-diaminopyrimidines and evaluated their biological activities, including antiproliferation, inhibition against Aurora kinases and cell cycle effects. These compounds generally exhibited more potent cytotoxicity against tumor cell lines compared with the VX-680 control, especially compound 11c, which showed the highest cytotoxicities, with IC50 values of 0.5-4.0 1/4M. Compound 11c had more than 35-fold more selectivity for Aurora A over Aurora B, and molecular docking analysis indicated that compound 11c form better interaction with Aurora A both from the perspective of structure and energy. Furthermore, compound 11c induced G2/M cell cycle arrest in HeLa cells. This series of compounds has the potential for further development as selective Aurora A inhibitors for anticancer activity.
Facile synthesis of benzamides to mimic an α-helix
Ahn, Jung-Mo,Han, Sun-Young
, p. 3543 - 3547 (2008/02/06)
A new α-helix mimetic was designed by using a benzamide as a rigid scaffold. It presents three functional groups corresponding to side chains of amino acids found at the i, i + 4, and i + 7 positions of an ideal α-helix, which are displayed on the same he
Inhibitors of prenyl transferases
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, (2008/06/13)
Compounds which inhibit prenyl transferases, particularly farnysyltransferase and geranylgeranyl transferase I, processes for preparing the compounds, pharmaceutical compositions containing the compounds, and methods of use.