20377-03-1Relevant articles and documents
POLYHETEROCYCLIC COMPOUNDS AS METTL3 INHIBITORS
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Page/Page column 338, (2021/06/11)
The present invention relates to compounds of formula (I) that function as inhibitors of METTL3 (N6-adenosine-methyltransferase 70 kDa subunit) enzyme activity: X-Y-Z (I) wherein X, Y and Z are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, and autoimmune diseases, as well as other diseases or conditions in which METTL3 activity is implicated.
Biological evaluation of new mimetics of annonaceous acetogenins: Alteration of right scaffold by click linkage with aromatic functionalities
Liu, Yanghan,Xiao, Qicai,Liu, Yongqiang,Li, Zheng,Qiu, Yatao,Zhou, Guang-Biao,Yao, Zhu-Jun,Jiang, Sheng
, p. 248 - 258 (2014/04/17)
A small library of analogues of annonaceous acetogenins through click linkage with aromatic moieties is established using a convergent modular fragment-assembly approach. These analogues exhibited low micromolar inhibitory activities against the proliferation of several human cancer cell lines. Structure-activity relationship (SAR) of these analogues indicates that replacement of the methoxy groups of ubiquinone ring with methyl groups is proved to be a useful strategy for improving the anticancer activity of quinone-acetogenin hybrids.
Photolysis of Quinolyl and Isoquinolyl Azides in Primary and Secondary Aliphatic Amines: Synthesis of Bicyclic Azepines, Diazepines, and Quinolyl- and Isoquinolyl-diamines
Hollywood, Frank,Nay, Barry,Scriven, Eric F. V.,Suschitzky, Hans,Khan, Zafar U.,Hull, Roy
, p. 421 - 429 (2007/10/02)
Photolysis of the title compounds in primary aliphatic amines gave in some cases bicyclic azepines and diazepines as well as o-diamines, while in secondary amines mainly the appropriate o-diamines are obtained.On the basis of the many examples studied guidelines are put forward to predict the nature of products from photolysis of bicyclic azides in primary and secondary amines and to obtain maximum yields.