1208222-55-2Relevant academic research and scientific papers
Structural insights into the design of small molecule inhibitors that selectively antagonize Mcl-1
Bernardo, Paul H.,Sivaraman, Thirunavukkarasu,Wan, Kah-Fei,Xu, Jin,Krishnamoorthy, Janarthanan,Sons, Chun Meng,Tian, Liming,Chin, Jasmine S. F.,Lim, Diane S. W.,Mok, Henry Y. K.,Yu, Victor C.,Tong, Joo Chuan,Chai, Christina L. L.
, p. 2314 - 2318 (2010)
The screening of a small focused library of rhodanine derivatives as inhibitors of Bcl-2 proteins led to the discovery of two structurally related compounds with different binding profiles against the Bcl-XL and the Mcl-1 proteins. Subsequent NMR studies with mutant proteins and in silico docking studies provide a possible rationale for the observed specificity.
BIARYLRHODANINE AND PYRIDYLRHODANINE COMPOUNDS AND THEIR USE
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Page/Page column 82; 83, (2010/04/06)
The present invention pertains generally to the field of therapeutic compounds, and more specifically to compounds related to rhodanine, which compounds are inter alia inhibitors and/or binders of antiapoptotic/pro-survival Bcl-2 proteins such as Bcl-XL and/or Mcl-1. More specifically, the present invention is concerned with Rhodanine- based Pan-Bcl-2 inhibitors and Mcl-1 -specific inhibitors as anti-cancer compounds. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and invivo, to inhibit and/or bind Bcl-2 proteins such as Bcl-XL and/or Mcl-1, and in the treatment of diseases and conditions that are mediated by Bcl-2 proteins, that are ameliorated by the inhibition of Bcl-2 protein function (such as Bcl-XL and/or Mcl-1 ) including proliferative conditions such as cancer, optionally in combination with another agent.
