Design and synthesis of benzylpiperidine inhibitors targeting the menin–MLL1 interface
Menin is an essential oncogenic cofactor for mixed lineage leukemia (MLL)-mediated leukemogenesis, functioning through its direct interaction with MLL1 protein. Therefore, targeting the menin–MLL1 protein–protein interface represents a promising strategy
Synthesis, cytotoxicity and topoisomerase inhibition properties of multifarious aminoalkylated indeno[1,2-c]isoquinolin-5,11-diones
A number of mono- or diaminoalkylated indeno[1,2-c]isoquinolin-5,11-diones analogs of 1 were synthesized and evaluated for their DNA binding affinities, topoisomerase inhibition properties and antiproliferative activities against human cancer cell lines (
Aryl-substituted benzimidazole and imidazopyridine ethers
Aryl substituted benzimidazole and imidazo[4,5]pyridine ethers are described as inhibitors of Cds1 and useful as adjuvants to chemotherapy or radiation therapy in the treatment of cancer.
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Page/Page column 14
(2010/02/15)
Butenolide endothelin antagonists with improved aqueous solubility
Continued development around our ET(A)-selective endothelin (ET) antagonist 1 (CI-1020) has led to the synthesis of analogues with improved aqueous solubility profiles. Poor solubility characteristics displayed by 1 required a complex buffered formulation
Patt, William C.,Cheng, Xue-Min,Repine, Joseph T.,Lee, Chet,Reisdorph, Bill R.,Massa, Mark A.,Doherty, Annette M.,Welch, Kathleen M.,Bryant, John W.,Flynn, Michael A.,Walker, Donnelle M.,Schroeder, Richard L.,Haleen, Stephen J.,Keiser, Joan A.
p. 2162 - 2168
(2007/10/03)
CNS active compounds
Compounds of the formula SPC1 Wherein X, R, n and B are as defined herein exhibit antidepressant activity.
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(2008/06/13)
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