5394-87-6Relevant articles and documents
Synthesis and Evaluation of Structurally Diverse C-2-Substituted Thienopyrimidine-Based Inhibitors of the Human Geranylgeranyl Pyrophosphate Synthase
Boutin, Rebecca,Guan, Tian Lai,Lacbay, Cyrus M.,Lee, Hiu-Fung,Matralis, Alexios N.,Park, Jaeok,Sebag, Michael,Tsantrizos, Youla S.,Waller, Daniel D.
, (2022/02/10)
Novel analogues of C-2-substituted thienopyrimidine-based bisphosphonates (C2-ThP-BPs) are described that are potent inhibitors of the human geranylgeranyl pyrophosphate synthase (hGGPPS). Members of this class of compounds induce target-selective apoptosis of multiple myeloma (MM) cells and exhibit antimyeloma activity in vivo. A key structural element of these inhibitors is a linker moiety that connects their (((2-phenylthieno[2,3-d]pyrimidin-4-yl)amino)methylene)bisphosphonic acid core to various side chains. The structural diversity of this linker moiety, as well as the side chains attached to it, was investigated and found to significantly impact the toxicity of these compounds in MM cells. The most potent inhibitor identified was evaluated in mouse and rat for liver toxicity and systemic exposure, respectively, providing further optimism for the potential value of such compounds as human therapeutics.
Stereoselective insertion of rhodium carbenoid to water under control with intramolecular participation of hydroxy group
Sugimura, Takashi,Nagai, Takao
, p. 286 - 287 (2008/09/20)
A chiral diazo ester having a hydroxy group in the proper geometry produces an adduct with water up to 92% de upon treatment with a rhodium catalyst. This high stereoselectivity is attributable to the intramolecular hydrogen bond between the internal hydroxy group and the rhodium carbenoid. Copyright
