Lee, Hiu-Fung published the artcileSynthesis and Evaluation of Structurally Diverse C-2-Substituted Thienopyrimidine-Based Inhibitors of the Human Geranylgeranyl Pyrophosphate Synthase, Category: alcohols-buliding-blocks, the publication is Journal of Medicinal Chemistry (2022), 65(3), 2471-2496, database is CAplus and MEDLINE.
Novel analogs 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 CML-07-119(13c)(I) was evaluated in mouse and rat for liver toxicity and systemic exposure, resp., providing further optimism for the potential value of such compounds as human therapeutics.
Journal of Medicinal Chemistry published new progress about 90-64-2. 90-64-2 belongs to alcohols-buliding-blocks, auxiliary class Carboxylic acid,Benzene,Alcohol,Natural product, name is 2-Hydroxy-2-phenylacetic acid, and the molecular formula is C8H8O3, Category: alcohols-buliding-blocks.
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