100200-87-1Relevant academic research and scientific papers
SYNTHESIS OF PHENOLS FROM METAL-CARBYNES AND DIYNES
Sivavec, Timothy M.,Katz, Thomas J.
, p. 2159 - 2162 (1985)
Metal-carbynes RCM(CO)4Br with diacetylenes give specific phenols in good yield.The reactions take only a few minutes at or below room temperature.
Computer-Assisted Discovery and Structural Optimization of a Novel Retinoid X Receptor Agonist Chemotype
Heitel, Pascal,Gellrich, Leonie,Kalinowsky, Lena,Heering, Jan,Kaiser, Astrid,Ohrndorf, Julia,Proschak, Ewgenij,Merk, Daniel
, p. 203 - 208 (2019/01/25)
As universal heterodimer partners of many nuclear receptors, the retinoid X receptors (RXRs) constitute key transcription factors. They regulate cell proliferation, differentiation, inflammation, and metabolic homeostasis and have recently been proposed as potential drug targets for neurodegenerative and inflammatory diseases. Owing to the hydrophobic nature of RXR ligand binding sites, available synthetic RXR ligands are lipophilic, and their structural diversity is limited. Here, we disclose the computer-assisted discovery of a novel RXR agonist chemotype and its systematic optimization toward potent RXR modulators. We have developed a nanomolar RXR agonist with high selectivity among nuclear receptors and superior physicochemical properties compared to classical rexinoids that appears suitable for in vivo applications and as lead for future RXR-targeting medicinal chemistry.
Photoinduced DNA cleavage by designed molecules with conjugated ene-yne-ketene functionalities
Nakatani, Kazuhiko,Isoe, Sachihiko,Maekawa, Satoshi,Saito, Isao
, p. 605 - 608 (2007/10/02)
Upon photoirradiation, diazoketone 1 was found to induce single strand cleavage of plasmid pBR322 DNA at concentration of 100 μM. Conjugate ene-yne moiety was essential for DNA-cleaving activities.
