50343-02-7Relevant articles and documents
NOVEL SMALL MOLECULE DRUG CONJUGATES OF GEMCITABINE DERIVATIVES
-
Page/Page column 52, (2019/08/26)
Disclosed are compounds having formula (I) or a pharmaceutically acceptable salt, ester, amide, solvate, or stereoisomer thereof, wherein L, Y1, Y2, Y3, Y4, Y5, Z1, Z2, Z3, Z4, Z5, Z6, and Effector are each as defined in the specification; compositions thereof; uses thereof; and methods of use thereof.
LABELLED COUMARIN DERIVATIVES
-
Page/Page column 13-14, (2016/07/05)
The present invention relates to compounds having selective binding for MAO-B as compared with MAO-A. The invention also provides radioactive versions of these compounds, and precursor compounds for the synthesis of these radioactive compounds. The radioactive compounds of the invention can find use for in vivo imaging applications.
A Novel Covalent mTOR Inhibitor, DHM25, Shows in Vivo Antitumor Activity against Triple-Negative Breast Cancer Cells
Fouqué, Amélie,Delalande, Olivier,Jean, Mickael,Castellano, Rémy,Josselin, Emmanuelle,Malleter, Marine,Shoji, Kenji F.,Hung, Mac Dinh,Rampanarivo, Hariniaina,Collette, Yves,Van De Weghe, Pierre,Legembre, Patrick
supporting information, p. 6559 - 6573 (2015/09/07)
Constitutive activation of the PI3K/mTOR signaling pathway contributes to carcinogenesis and metastasis in most, if not all, breast cancers. From a chromene backbone reported to inhibit class I PI3K catalytic subunits, several rounds of chemical syntheses led to the generation of a new collection of chromologues that showed enhanced ability to kill PI3K-addicted cancer cells and to inhibit Akt phosphorylation at serine 473, a hallmark of PI3K/mTOR activation. This initial screen uncovered a chromene designated DHM25 that exerted potent antitumor activity against breast tumor cell lines. Strikingly, DHM25 was shown to be a selective and covalent inhibitor of mTOR using biochemical and cellular analyses, modeling, and a large panel of kinase activity assays spanning the human kinome (243 kinases). Finally, in vivo, this novel drug was an efficient inhibitor of growth and metastasis of triple-negative breast cancer cells, paving the way for its clinical application in oncology. (Figure Presented).