63086-36-2Relevant academic research and scientific papers
INHIBITORS OF LYSINE SPECIFIC DEMETHYLASE-1
CHEN Young K.,KANOUNI Toufike,STAFFORD Jeffrey Alan,VEAL James Marvin
Paragraph 00105, (2016/04/26)
The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
Scalable synthesis of functionalised 2-pyridones via [4+2] cycloaddition reactions of 2-pyrazinones and alkynylboronates
Harker, Wesley R.R.,Delaney, Patrick M.,Simms, Michael,Tozer, Matthew J.,Harrity, Joseph P.A.
, p. 1546 - 1552 (2013/02/25)
The multigram synthesis of N-protected 2-pyridone boronic acid derivatives via a [4+2] cycloaddition of alkynylboronates with 2-pyrazinones is presented. The reactions are highly chemoselective, and generally highly regioselective although trimethylsilyl-substituted alkynylboronates have proven to be an exception. Nonetheless, in this latter case, separation of regioisomers was successfully accomplished via high performance counter-current chromatography allowing isolation of analytically pure 2-pyridones. Further derivatisations of trimethylsilyl-substituted 2-pyridone boronates were performed providing access to a selection of functionalised scaffolds.
Synthesis and fungicidal activity of 3,5-dichloropyrazin-2(1H)-one derivatives
Francois, Isabelle E.J.A.,Cammue, Bruno P.A.,Bresseleers, Sara,Fleuren, Hein,Hoornaert, Georges,Mehta, Vaibhav P.,Modha, Sachin G.,Van der Eycken, Erik V.,Thevissen, Karin
supporting information; experimental part, p. 4064 - 4066 (2010/03/25)
We synthesized a family of 3,5-dichloropyrazin-2(1H)-one derivatives and assessed their in vitro fungicidal activity against Candida albicans. Compounds 11 and 20 were most active against C. albicans and induced accumulation of reactive oxygen species in
A Model for Metabolic Activation of Dialkylnitrosoamines. Oxidative Dealkylation 2-(N-Nitrosoalkylamino)acetonitriles by a Flavin Mimic in Aqueous Solution
Yano, Yumihiko,Yokoyama, Takeshi,Ikuta, Masato,Yoshida, Kitaro
, p. 5606 - 5610 (2007/10/02)
It is found for the first time that a flavin mimic, benzodipteridine (BDP), reacts with 2-(N-nitrosoalkylamino)acetonitriles via oxidative dealkylation to yield the corresponding alcohols (ROH) and the 2-e-reduced BDP in aqueous acetonitrile.Kinetic studies reveal that the rates are first order with respect to and ->, respectively.Kinetic isotope effects (kH/kD) for RN(NO)CD2CN (R = Me, n-Bu, Ph, and PhCH2) are found to be 2.2-4.2, indicating that deprotonation is involved in the rate-determining step.The mechanism of the oxidative dealkylation of the nitrosoamines by the flavin mimic is discussed.
