- INHIBITORS OF LYSINE SPECIFIC DEMETHYLASE-1
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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.
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- Scalable synthesis of functionalised 2-pyridones via [4+2] cycloaddition reactions of 2-pyrazinones and alkynylboronates
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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.
- Harker, Wesley R.R.,Delaney, Patrick M.,Simms, Michael,Tozer, Matthew J.,Harrity, Joseph P.A.
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p. 1546 - 1552
(2013/02/25)
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- SUBSTITUTED OXAZOLIDINONES AND THEIR USE
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The invention relates to novel substituted oxazolidinones, to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases, and to the use thereof for producing medicaments for treatment and/or prophylaxis of diseases
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Page/Page column 46
(2010/12/29)
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- Intramolecular Diels-Alder synthesis of 7-aza-α-carboline compounds
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An efficient, versatile, and scalable route for the synthesis of 7-aza-α-carboline compounds is described. The tricyclic system has been prepared from modified pyrazinones using a key intramolecular [4+2] Diels-Alder transformation.
- Wallace, Michael B.,Scorah, Nicholas,Vu, Phong H.,Brown, Jason W.,Stafford, Jeffrey A.,Dong, Qing
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supporting information; experimental part
p. 1739 - 1741
(2010/05/18)
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- Synthesis and fungicidal activity of 3,5-dichloropyrazin-2(1H)-one derivatives
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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
- 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
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supporting information; experimental part
p. 4064 - 4066
(2010/03/25)
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- Design and synthesis of novel type VI-like β-turn mimetics. Diversity at the i+1 and the i+2 position
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In this paper, a synthetic approach for functionalised 5-aminopiperidinone- 2-carboxylate (APC) systems as non-pro cis-peptide bond containing external β-turn mimics is presented. The scope and limitations of the synthetic method are discussed and the pot
- De Borggraeve, Wim M.,Verbist, Bie M.P.,Rombouts, Frederik J.R.,Pawar, Vijaykumar G.,Smets, Wim J.,Kamoune, Laila,Alen, Jo,Van Der Eycken, Erik V.,Compernolle, Frans,Hoornaert, Georges J.
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p. 11597 - 11612
(2007/10/03)
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- A new synthesis of substituted 2(1H)-pyrazinones
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The hydrohalides of 2-sec-aminoalkanenitriles on treatment with oxalyl halides in o-dichlorobenzene at 80-100° give 3,5-dihalo-2(1H)-pyrazinones, of which the 3-halo substituent is easily replaced by nucleophiles. A reaction mechanism for the pyrazinone s
- Vekemans,Pollers Wieers,Hoornaert
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p. 919 - 923
(2007/10/02)
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