1296223-77-2

Upstream product

• 180695-80-1 tert-butyl 4-azidopiperidine-1-carboxylate 
• 403-33-8 methyl 4-flurobenzoate 
• 73874-95-0 (piperidin-4-yl)carbamic acid tert-butyl ester 
• 1452394-22-7 methyl 4-(4-azidopiperidin-1-yl)benzoate 

Downstream Products

• 1452395-03-7 C₁₉H₂₁FN₂O₄S 
• 1452395-02-6 C₂₀H₂₁N₃O₄S 
• 1452395-01-5 C₁₈H₂₃N₃O₄S₂ 
• 1452395-00-4 C₂₀H₂₄N₂O₄S 
• 1452394-99-8 C₁₉H₂₂N₂O₄S 
• 1452394-98-7 C₂₀H₂₂ClN₃O₃ 
• 1452394-97-6 C₂₂H₂₇N₃O₃ 
• 1452394-96-5 C₂₀H₂₉N₃O₃ 
• 1452394-95-4 C₁₈H₂₁N₃O₃S 
• 1452394-94-3 C₁₇H₂₅N₃O₃ 
• 1452394-93-2 C₁₉H₂₈N₂O₃ 
• 1452394-92-1 C₂₂H₃₀N₄O₃ 
• 1452394-91-0 C₂₀H₂₆N₂O₃ 
• 1452394-90-9 C₂₂H₂₂N₂O₃S 

Relevant academic research and scientific papers

Design and Synthesis of Novel Epigenetic Inhibitors Targeting Histone Deacetylases, DNA Methyltransferase 1, and Lysine Methyltransferase G9a with in Vivo Efficacy in Multiple Myeloma

Concomitant inhibition of key epigenetic pathways involved in silencing tumor suppressor genes has been recognized as a promising strategy for cancer therapy. Herein, we report a first-in-class series of quinoline-based analogues that simultaneously inhibit histone deacetylases (from a low nanomolar range) and DNA methyltransferase-1 (from a mid-nanomolar range, IC50 1 log unit), and a suitable pharmacokinetic profile. In vivo, 12a achieved significant antitumor efficacy in a xenograft mouse model of human multiple myeloma.

NOVEL COMPOUNDS FOR USE IN CANCER

It relates to the compounds of formula (I), or their pharmaceutically or veterinary acceptable salts, or their stereoisomers or mixtures of stereoisomers, wherein X, L,R1, R 2, and R 3 are as defined herein, which are cancer cell differentiation inducing agents. It also relates to pharmaceutical or veterinary compositions containing them, and to their use in medicine, in particular in the treatment and/or prevention of cancer, in particular by cell differentiation therapy.

Disubstituted 1-aryl-4-aminopiperidine library synthesis using computational drug design and high-throughput batch and flow technologies

A platform that incorporates computational library design, parallel solution-phase synthesis, continuous flow hydrogenation, and automated high throughput purification and reformatting technologies was applied to the production of a 120-member library of 1-aryl-4-aminopiperidine analogues for drug discovery screening. The application described herein demonstrates the advantages of computational library design coupled with a flexible, modular approach to library synthesis. The enabling technologies described can be readily adopted by the traditional medicinal chemist without extensive training and lengthy process development times.