1613475-26-5

Upstream product

• 157160-99-1 4-Chloro-3-nitrobenzoic acid tert-butyl ester 
• 109-01-3 1-methyl-piperazine 
• 1613475-23-2 tert-butyl 3-nitro-4-(4-methylpiperazin-1-yl)benzoate 
• 1613475-24-3 tert-butyl 3-amino-4-(4-methylpiperazin-1-yl)benzoate 
• 1613475-25-4 tert-butyl 3-(benzyloxycarbonylamino)-4-(4-methylpiperazin-1-yl)benzoate 

Downstream Products

• 1613475-22-1 benzyl N-[5-carbamoyl-2-(4-methylpiperazin-1-yl)phenyl]carbamate 

Relevant academic research and scientific papers

Discovery of a Novel Inhibitor of Histone Lysine-Specific Demethylase 1A (KDM1A/LSD1) as Orally Active Antitumor Agent

We report the stereoselective synthesis and biological activity of a novel series of tranylcypromine (TCPA) derivatives (14a-k, 15, 16), potent inhibitors of KDM1A. The new compounds strongly inhibit the clonogenic potential of acute leukemia cell lines. In particular three molecules (14d, 14e, and 14g) showing selectivity versus MAO A and remarkably inhibiting colony formation in THP-1 human leukemia cells, were assessed in mouse for their preliminary pharmacokinetic. 14d and 14e were further tested in vivo in a murine acute promyelocytic leukemia model, resulting 14d the most effective. Its two enantiomers were synthesized: the (1S,2R) enantiomer 15 showed higher activity than its (1R,2S) analogue 16, in both biochemical and cellular assays. Compound 15 exhibited in vivo efficacy after oral administration, determining a 62% increased survival in mouse leukemia model with evidence of KDM1A inhibition. The biological profile of compound 15 supports its further investigation as a cancer therapeutic.

Cyclopropylamine derivatives as histone demethylase inhibitors

The present invention relates to cyclopropyl derivatives of general formula (I), wherein R1, and R2 are as defined in the specification. The present application also relates to pharmaceutical compositions containing such compounds an

CYCLOPROPYLAMINE DERIVATIVES USEFUL AS INHIBITORS OF HISTONE DEMETHYLASES KDM1A

(I) The present invention relates to cyclopropyl derivatives of general formula (I), wherein A, R1, and R2 are as defined in the specification. The present application also relates to pharmaceutical compositions containing such compounds and to their use in therapy.