372109-21-2Relevant academic research and scientific papers
An oxidative amidation and heterocyclization approach for the synthesis of β-carbolines and dihydroeudistomin y
Meruva, Suresh Babu,Raghunadh, Akula,Kamaraju, Raghavendra Rao,Kumar, U.K. Syam,Dubey
, p. 471 - 480 (2014/03/21)
A novel synthetic methodology has been developed for the synthesis of dihydro-β-carboline derivatives employing oxidative amidation-Bischler- Napieralski reaction conditions using tryptamine and 2,2-dibromo-1- phenylethanone as key starting materials. A number of dihydro-β-carboline derivatives have been synthesized in moderate to good yields using this methodology. Attempts were made towards the conversion of these dihydro-β-carbolines to naturally occurring eudistomin alkaloids.
Design, synthesis and biological evaluation of new tryptamine and tetrahydro-β-carboline-based selective inhibitors of CDK4
Jenkins, Paul R.,Wilson, James,Emmerson, Daniel,Garcia, Marcos D.,Smith, Matthew R.,Gray, Stephen J.,Britton, Robert G.,Mahale, Sachin,Chaudhuri, Bhabatosh
, p. 7728 - 7739 (2008/12/23)
We present the design, synthesis and biological activity of a library of substituted (biphenylcarbonyl)-tryptamine and (biphenylcarbonyl)-tetrahydro-β-carboline compounds related to the natural product fascaplysin, as novel inhibitors of CDK4/cyclin D1. We show all these molecules, prepared using the Suzuki-Miyaura reaction, being selective inhibitors of CDK4 over CDK2. The most active compounds have a CDK4 IC50 in the range 9-11 μM, three of them containing the para-biphenyl plus para-substituents supporting the existence of a π-stacking pocket within the active site of CDK4.
