Synthetic approaches to indolo[6,7-a]pyrrolo[3,4-c]carbazoles: potent cyclin D1/CDK4 inhibitors |
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Authors: | Faul Margaret M Engler Thomas A Sullivan Kevin A Grutsch John L Clayton Marcella T Martinelli Michael J Pawlak Joseph M LeTourneau Michael Coffey D Scott Pedersen Steven W Kolis Stanley P Furness Kelly Malhotra Sushant Al-awar Rima S Ray James E |
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Institution: | Global Chemical Process Research and Development, Indianapolis, Indiana 46285, USA. mfaul@amgen.com |
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Abstract: | Synthesis of indolo6,7-a]pyrrolo3,4-c]carbazoles 1, a new class of cyclin D1/CDK4 inhibitors, by oxidation of the corresponding aryl indolylmaleimides 2, will be described. Two approaches to the synthesis of 2 were identified that required new methods for the synthesis of 7-substituted indole acetamides 3 and N-methyl (indol-7-yl)oxoacetates 6. The chemistry developed enabled introduction of functionality (-OR, NR(2)) at C(12) and N(13) facilitating structure-activity relationship (SAR) evaluation of this indolocarbazole platform. |
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