Synthesis of 1-Indolyl-3,5,8-Substituted γ-Carbolines: One Pot Metal-Solvent Free Protocol and Biological Evaluation

  1. Premansh DudheORCID Logo,
  2. Mena Asha Krishnan,
  3. Kratika Yadav,
  4. Diptendu Roy,
  5. Krishnan Venkatasubbaiah,
  6. Biswarup Pathak and
  7. Venkatesh ChelvamORCID Logo

Submitting author affiliation: Indian Institute of Technology Indore, Indore, India

Beilstein Arch. 2020, 2020131.

Published 19 Nov 2020

  • Preprint


1,5-Disubstituted indole-2-carboxaldehyde derivatives (1ah) and glycine alkyl esters (2ac) are shown to undergo a novel cascade imination-heterocylisation in the presence of organic base DIPEA to provide 1-indolyl 3,5,8-substituted g-carbolines (3aaea) in good yields. The g-carbolines are fluorescent and exhibit anticancer activities against cervical, lung, breast, skin and kidney cancers.

Keywords: γ-Carboline; cascade reaction; cytotoxicity; cell uptake; density functional theory; fluorescence.

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Dudhe, P.; Krishnan, M. A.; Yadav, K.; Roy, D.; Venkatasubbaiah, K.; Pathak, B.; Chelvam, V. Beilstein Arch. 2020, 2020131. doi:10.3762/bxiv.2020.131.v1

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