2. Academic Validation
  3. Design and synthesis of novel phenyl -1, 4-beta-carboline-hybrid molecules as potential anticancer agents

Design and synthesis of novel phenyl -1, 4-beta-carboline-hybrid molecules as potential anticancer agents

  • Eur J Med Chem. 2017 Mar 10:128:123-139. doi: 10.1016/j.ejmech.2017.01.014.
S Samundeeswari 1,  Bahubali Chougala 1,  Megharaja Holiyachi 1,  Lokesh Shastri 2,  Manohar Kulkarni 1,  Suneel Dodamani 3,  Sunil Jalalpur 3,  Shrinivas Joshi 4,  Sheshagiri Dixit 4,  Vinay Sunagar 5,  Ravindra Hunnur 6
Affiliations

Affiliations

  • 1 Department of Chemistry, Karnatak University, Dharwad, 580 003, Karnataka, India.
  • 2 Department of Chemistry, Karnatak University, Dharwad, 580 003, Karnataka, India. Electronic address: drlashastri@kud.ac.in.
  • 3 Dr. Prabhakar Kore Basic Science Research Center, KLE University, Belgaum 590010, Karnataka, India.
  • 4 Novel Drug Design and Discovery Laboratory, Department of Pharmaceutical Chemistry, S.E.T's College of Pharmacy, Sangolli Rayanna Nagar, Dharwad, 580002, Karnataka, India.
  • 5 Department of Chemistry, G.S.S. College, Belagavi, Karnataka, India.
  • 6 Research Center, Aurobindo Pharma Ltd, Hyderabad, A.P, India.
PMID: 28171832 DOI: 10.1016/j.ejmech.2017.01.014
Abstract

A series of beta-carbolines with Other heterocycles linked by phenyl ring has been designed and synthesized. The key intermediates 3 and 5 were synthesized by condensing tryptamine and teraldehyde via Pictet- Spengler method. All the newly synthesized compounds were tested for their Anticancer activity against sixty human cell lines at NCI. The five dose results of compounds 3 and 7a showed enhancement of Anticancer activity (GI50 values range from 1.00 to 7.10 μM) against all the cell lines in comparison with some of earlier molecules. In addition to this protein binding and CT-DNA intercalation studies showed molecules are highly potential. The molecular docking studies, which support the multiple mode of interaction with DNA, moreover the synthesized compounds 3 and 7a are more potential and possess drug -like nature.

Keywords

Beta-carboline-hybrid; Molecular docking; Pictet- Spengler; Protein binding; Tryptamine.

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