2. Academic Validation
  3. Design, synthesis and biological evaluation of 2-(3,4-dimethoxyphenyl)-6 (1,2,3,6-tetrahydropyridin-4-yl)imidazo[1,2-a]pyridine analogues as antiproliferative agents

Design, synthesis and biological evaluation of 2-(3,4-dimethoxyphenyl)-6 (1,2,3,6-tetrahydropyridin-4-yl)imidazo[1,2-a]pyridine analogues as antiproliferative agents

  • Bioorg Med Chem Lett. 2019 Sep 15;29(18):2551-2558. doi: 10.1016/j.bmcl.2019.08.013.
Surendar Chitti 1,  SrinivasaRao Singireddi 1,  Pochana Santosh Kumar Reddy 1,  Prakruti Trivedi 2,  Yamini Bobde 2,  Chandan Kumar 3,  Krishnan Rangan 1,  Balaram Ghosh 4,  Kondapalli Venkata Gowri Chandra Sekhar 5
Affiliations

Affiliations

  • 1 Department of Chemistry, Birla Institute of Technology and Science, Pilani, Hyderabad Campus, Jawahar Nagar, Hyderabad 500 078, Telangana, India.
  • 2 Department of Pharmacy, Birla Institute of Technology and Science, Pilani, Hyderabad Campus, Jawahar Nagar, Hyderabad 500 078, Telangana, India.
  • 3 Department of Bioinformatics, Pondicherry University, Pondicherry 605014, India.
  • 4 Department of Pharmacy, Birla Institute of Technology and Science, Pilani, Hyderabad Campus, Jawahar Nagar, Hyderabad 500 078, Telangana, India. Electronic address: balaram@hyderabad.bits-pilani.ac.in.
  • 5 Department of Chemistry, Birla Institute of Technology and Science, Pilani, Hyderabad Campus, Jawahar Nagar, Hyderabad 500 078, Telangana, India. Electronic address: kvgc@hyderabad.bits-pilani.ac.in.
PMID: 31420269 DOI: 10.1016/j.bmcl.2019.08.013
Abstract

Two series of forty five novel 2-(3,4-dimethoxyphenyl)-6-(1,2,3,6-tetrahydropyridin-4-yl) imidazo[1,2-a]pyridine analogues (IPA 1-22, IPS 1-22 and IP-NH) have been designed, synthesized and structures confirmed by 1H NMR, 13C NMR, mass spectrometry. Furthermore, single crystal was developed for IPS-13. All the final derived conjugates were evaluated for their in vitro antiproliferative activity against a panel of diverse Cancer cell lines viz., A549 (lung Cancer), HeLa (cervical Cancer), B16F10 (melanoma) and found to show potent Anticancer activity on the tested cell lines. Many of them showed the IC50 values in the range 2.0-20.0 µM. The most active compounds (IPA 5,6,8,9,12,16,17,19 and IPS 7,8,9,22) from IPA and IPS series were screened to determine their cytotoxicity on HEK-293 (human embryonic kidney) normal cell line and were found to be nontoxic to normal human cells. The molecular interactions of the derivatised conjugates were also supported by molecular docking simulations. These derivatives may serve as lead structures for development of novel potential Anticancer drug candidates.

Keywords

Anticancer; Apoptosis; Cytotoxicity; Imidazo[1,2-a]pyridine; Molecular docking.

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