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Discovery of 3-(benzofuran-2-ylmethyl)-1H-indole derivatives as potential autophagy inducers in cervical cancer cells.

Authors
  • Siddiqui, Shaziyaparveen K1
  • SahayaSheela, Vinodh J2
  • Kolluru, Srinivas3
  • Pandian, Ganesh N4
  • Santhoshkumar, Thankayyan R5
  • Dan, Vipin M6
  • Ramana, Chepuri V7
  • 1 Division of Organic Chemistry, CSIR-National Chemical Laboratory, Dr. Homi Bhabha Road, Pune 411 008, India; Academy of Scientific and Innovative Research (AcSIR), Anusandhan Bhawan, 2 Rafi Marg, New Delhi 110002, India. , (India)
  • 2 Division of Organic Chemistry, CSIR-National Chemical Laboratory, Dr. Homi Bhabha Road, Pune 411 008, India; Institute for Integrated Cell-Material Sciences (WPI-iCeMS), Kyoto University, Kitashirakawa-Oiwakecho, Sakyo-ku, Kyoto 606-8501, Japan. , (India)
  • 3 Division of Organic Chemistry, CSIR-National Chemical Laboratory, Dr. Homi Bhabha Road, Pune 411 008, India; Academy of Scientific and Innovative Research (AcSIR), Anusandhan Bhawan, 2 Rafi Marg, New Delhi 110002, India. Electronic address: [email protected] , (India)
  • 4 Institute for Integrated Cell-Material Sciences (WPI-iCeMS), Kyoto University, Kitashirakawa-Oiwakecho, Sakyo-ku, Kyoto 606-8501, Japan. , (Japan)
  • 5 Rajiv Gandhi Centre for Biotechnology, Thycaud PO, Poojappura, Thiruvananthapuram 695 014, India. , (India)
  • 6 Microbiology Division, Jawaharlal Nehru Tropical Botanic Garden and Research Institute, Palode, Thiruvananthapuram, India. Electronic address: [email protected] , (India)
  • 7 Division of Organic Chemistry, CSIR-National Chemical Laboratory, Dr. Homi Bhabha Road, Pune 411 008, India; Academy of Scientific and Innovative Research (AcSIR), Anusandhan Bhawan, 2 Rafi Marg, New Delhi 110002, India. Electronic address: [email protected] , (India)
Type
Published Article
Journal
Bioorganic & medicinal chemistry letters
Publication Date
Jul 23, 2020
Volume
30
Issue
19
Pages
127431–127431
Identifiers
DOI: 10.1016/j.bmcl.2020.127431
PMID: 32769048
Source
Medline
Keywords
Language
English
License
Unknown

Abstract

In this manuscript we have documented the identification of a novel anticancer scaffold 3-(benzofuran-2-ylmethyl)-1H-indole. This scaffold has been designed by tweaking the known bisindolylmethane scaffold of natural products that display a wide range of biological activities. A series of 24 new conjugates have been synthesized and among them 5 derivatives exhibited IC50 values less than 40 µM against two cervical cancer cell lines SiHa and C33a. Further mechanistic studies of two compounds 3eb and 3ec revealed that the toxicity of these compounds was due to the effective induction of autophagy mediated cell death. The autophagy induction was confirmed by the progressive conversion of LC3I to LC3II and downregulation of p62 in cervical cancer cells. Copyright © 2020 Elsevier Ltd. All rights reserved.

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