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      Permanent link:
      https://www.ias.ac.in/article/fulltext/jcsc/128/08/1245-1263

    • Keywords

       

      Phthalimides; apoptosis; molecular docking; aryl piperazine; cancer cells.

    • Abstract

       

      Understanding of apoptosis or programmed cell death has provided the basis for novel therapeutics that has resulted in rationally designed anticancer strategies. Recently, inducers of apoptosis have been used in cancer therapy. In this work, we describe the role of chiral phthalimides functionalized with piperazines aspotential apoptotic inducers. The listed twenty phthalimides were assessed for their in vitro apoptotic activity against testicular germ cells. All phthalimides showed a significant apoptotic response (∼39 to ∼68%). TUNEL assay and acridine orange fluorescence staining were carried out to investigate the molecular mechanismsresponsible for the cell death. Phthalimides exhibited substantial apoptotic induction following the intrinsic pathway mechanism. Studies advocated that the apoptotic induction was mediated through caspase-9, caspase-3, JNK MAP kinase and tumor suppressor p53, which was accompanied by DNA fragmentation and nuclearcondensation. Besides, the best five phthalimides regarding apoptotic action were evaluated for in vitro cytotoxic effects against CAL-72 and MCF-7 cancer cell lines. Compounds showed efficient killing of cancer cells. This discovery of functionalized phthalimides as apoptotic inducers would be highly valuable in understanding the mechanism of apoptosis at the molecular level and opens up new possibilities for therapeutic strategies.

    • Author Affiliations

       

      ANIL K SINGH1 JITENDER K BHARDWAJ2 ANA OLIVAL3 YOGESH KUMAR1 AVIJIT PODDER4 ANKUR MAHESHWARI5 RENUKA AGRAWAL6 N LATHA4 BRAJENDRA K SINGH1 HELENA TOMÁS3 JOÃO RODRIGUES3 RAM KISHAN7 B RUPINI8 BRIJESH RATHI9

      1. Bioorganic Research Laboratory, Department of Chemistry, University of Delhi, Delhi 110 007, India
      2. Reproductive Physiology Laboratory, Department of Zoology, Kurukshetra University, Kurukshetra, Haryana 136 119, India
      3. CQM-Centro de Química da Madeira, MMRG, Universidade da Madeira, Campus da Penteada, 9020-105 Funchal, Portugal
      4. Bioinformatics Infrastructure Facility, Sri Venkateswara College, University of Delhi, Dhaula Kuan, New Delhi 110 021, India
      5. Department of Zoology, Zakir Husain Delhi College, University of Delhi, J L N Marg, New Delhi 110 002, India
      6. Department of Botany, Miranda House,University of Delhi, Delhi 110 007, India
      7. Department of Chemistry, University of Delhi, Delhi 110 007, India
      8. School of Agriculture, Environmental Studies, Indira Gandhi National Open University, New Delhi 110 068, India
      9. Department of Chemistry, Hansraj College, University of Delhi, Malka Ganj, Delhi 110 007, India

    • Dates

       
      Published
      1 August 2016
      Manuscript received
      31 March 2016
      Manuscript revised
      25 May 2016
      Accepted
      30 May 2016

    • Supplementary Material

       

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