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An Efficient Combinatorial Synthesis of Allocolchicine Analogues via a Triple Cascade Reaction and their Evaluation as Inhibitors of Insulin Aggregation

Authors

  • Subhendu Bhowmik,

    1. Medicinal & Process Chemistry Division, CSIR–Central Drug Research Institute, BS 10/1, Sector 10, Jankipuram Extension, Sitapur Rd, Lucknow 226031 (India)
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  • Shruti Khanna,

    1. Department of Chemistry, Indian Institute of Technology Kanpur, Kanpur 208016 (India)
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  • Dr. Kumkum Srivastava,

    1. Parasitology Division, CSIR–Central Drug Research Institute, Lucknow 226031 (India)
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  • Mohammad Hasanain,

    1. Drug Target Discovery & Development Division, CSIR–Central Drug Research Institute, Lucknow 226031 (India)
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  • Dr. Jayanta Sarkar,

    1. Drug Target Discovery & Development Division, CSIR–Central Drug Research Institute, Lucknow 226031 (India)
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  • Prof. Sandeep Verma,

    Corresponding author
    1. Department of Chemistry, Indian Institute of Technology Kanpur, Kanpur 208016 (India)
    • Sandeep Verma, Department of Chemistry, Indian Institute of Technology Kanpur, Kanpur 208016 (India)

      Sanjay Batra, Medicinal & Process Chemistry Division, CSIR–Central Drug Research Institute, BS 10/1, Sector 10, Jankipuram Extension, Sitapur Rd, Lucknow 226031 (India)

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  • Dr. Sanjay Batra

    Corresponding author
    1. Medicinal & Process Chemistry Division, CSIR–Central Drug Research Institute, BS 10/1, Sector 10, Jankipuram Extension, Sitapur Rd, Lucknow 226031 (India)
    2. Academy of Scientific & Innovative Research (AcSIR), 2 Rafi Marg, New Delhi 110001 (India)
    • Sandeep Verma, Department of Chemistry, Indian Institute of Technology Kanpur, Kanpur 208016 (India)

      Sanjay Batra, Medicinal & Process Chemistry Division, CSIR–Central Drug Research Institute, BS 10/1, Sector 10, Jankipuram Extension, Sitapur Rd, Lucknow 226031 (India)

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Abstract

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A controlled cascade: A divergent, diastereoselective and efficient one-pot synthesis of allocolchicinoids via a cascade Suzuki–Michael addition–Carbocyclization sequence is described. The utility of the compounds as possible inhibitors of insulin aggregation is also presented.

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