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STUDY ON MARINE NATURAL PRODUCTS: BRYOSTATIN AND ITS ANALOGUE AS ANTICANCER AGENT

  • Unique Paper ID: 165856
  • Volume: 11
  • Issue: 1
  • PageNo: 2540-2544
  • Abstract:
  • Bryostatins are a unique family of novel chemotherapeutics of marine origin isolated from Bugula neritina. Although the biochemical basis of their therapeutic activity is unknown, these macrolactones have a high affinity for protein kinase C (PKC) isozymes, compete for the phorbol-ester binding site on PKC, and stimulate kinase activity in vitro and in vivo. Computer modeling has generated a new class of bryostatin analogs that retain the putative recognition domain of bryostatins but are simplified by removing and modifying the C1–C14 middle domain. The solution structures of the two synthetic analogs were determined by NMR spectroscopy and found to be very similar to the previously reported structures of bryostatins 1 and 10. Furthermore, these structures seem to indicate that the stereochemistry of the C3 hydroxyl group plays an important role in the shape of the macrolactone. All analogs bound strongly to a mixture of PKC isozymes, and several showed significant in vitro growth inhibitory activity against human cancer cell lines. Collectively, this work provides important steps toward the development and understanding of simplified, synthetically accessible analogs of bryostatins as potential chemotherapeutic agents.
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Cite This Article

  • ISSN: 2349-6002
  • Volume: 11
  • Issue: 1
  • PageNo: 2540-2544

STUDY ON MARINE NATURAL PRODUCTS: BRYOSTATIN AND ITS ANALOGUE AS ANTICANCER AGENT

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