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Synthesis and biological evaluation of novel exo-methylene cyclopentanone tetracyclic diterpenoids as antitumor agents

The structure of exo-methylene cyclopentanone, which exists in nature tetracyclic diterpenoids products, has been proved to be an innate group for the treatment of cancer and inflammation. In this letter, four different scaffolds of tetracyclic diterpenoids including the structure exo-methylene cycl... Full description

Journal Title: Bioorganic & Medicinal Chemistry Letters 1 January 2011, Vol.21(1), pp.130-132
Main Author: Li, Jing
Other Authors: Zhang, Dayong , Wu, Xiaoming
Format: Electronic Article Electronic Article
Language: English
Subjects:
ID: ISSN: 0960-894X ; DOI: 10.1016/j.bmcl.2010.11.055
Link: http://dx.doi.org/10.1016/j.bmcl.2010.11.055
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recordid: sciversesciencedirect_elsevierS0960-894X(10)01680-X
title: Synthesis and biological evaluation of novel exo-methylene cyclopentanone tetracyclic diterpenoids as antitumor agents
format: Article
creator:
  • Li, Jing
  • Zhang, Dayong
  • Wu, Xiaoming
subjects:
  • Ent -Kaurane
  • Steviol
  • Isosteviol
  • Exo -Methylene Cyclopentanone
  • Antitumor Agents
ispartof: Bioorganic & Medicinal Chemistry Letters, 1 January 2011, Vol.21(1), pp.130-132
description: The structure of exo-methylene cyclopentanone, which exists in nature tetracyclic diterpenoids products, has been proved to be an innate group for the treatment of cancer and inflammation. In this letter, four different scaffolds of tetracyclic diterpenoids including the structure exo-methylene cyclopentanone were synthesized from steviol and isosteviol and evaluated in vitro for their antitumor activity against three human cancer lines. Compounds 1a, 1b, 2b and 3b showed significant cytotoxicity, particularly, tetracyclic diterpenoids 2b, 3b were identified as the most potent and selective anticancer agents superior to adriamycin with IC50 values of 0.9μM and 1.5μM, against Hep-G2 and MDA-MB-231 cell lines, respectively.
language: eng
source:
identifier: ISSN: 0960-894X ; DOI: 10.1016/j.bmcl.2010.11.055
fulltext: fulltext
issn:
  • 0960894X
  • 0960-894X
url: Link


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titleSynthesis and biological evaluation of novel exo-methylene cyclopentanone tetracyclic diterpenoids as antitumor agents
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identifierISSN: 0960-894X ; DOI: 10.1016/j.bmcl.2010.11.055
subjectEnt -Kaurane ; Steviol ; Isosteviol ; Exo -Methylene Cyclopentanone ; Antitumor Agents
descriptionThe structure of exo-methylene cyclopentanone, which exists in nature tetracyclic diterpenoids products, has been proved to be an innate group for the treatment of cancer and inflammation. In this letter, four different scaffolds of tetracyclic diterpenoids including the structure exo-methylene cyclopentanone were synthesized from steviol and isosteviol and evaluated in vitro for their antitumor activity against three human cancer lines. Compounds 1a, 1b, 2b and 3b showed significant cytotoxicity, particularly, tetracyclic diterpenoids 2b, 3b were identified as the most potent and selective anticancer agents superior to adriamycin with IC50 values of 0.9μM and 1.5μM, against Hep-G2 and MDA-MB-231 cell lines, respectively.
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abstractThe structure of exo-methylene cyclopentanone, which exists in nature tetracyclic diterpenoids products, has been proved to be an innate group for the treatment of cancer and inflammation. In this letter, four different scaffolds of tetracyclic diterpenoids including the structure exo-methylene cyclopentanone were synthesized from steviol and isosteviol and evaluated in vitro for their antitumor activity against three human cancer lines. Compounds 1a, 1b, 2b and 3b showed significant cytotoxicity, particularly, tetracyclic diterpenoids 2b, 3b were identified as the most potent and selective anticancer agents superior to adriamycin with IC50 values of 0.9μM and 1.5μM, against Hep-G2 and MDA-MB-231 cell lines, respectively.
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date2011-01-01