One-pot synthesis and evaluation of novel 3-aryl-6-ethoxycarbonyl-4-hydroxy-2H-pyran-2-one as a potent cytotoxic agentElectronic supplementary information (ESI) available. See DOI: 10.1039/c4ra10015h

A series of new open chain analogs of Phelligridin J were synthesized by a clean one-pot approach. These compounds were evaluated for their in vitro cytotoxicity against normal and breast cancer cell lines. All the compounds exhibited potent cytotoxic activity in the lower micro molar range. Compoun...

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Main Authors Dhage, Ganesh Raosaheb, Thopate, Shankar Ramchandra, Ramteke, Shefali Nishikant, Kulkarni, Prasad Padmakar
Format Journal Article
LanguageEnglish
Published 04.11.2014
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Abstract A series of new open chain analogs of Phelligridin J were synthesized by a clean one-pot approach. These compounds were evaluated for their in vitro cytotoxicity against normal and breast cancer cell lines. All the compounds exhibited potent cytotoxic activity in the lower micro molar range. Compound 5o exhibited the maximum cytotoxic activity with IC 50 values of 12.49 and 13.76 μM, whereas compound 5a showed two-fold selectivity viz. IC 50 values of 21.80 to 43.40 μM against breast cancer (MCF7) and normal fibroblast (NIH3T3) cell lines, respectively. A series of new open chain analogs of Phelligridin J were synthesized and these compounds were found to be highly potent cytotoxic agents.
AbstractList A series of new open chain analogs of Phelligridin J were synthesized by a clean one-pot approach. These compounds were evaluated for their in vitro cytotoxicity against normal and breast cancer cell lines. All the compounds exhibited potent cytotoxic activity in the lower micro molar range. Compound 5o exhibited the maximum cytotoxic activity with IC 50 values of 12.49 and 13.76 μM, whereas compound 5a showed two-fold selectivity viz. IC 50 values of 21.80 to 43.40 μM against breast cancer (MCF7) and normal fibroblast (NIH3T3) cell lines, respectively. A series of new open chain analogs of Phelligridin J were synthesized and these compounds were found to be highly potent cytotoxic agents.
Author Dhage, Ganesh Raosaheb
Ramteke, Shefali Nishikant
Thopate, Shankar Ramchandra
Kulkarni, Prasad Padmakar
AuthorAffiliation Department of Chemistry
Prof. John Barnabas Post Graduate School of Biological Studies
Ahmednagar College
Biometry and Nutrition Group
Agharkar Research Institute
AuthorAffiliation_xml – name: Agharkar Research Institute
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  givenname: Ganesh Raosaheb
  surname: Dhage
  fullname: Dhage, Ganesh Raosaheb
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  givenname: Shankar Ramchandra
  surname: Thopate
  fullname: Thopate, Shankar Ramchandra
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  givenname: Shefali Nishikant
  surname: Ramteke
  fullname: Ramteke, Shefali Nishikant
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  givenname: Prasad Padmakar
  surname: Kulkarni
  fullname: Kulkarni, Prasad Padmakar
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Title One-pot synthesis and evaluation of novel 3-aryl-6-ethoxycarbonyl-4-hydroxy-2H-pyran-2-one as a potent cytotoxic agentElectronic supplementary information (ESI) available. See DOI: 10.1039/c4ra10015h
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