Synthesis of yashabushidiol and its analogues and their cytotoxic activity against cancer cell lines

  • Bioorg Med Chem Lett. 2009 Jun 1;19(11):3125-7. doi: 10.1016/j.bmcl.2009.03.061.
M Narasimhulu  1 ,  T Srikanth Reddy ,  K Chinni Mahesh ,  A Sai Krishna ,  J Venkateswara Rao ,  Y Venkateswarlu
Affiliations
  • 1. Organic Division-I, Natural Products Laboratory, Indian Institute of Chemical Technology, Hyderabad, India.
PMID: 19410455 DOI: 10.1016/j.bmcl.2009.03.061
Abstract

A total synthesis of yashabushidiol (1a), a linear diarylheptanoid having 1,3- diol system and its analogues has been achieved by alkynylation of 3-hydroxy-5-phenyl pentanal with substituted phenyl acetylenes. All the compounds have shown significant anti-proliferative activity on human leukemia (THP-1, U-937) and melanoma (A-375) cell lines. Compounds 2a and 2b were found to be most potent with an IC(50) of 12.82 microg/mL and 12.62 microg/mL, respectively, on THP-1 leukemia cell line.