title: Synthesis of 86 species of 1,5-diaryl-3-oxo-1,4-pentadienes analogs of curcumin can yield a good lead in vivo.
abstract: BACKGROUND
  Curcumin is known to possess many anti-tumor properties such as inhibition of tumor growth and induction of apotosis. However, limited bioavailability of curcumin prevents its clinical application. A synthesized curcumin analog, 1,5-diaryl-3-oxo-1,4-pentadiene such as GO-Y030, has the improved anti-tumor potential in vitro as well as in mouse model of colorectal carcinogenesis.
  
  
  RESULTS
  These compounds were divided into two groups; one is the higher anti-proliferative group, in which 79.7% of 1,5-diaryl-3-oxo-1,4-pentadienes were clustered. One of the 1,5-diaryl-3-oxo-1,4-pentadiene analogs, GO-Y078 has the most enhanced growth inhibition, and its solubility was improved, compared with curcumin. GO-Y078 inhibits NF-κB transactivation, as well as expression of TP53 and DR5 more effectively than curcumin. In a mouse model, GO-Y078 presented 1.4 fold more survival elongation that was not achieved by curcumin and GO-Y030.
  
  
  CONCLUSIONS
  The 1,5-diaryl-3-oxo-1,4-pentadiene analogs can yield good lead compounds for cancer chemotherapy, to overcome low bioavailability of curcumin.
authors: Dept. Clinical Oncology, Institute of Development, Aging, and Cancer, Tohoku University, Seiryo-cho 4-1, Aoba-ku, Sendai, Japan.
authors: Chieko
authors: C
authors: Kudo
authors: Hiroyuki
authors: H
authors: Yamakoshi
authors: Atsuko
authors: A
authors: Sato
authors: Hiroshi
authors: H
authors: Nanjo
authors: Hisatsugu
authors: H
authors: Ohori
authors: Chikashi
authors: C
authors: Ishioka
authors: Yoshiharu
authors: Y
authors: Iwabuchi
authors: Hiroyuki
authors: H
authors: Shibata
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