Design, synthesis and anticancer activity of novel dihydrobenzofuro[4,5-b][1,8]naphthyridin-6-one derivatives

  • Bioorg Med Chem Lett. 2011 Oct 1;21(19):5730-4. doi: 10.1016/j.bmcl.2011.08.016.
Jin-Ah Kang  1 ,  Zunhua Yang ,  Ji Yeon Lee ,  Umasankal De ,  Tae Hyung Kim ,  Ji Young Park ,  Hye Jin Lee ,  Yun Jung Park ,  Pusoon Chun ,  Hyung Sik Kim ,  Lak Shin Jeong ,  Hyung Ryong Moon
Affiliations
  • 1. College of Pharmacy and Research Institute for Drug Development, Pusan National University, Busan 609-735, Republic of Korea.
PMID: 21885273 DOI: 10.1016/j.bmcl.2011.08.016
Abstract

On the basis of the chemical structures of psorospermin with a xanthone template and acronycine derivatives with an acridone template, rac-1 and rac-2 constructed on an 1,2-dihydrobenzofuro[4,5-b][1,8]naphthyridin-6(11H)-one scaffold were designed and synthesized as potential Anticancer agents. Their Anticancer activities were evaluated against five human Cancer cell lines. Rac-2 showed similar Anticancer activity to doxorubicin and rac-1 exhibited even higher Anticancer activity against LNCaP (IC(50)=0.14 μM), DU145 (IC(50)=0.15 μM), PC3 (IC(50)=0.30 μM) and MCF-7 (IC(50)=0.26 μM) Cancer lines than doxorubicin and rac-2. Also, rac-1 revealed very potent Anticancer activity (IC(50)=0.15 μM) against MCF-7/ADR cell (doxorubicin-resistant breast Cancer cell) lines and induced G2/M phase arrest of the cell cycle in MCF-7/ADR cells.