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

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

Affiliation

  • 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.

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