Synthesis and cytotoxicity of acetyl-4H,9H-naphtho[2,3-b]thiophene-4,9-diones

  • Bioorg Med Chem Lett. 1998 Oct 6;8(19):2763-8. doi: 10.1016/s0960-894x(98)00496-x.
L J Huang  1 ,  S C Kuo ,  C Y Perng ,  Y H Chao ,  T S Wu ,  A T McPhail ,  A Mauger ,  H H Cheng ,  K H Lee
Affiliations
  • 1. Graduate Institute of Pharmaceutical Chemistry, China Medical College, Taichung, Taiwan, Republic of China.
PMID: 9873618 DOI: 10.1016/s0960-894x(98)00496-x
Abstract

Several new acetyl-4H,9H-naphtho[2,3-b]thiophene-4,9-diones were synthesized and evaluated for in vitro cytotoxicity by NCI against seven Cancer cell types. 2,7-Diacetyl naphtho[2,3-b]thiophene-4,9-dione (9) showed significant cytotoxicity against leukemia cells with log GI50 values of -7.61 against SR cells and -7.18 against MOLT-4 cells. 3-Acetyl-naphtho[2,3-b]thiophene-4,9-dione (6) also demonstrated potent cytotoxicity in the latter cell line with log GI50 < -8.