I‐Li Chen, Yeh‐long Chen, C. Tzeng
Jul 1, 2002
Citations
0
Influential Citations
30
Citations
Quality indicators
Journal
Helvetica Chimica Acta
Abstract
Some 4-anilinofuro[2,3-b]quinoline derivatives were synthesized from dictamnine, a natural alkaloid, and evaluated for their cytotoxicity in the NCI's full panel of 60 human cancer cell lines derived from nine cancer cell types, including leukemia, non-small-cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, renal cancer, prostate cancer, and breast cancer. 1-[4-(Furo[2,3-b]quinolin-4-ylamino)phenyl]ethanone (5) (mean GI50=0.025 μM), bearing an 4-acetylanilino substituent at C(4) of furo[2,3-b]quinoline, was more active than its 3-acetylanilino counterpart 7 (mean GI50=5.27 μM), and both clinically used anticancer drugs, N-[4-(acridin-9-ylamino)-3-methoxyphenyl]methanesulfonamide (m-AMSA; mean GI50=0.44 μM) and daunomycin (mean GI50=0.044 μM). Compound 5 was capable of inhibiting all types of cancer cells tested with a mean GI50 of less than 0.04 μM in each case except for the non-small-cell lung cancer (average GI50=1.75 μM). Although non-small-cell lung cancer is resistant to compound 5, the sensitivity within this type of cancer cells varies: HOP-62 (GI50<0.01 μM), NCI-H460 (GI50=0.01 μM), and NCI-H522 (GI50<0.01 μM) are very sensitive, while HOP-92 (GI50 = 12.4 μM) is resistant. Among these non-small-cell lung cancers, NCI-H522 was found to be very sensitive to 5, 8a, and 8b with a GI50 values of <0.01, 0.074, and <0.01 μM, respectively.