Abstract
The present work reports the synthesis of novel 5-Oxo-5,6,7,8-tetrahydroquinoline and 2,5-dioxo-5,6,7,8-tetrahydroquinoline derivatives containing enaminone system and bearing a sulfonamide moiety. The newly synthesized compounds were designed in compliance with the general pharmacophoric requirements for carbonic anhydrase inhibiting anticancer drugs, as this may play a role in their anticancer activity. Twelve of the newly synthesized compounds were evaluated for their in vitro anticancer activity against human breast cancer cell line (MCF7). Compounds 5c, 7, 10, and 12c showed IC50 values (0.048, 0.040, 0.041, 0.044 μM, respectively) comparable to that of the reference drug doxorubicin (IC50 = 0.04 μM). On the other hand, compounds 12a, 12d, and 16b exhibited better activity than doxorubicin with an IC50 values (0.025, 0.036, 0.015 μM, respectively).
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The authors acknowledge with thanks the NMR unit at King Abdulaziz University for their technical support.
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Ahmed, N.S., Badahdah, K.O. & Qassar, H.M. Novel quinoline bearing sulfonamide derivatives and their cytotoxic activity against MCF7 cell line. Med Chem Res 26, 1201–1212 (2017). https://doi.org/10.1007/s00044-017-1850-9
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DOI: https://doi.org/10.1007/s00044-017-1850-9