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Design, synthesis and biological evaluation of novel thiophene and theinopyrimidine derivatives as anticancer agents

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Abstract

Some novel thiophene and theinopyrimidine derivatives have been synthesized. Their structures were confirmed by elemental analyses, infrared, 1H NMR, 13C NMR and mass spectral data. All the target compounds were screened against liver adenocarcinoma (HepG2) cell line. Compounds 9c, 9b, 10b, and 7c in a sequent were the most potent compounds between all the test compounds with IC50 values [0.01063, 0.01158, 0.01729, 0.01957 µM], respectively. Compounds 13b, 7b, 5d, 9a, 8a, and 11b showed higher activity with IC50 values ranged from 0.02231 to 0.03673 µM when compared with 5-flurouracil (A) as a reference drug (IC50 = 0.0384 µM).

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Author contributions

M.B.L. proposed the subject and carried out the synthesis, purification and characterization of the compounds. P.F.L. conceived the study and participated in its design, experiments, results, discussion, and coordination.

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Authors and Affiliations

  1. Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Beni-Suef University, Beni Suef, 62514, Egypt

    Madlen B. Labib & Phoebe F. Lamie

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  1. Madlen B. Labib
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  2. Phoebe F. Lamie
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Correspondence to Phoebe F. Lamie.

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Labib, M.B., Lamie, P.F. Design, synthesis and biological evaluation of novel thiophene and theinopyrimidine derivatives as anticancer agents. Med Chem Res 25, 2607–2618 (2016). https://doi.org/10.1007/s00044-016-1703-y

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  • DOI: https://doi.org/10.1007/s00044-016-1703-y

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