Synthesis and Antitumor Evaluation of Some New Derivatives and Fused Heterocyclic Compounds Derived from Thieno[2,3- b]pyridine: Current Perspective

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Synthesis and Antitumor Evaluation of Some New Derivatives and Fused Heterocyclic Compounds Derived from Thieno[2,3- b]pyridine: Current Perspective

July 29, 2020 Chemistry 0

On the basis of the proven activity of thieno[2,3-b]pyridines as anticancer, we have designed to
synthesize a novel several heterocyclic compounds utilizing thieno[2,3-b]pyridine as a skeleton
through various chemical reactions. The synthesized compounds bear rings that are either directly
attached to the thieno[2,3-b]pyridine as in compounds 4 to 6 and 9 or connected through an amide
bridge as compounds 2, 3ab, 7, and 8. As well as, compounds 10, 12 to 28, 30, 31, and 33 to 36
bear fused rings to the thieno[2,3-b]pyridine back-bone. The newly synthesized compounds were
screened for their antiproliferative activity in vitro against hepatocellular carcinoma (HepG-2) and
breast cancer (MCF-7) compared with the standard drug (doxorubicin). Compounds 3b, 4, 6, 22, and
28 exhibited promising growth inhibitory effect toward both HepG-2 and MCF-7 cell lines with IC50
values ranging from 5.88 to 11.70 μg/ mL and 9.64 to 15.10 μg/mL, respectively.

Author (s) Details

Aisha Y. Hassan
Department of Chemistry, Faculty of Science (Girls), Al‐Azhar University, Cairo, Egypt.

Samiha A. El-Sebaey
Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy (Girls), Al‐Azhar University, Cairo, Egypt.

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