Synthesis and Antitumor Evaluation of Some New Derivatives and Fused Heterocyclic Compounds Derived from Thieno[2,3- b]pyridine: Current Perspective | Chapter 2 | Current Research and Development in Chemistry Vol. 3

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, 3a-b, 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.

View Book :- http://bp.bookpi.org/index.php/bpi/catalog/book/217

Synthesis and Antitumor Evaluation of Some New Derivatives and Fused Heterocyclic Compounds Derived from Thieno[2,3‐ b]pyridine: Recent Perspective | Chapter 1 | Current Research and Development in Chemistry Vol. 3

As a continuation of our research on developing anticancer agents and based on the proven
proprieties of thieno[2,3‐b]pyridines as anticancer, we have designed to synthesize novel thieno[2,3‐
b]pyridine derivatives that incorporate different biologically active heterocycles through various
chemical reactions. All of the newly obtained compounds, compared with the standard anticancer
drug (doxorubicin), were screened in vitro for their antitumor activity against hepatocellular carcinoma
(HepG‐2) and human breast cancer (MCF‐7) cell lines. The results revealed that compounds 3, 7, 12,
and 19 were found to be the most potent against both HepG‐2 and MCF‐7 cell lines exhibiting IC50
values ranging from 3.67 to 11.50 and 5.13 to 11.80 μg/mL, respectively, among which compound 7
has a more potent activity than the reference drug doxorubicin against HepG‐2 cell line, showing IC50
value of 3.67 μg/mL (doxorubicin 4.65 μg/mL).

Author(s) Details

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

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

View Book :- http://bp.bookpi.org/index.php/bpi/catalog/book/217