Antiproliferative Activity of Some Newly Synthesized Substituted Nicotinamides Candidates Using Pyridine-2(1 H) thione Derivatives as Synthon

Dina H Elnaggar; Ashraf M Mohamed; Naglaa A Abdel Hafez; Mohamed E Azab; Manar E A Elasasy; Hanem M Awad; Thoraya A Farghaly; Abd El-Galil E Amr

doi:10.1021/acsomega.1c06951

Antiproliferative Activity of Some Newly Synthesized Substituted Nicotinamides Candidates Using Pyridine-2(1 H) thione Derivatives as Synthon

ACS Omega. 2022 Mar 16;7(12):10304-10316. doi: 10.1021/acsomega.1c06951. eCollection 2022 Mar 29.

Authors

Dina H Elnaggar¹, Ashraf M Mohamed¹, Naglaa A Abdel Hafez¹, Mohamed E Azab², Manar E A Elasasy¹, Hanem M Awad³, Thoraya A Farghaly⁴, Abd El-Galil E Amr⁵

Affiliations

¹ Applied Organic Chemistry Department, National Research Centre, Dokki 12622, Giza, Egypt.
² Chemistry Department, Faculty of Science, Ain Shams University, Abbasia, Cairo 11566, Egypt.
³ Department of Tanning Materials and Leather Technology, National Research Centre, Dokki, Cairo 12622, Egypt.
⁴ Department of Chemistry, Faculty of Science, Cairo University, Giza 12613, Egypt.
⁵ Organic Chemistry Department, Chemical Industries Research Division, National Research Centre, Cairo 12622, Egypt.

Abstract

Some new pyridinethione and thienopyridine derivatives have been synthesized and evaluated for their antiproliferative activity using the MTT assay. Nicotinamide derivatives 3 have been synthesized and used for the preparation of new condensed thieno [2,3-b]pyridines by their reactions with active halo compounds. Finally the synthesized thienopyridine underwent ring closure whenever possible through boiling in a solution of sodium ethoxide. The antiproliferative evaluation against (HCT-116, HepG-2, and MCF-7) human cancer cells and one human healthy cell line (BJ-1) revealed that compounds 3b, 4c-5d, 7b-12a, 10d, and 13b have interesting antitumor activity specifically as antihepatocellular and anticolon cellular carcinoma agents. Besides, the docking results for most active derivatives were in agreement with the in vitro antitumor results.