Litcius/Paper detail

Synthesis, molecular docking of new amide thiazolidine derived from isoniazid and studying their biological activity against cancer cells

Ahmed A. Majed, Dunya AL-Duhaidahawi, Haider A. Omran, Sabah Abbas, Dawood S. Abid, Ahmed Y. Hmood

2023Journal of Biomolecular Structure and Dynamics12 citationsDOIOpen Access PDF

Abstract

BCL2, an antiapoptotic protein, is overexpressed in many cancers, making it a good cancer treatment target. In 30 years, few BCL2 targeting agents have shown clinical significance. This work designed new amide thiazolidine derived from isoniazid targeting BCL2 and tested them on cancer cell lines, for binding affinities, the novel candidates were docked to the BCL2 target receptor. IC50 of compound A8 46.67 ± 0.9 and 57.14 ± 0.88 μg/ml against PC3 and HEPG2 respectively with docking score −7.6 Kcal/mol with 6GL8 make it the best compound in this series. Melting point, FT-IR, elemental microanalysis (CHN), 1HNMR, and 13CNMR confirmed chemical structures.Communicated by Ramaswamy H. Sarma

Topics & Concepts

AmideChemistryThiazolidineDocking (animal)IsoniazidStereochemistryCombinatorial chemistryBiochemistryMedicineTuberculosisPathologyNursingComputational Drug Discovery MethodsSynthesis and biological activityClick Chemistry and Applications