Journal: Journal of Enzyme Inhibition and Medicinal Chemistry

Article Title: Novel topoisomerase II/EGFR dual inhibitors: design, synthesis and docking studies of naphtho[2′,3′:4,5]thiazolo[3,2- a ]pyrimidine hybrids as potential anticancer agents with apoptosis inducing activity

doi: 10.1080/14756366.2023.2205043

Figure Lengend Snippet: Examples for anticancer agents targeting topoisomerase II.

Article Snippet: Using the procedure outlined in topoisomerase II Drug Screening Kit (Topogen, USA), the effect of 6a , 6c and 6i on topoisomerase II inhibition and the effectiveness of catenated/decatenated kDNA formation were examined.

Techniques:

Journal: Journal of Enzyme Inhibition and Medicinal Chemistry

Article Title: Novel topoisomerase II/EGFR dual inhibitors: design, synthesis and docking studies of naphtho[2′,3′:4,5]thiazolo[3,2- a ]pyrimidine hybrids as potential anticancer agents with apoptosis inducing activity

doi: 10.1080/14756366.2023.2205043

Figure Lengend Snippet: Diagram represents design of novel hybrids based upon thiazolo[3,2- a ] pyrimidine and 1,4-naphthoquinone moieties as dual topo II/EGFR inhibitor.

Article Snippet: Using the procedure outlined in topoisomerase II Drug Screening Kit (Topogen, USA), the effect of 6a , 6c and 6i on topoisomerase II inhibition and the effectiveness of catenated/decatenated kDNA formation were examined.

Techniques:

Journal: Journal of Enzyme Inhibition and Medicinal Chemistry

Article Title: Novel topoisomerase II/EGFR dual inhibitors: design, synthesis and docking studies of naphtho[2′,3′:4,5]thiazolo[3,2- a ]pyrimidine hybrids as potential anticancer agents with apoptosis inducing activity

doi: 10.1080/14756366.2023.2205043

Figure Lengend Snippet: Effect of the tested hybrids ( 6a, 6c and 6i ) and Dox on topoisomerase IIα concentration in MCF-7 cell line.

Article Snippet: Using the procedure outlined in topoisomerase II Drug Screening Kit (Topogen, USA), the effect of 6a , 6c and 6i on topoisomerase II inhibition and the effectiveness of catenated/decatenated kDNA formation were examined.

Techniques: Concentration Assay

Journal: Journal of Enzyme Inhibition and Medicinal Chemistry

Article Title: Novel topoisomerase II/EGFR dual inhibitors: design, synthesis and docking studies of naphtho[2′,3′:4,5]thiazolo[3,2- a ]pyrimidine hybrids as potential anticancer agents with apoptosis inducing activity

doi: 10.1080/14756366.2023.2205043

Figure Lengend Snippet: DNA topo II inhibition assay of 6i , 6a and 6c .

Article Snippet: Using the procedure outlined in topoisomerase II Drug Screening Kit (Topogen, USA), the effect of 6a , 6c and 6i on topoisomerase II inhibition and the effectiveness of catenated/decatenated kDNA formation were examined.

Techniques: Inhibition

Journal: Journal of Enzyme Inhibition and Medicinal Chemistry

Article Title: Novel topoisomerase II/EGFR dual inhibitors: design, synthesis and docking studies of naphtho[2′,3′:4,5]thiazolo[3,2- a ]pyrimidine hybrids as potential anticancer agents with apoptosis inducing activity

doi: 10.1080/14756366.2023.2205043

Figure Lengend Snippet: Docking and binding pattern of hybrids 6a ( A & B ), 6c ( C & D ), 6i ( E & F ) and Dox. ( G & H ) showing interactions with different amino acid residues found in the active site of human topo IIα ATPase (PDB code 1ZXM).

Article Snippet: Using the procedure outlined in topoisomerase II Drug Screening Kit (Topogen, USA), the effect of 6a , 6c and 6i on topoisomerase II inhibition and the effectiveness of catenated/decatenated kDNA formation were examined.

Techniques: Binding Assay