Inhibition of protein kinases by anticancer DNA intercalator, 4-butylaminopyrimido[4',5':4,5]thieno(2,3-)quinoline.

Targeting protein kinases (PKs) has been a promising strategy in treating cancer, as PKs are key regulators of cell survival and proliferation. Here in this study, we studied the ability of pyrimido[4',5':4,5]thieno(2,3-)quinolines (PTQ) to inhibit different PKs by performing computational docking and screening. Docking studies revealed that 4-butylaminopyrimido[4',5':4,5]thieno(2,3-)quinoline (BPTQ) has a higher order of interaction with the kinase receptors than other PTQ derivatives.

Cell Cycle Arrest and Induction of Apoptosis in Colon Adenocarcinoma Cells by a DNA Intercalative Quinoline Derivative, 4-Morpholinopyrimido [4',5':4,5] Selenolo (2,3-b) Quinoline.

Circular dichroism, topological studies, molecular docking, absorbance, and fluorescence spectral titrations were employed to study the interaction of 4-morpholinopyrimido [4',5':4,5] selenolo (2,3-b) quinoline (MPSQ) with DNA. The association constants of MPSQ-DNA interactions were of the order of 10(4) M(-1). Melting temperature, topological, and docking studies confirmed that the mode of interaction was by intercalation with preference to d(GpC)-d(CpG) site of DNA.

DNA intercalative 4-butylaminopyrimido[4',5':4,5]thieno(2,3-b)quinoline induces cell cycle arrest and apoptosis in leukemia cells.

Purpose: DNA intercalators are one of the interesting groups in cancer chemotherapy. The development of novel anticancer small molecule has gained remarkable interest over the last decade. In this study, we synthesized and investigated the ability of a tetracyclic-condensed quinoline compound, 4-butylaminopyrimido[4',5':4,5]thieno(2,3-b)quinoline (BPTQ), to interact with double-stranded DNA and inhibit cancer cell proliferation.