The administration of a compound advantageously efficacious as ROS1 inhibitor and its effect on subjects with cancer includes administering a compound having certain structural components such as a quinoline moiety in the backbone and at least one tertiary amine containing moiety in a side chain as well as heteroatoms, in particular oxygen atoms, present in the backbone and the side chain for treating a subject suffering from a disease such as cancer. The presence of such structural components allows for an advantageous interaction with the ROS1 kinase domain, in particular with the hinge region. The administered compounds represent a highly promising opportunity in particular for patients bearing ROS1-dependent cancer. A method for targeting tumor cells harboring an abnormality in ROS1 gene includes contacting a cell with compounds of the present invention as well as pharmaceutical compositions comprising such compounds.