Previously, we reported the synthesis and cytotoxic evaluation of several 9-anilino-2-(methylthio)thiazolo[5,4-b]quinoline derivatives with a fluorine atom at 7-position. This modification did not improve the activity. Novel derivatives of 9-anilino-7-substituted-thiazolo[5,4-b]quinoline were synthesized and tested in vitro against several human tumor cell lines In general, 7-chloro and 7-methoxy derivatives were more active than 7-fluoro analogues. SAR analysis indicated that the activity is regulated by the substitution pattern at the aniline ring. Additional studies about electronic properties of all compounds indicated that LUMO energy values and dipole moment orientation are related to the cytotoxic activity.

Synthesis, cytotoxic activity, and SAR analysis of novel derivatives of 9-anilino-7-susbtituted-2-(methylthio)thiazolo[5,4-<i>b</i>]quinoline

244th National Meeting (2012)

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Synthesis, cytotoxic activity, and SAR analysis of novel derivatives of 9-anilino-7-susbtituted-2-(methylthio)thiazolo[5,4-b]quinoline