Synthesis and antiproliferative activity of amino-substituted benzimidazo[1,2- $${\varvec{a}}$$ a ]quinolines as mesylate salts designed by 3D-QSAR analysis

Synthesis and antiproliferative activity of amino-substituted benzimidazo[1,2- $${\varvec{a}}$$... Keywords Amines · Benzimidazo[1,2-a]quinolines · 17]. Additional biological studies including DNA-binding Mesylate salts · 3D-QSAR · Anticancer · Microwave propensities, topoisomerases I and II inhibition, cell cycle perturbances and cellular localization confirmed the anti- cancer potency of these derivatives. Therefore, considering Introduction all of the above and that positively charged cyclic benzimida- zole derivatives could contribute significantly to the complex Being part of nitrogen-containing heterocycles, benzimida- stability with potential biological targets as well as improve the solubility of compounds, we designed novel cyclic deriva- zoles are common building motifs of synthetic or naturally tives as mesylate salts by using QSAR analysis, one of the occurring biologically active organic molecules [1–3]. Benz- few computations techniques that can be applied to study imidazoles possess a wide range of biological activities such their antiproliferative activity. as anticancer [4], antiviral [5], antibacterial [6], antifungal In the present work, we applied 3D-QSAR modelling [7], and antihypertension [8–10]. based on a VolSurf+ approach in order to make the more Recently, our scientific research was focused on the synthesis of condensed, tetracyclic benzannulated benzim- effective experimental searching for novel benzimidazole derivatives with enhanced antiproliferative activity. The idazole derivatives possessing a highly conjugated skeleton substituted with diverse Molecular Diversity Springer Journals

Synthesis and antiproliferative activity of amino-substituted benzimidazo[1,2- $${\varvec{a}}$$ a ]quinolines as mesylate salts designed by 3D-QSAR analysis

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Springer International Publishing
Copyright © 2017 by Springer International Publishing Switzerland
Life Sciences; Biochemistry, general; Organic Chemistry; Polymer Sciences; Pharmacy
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