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Published on: June 23, 2019
Synthesis and antiproliferative activity of some new DNA-targeted alkylating pyrroloquinolines
M G Ferlin1, L Dalla Via, O M Gia
1Dipartimento di Scienze Farmaceutiche dell'Università di Padova, Via F. Marzolo, 5 35131 Padua, Italy. mariagrazia.ferlin@unipd.it
Abstract:
Two novel DNA-direct alkylating agents, consisting of aniline mustard linked to an angular 3H-pyrrolo[3,2-f]quinoline nucleus, were synthetized and assayed for their in vitro antiproliferative activity. Simple convergent synthesis, consisting of separate preparation of 9-chloro-3H-pyrrolo[3,2-f]quinoline and p-amino-aniline derivatives, and following their linkage by substitution reactions 8a, b and 10, yielded the corresponding diol derivatives 7b and 9. Biological properties were evaluated with respect to cell growth inhibition, ability to form cross-links with DNA, and capacity to give rise to a molecular complex with the macromolecule for 7b, 8b, 9 and 10.
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