Synthesis of novel indole derivatives as promising DNA-binding agents and evaluation of antitumor and antitopoisomerase I activities

European Journal of Medicinal Chemistry
Elizabeth Almeida LafayetteMaria do Carmo Alves de Lima

Abstract

Molecules bearing indole nucleus present diverse biological properties such as antitumor and anti-inflammatory activities that can be associated both to DNA and protein interactions. This study focused on the synthesis of new indole derivatives with thiazolidines and imidazolidine rings condensed as side chains as well as the evaluation of their ability to interact with the DNA and antitumor and topoisomerase inhibition activities. All derivatives were successfully synthesized and their structures were elucidated by mass spectrometry (MS), infrared (IR), spectroscopy (1)H NMR, (13)C NMR, COSY (1)H-(1)H and HSQC (1)H-(13)C. The antitumor activity was evaluated against different cancer cell lines using the antiproliferative MTT assay. DNA binding ability was analyzed by absorption spectroscopy and fluorescence technique using ethidium bromide (EB) as a fluorescent probe. Changes were observed in spectroscopic properties of the compounds after interacting with ctDNA (calf thymus DNA), with hypochromic and hyperchromic effects, besides blue or red shifts in the maxima of spectra. The indole derivative 5-(1H-Indol-3-ylmethylene)-thiazolidin-2,4-dione (4c) presented the best results in antitumor assay against the breast line tested (...Continue Reading

Citations

Mar 14, 2019·Anti-cancer Agents in Medicinal Chemistry·Kamalpreet Kaur, Vikas Jaitak
Apr 29, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Volodymyr HorishnyMarina Sokovic
Dec 29, 2020·International Journal of Biological Macromolecules·Josival Emanuel Ferreira AlvesSinara Mônica Vitalino de Almeida

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