@conference{
author = "Koračak, Ljiljana and Selaković, Milica and Lupšić, Ema and Podolski-Renić, Ana and Selaković, Života and Novaković, Miroslav and Pešić, Milica and Opsenica, Igor M.",
year = "2024",
abstract = "Artesunate, a derivative of the natural product artemisinin, displays anticancer activity against a wide variety of cancer cell lines. While natural products serve as excellent lead compounds, additional synthetic transformations are often necessary to achieve ‘‘tailor-made’’ final structure.1 The concept of hybrid molecules with fusion of two different pharmacophores where one or both may be inspired by naturally occurring molecules allowing significant enhancements in physicochemical and pharmacokinetic roperties.2
This study focused on synthesizing novel hybrid molecules combining artesunate and a pyrimidine scaffold to assess their efficacy against both sensitive and multidrug-resistant (MDR) human non-small cell lung carcinoma (NSCLC) cells. Several synthesized hybrids exhibited higher activity against both examined cell lines than the parent compounds. In addition, increased sensitivity of MDR NSCLC cells to doxorubicin was observed when it was applied in combination with novel hybrid molecules as well as the inhibition of P-glycoprotein activity.
References:
1) Z. Guo, Acta Pharm. Sin. B, 2017, 7, 119–136
2) C. Borsari, D. J. Trader, A. Tait and M. P. Costi, J. Med. Chem., 2020, 63, 1908–1928",
publisher = "Belgium: Scientific Conference Producers - LD Organisation srl",
journal = "Book of Abstracts: EFSM-ISMC: International Symposium on Medicinal Chemistry; 2024 Sep 1-5; Rome, Italy",
title = "Synthesis of Artesunate-Pyrimidine Hybrids and Evaluation of Their Activity Against Multidrug-Resistant Cancer Cells",
pages = "345",
url = "https://hdl.handle.net/21.15107/rcub_ibiss_7024"
}
