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Design, Synthesis, and Anticancer Evaluation of Fused 1,2-diazine Derivatives

1
Faculty of Chemistry, Alexandru Ioan Cuza University of Iasi, 11 Carol I, 700506 Iasi, Romania
2
CERNESIM Research Centre, Alexandru Ioan Cuza University of Iasi, 11 Carol I, 700506 Iasi, Romania
*
Author to whom correspondence should be addressed.
Presented at the 2nd Molecules Medicinal Chemistry Symposium (MMCS): Facing Novel Challenges in Drug Discovery, Barcelona, Spain, 15–17 May 2019.
Proceedings 2019, 22(1), 26; https://doi.org/10.3390/proceedings2019022026
Published: 7 August 2019
(This article belongs to the Proceedings of The Molecules Medicinal Chemistry Symposium)
PDF [141 KB, uploaded 7 August 2019]

Abstract

Cancer is one of the most serious and merciless health problems of humankind, and the number of new cases is expected to increase in the next decades. Despite extensive cancer research in order to find more effective drugs and treatments, cancer chemotherapy is complex and complicated, because of the limited efficacy of drugs, significant levels of toxicity, and lack of selectivity, and the emergence of drug resistance and multidrug resistance make the situation even worse. We report here the design, synthesis, structure, and in vitro anticancer activity of two series of compounds derived from pyridazine and phthalazine. The in vitro anticancer activity was tested on a panel of 60 human tumor cell lines representing cancers of the brain, breast, colon, kidney, lung, ovary, prostate, as well as leukemia and melanoma, to the National Cancer Institute (USA). The test was conducted on a single dose and five dose assay. Notably, from the tested compounds, five of them show very good anticancer activity (superior to Doxorubicin, the NCI standard drug for this type of analysis), with a growth inhibition in the area of nanomolar, between 20–100 nM, on several cancer cell lines: breast cancer MCF7, colon cancer HCT-15, KM12 and SW-620, leukemia K562 and SR, melanoma MDA-MB-435, SK-MEL-5, and UACC-62, and renal cancer A498. SAR correlation in the two series and in between the two series has been performed. One compound has an excellent anticancer activity against breast cancer MCF7 cell, leukemia SR cell, and melanoma MDA-MB-435 cell, in the area of 20 nM.
Keywords: breast cancer; colon cancer; leukemia; melanoma; renal cancer; nano molar anticancer activity; pyridazine; phthalazine breast cancer; colon cancer; leukemia; melanoma; renal cancer; nano molar anticancer activity; pyridazine; phthalazine
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).
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Vasilichia, A.; Dorina, A.-M.; Violeta, M.; Ramona, D.; Ionel, M.I. Design, Synthesis, and Anticancer Evaluation of Fused 1,2-diazine Derivatives. Proceedings 2019, 22, 26.

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