Wydział Chemii

Izabela Jęśkowiak

Stanisław Ryng

Marta Świtalska

Joanna Wietrzyk

Iwona Bryndal

Tadeusz Lis

Marcin Mączyński

2020

Molecules

25

88/1-88/16

10.3390/molecules25010088

Naukowa

Angielski

Artykuł

Thanks to the progress in oncology, pharmacological treatment of cancer is gaining in importance and in the near future anti-cancer chemotherapeutics are expected to be the main method of treatment for cancer diseases. What is more, the search for new anti-cancer compounds with the desired application properties is constantly underway. As a result of designed syntheses, we obtained some new N’-substituted 5-chloro-3-methylisothiazole-4-carboxylic acid hydrazide derivatives with anticancer activity. The structure of new compounds was determined by mass spectrometry (MS), elemental analysis, proton nuclear magnetic resonance spectroscopy (¹H-NMR), carbon nuclear magnetic resonance spectroscopy (¹³C-NMR), ¹H-¹³C NMR correlations and infrared spectroscopy (IR). Moreover, the structures of the compounds were confirmed by crystallographic examination. The antiproliferative MTT tests for 11 prepared compounds was conducted towards human biphenotypic B cell myelomonocytic leukemia MV4-11. SRB test was used to examine their potential anticancer activity towards human colon adenocarcinoma cell lines sensitive LoVo, resistant to doxorubicin LoVo/DX, breast adenocarcinoma MCF-7 and normal non-tumorigenic epithelial cell line derived from mammary gland MCF-10A. The most active compound was 5-chloro-3-methyl-N′-[(1E,2E)-(3-phenyloprop-2-en-1-ylidene]isothiazole-4-carbohydrazide, which showed the highest antiproliferative activity against all tested cell lines.

5-chloro-3-methylisothiazole-4-carboxylic acid hydrazide derivatives, antiproliferative activity, isothiazole

CC-BY

http://dx.doi.org/10.3390/molecules25010088

http://www.mdpi.com/journal/metals