Anti-Proliferative Activity of Ethylenediurea Derivatives with Alkyl and Oxygen-Containing Groups as Substituents

含烷基和含氧基团取代的乙撑二脲衍生物的抗增殖活性

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作者:Maxim Oshchepkov, Leonid Kovalenko, Antonida Kalistratova, Galina Sherstyanykh, Evgenia Gorbacheva, Alexey Antonov, Nisreen Khadour, Mikhail Akimov

Conclusions

The results obtained on the ethylenediurea analogs with ethyl substituent in the aromatic ring are promising for the development of novel anticancer therapeutics.

Methods

Ten new analogs of ethylenediurea with these substitutions were tested for anti-proliferative activity in the human cancer cell lines MDA-MB-231 (breast cancer), A-375 (melanoma), and U-87 MG (glioblastoma) during 72 h of incubation using resazurin test and evaluated the substances receptor using molecular docking.

Results

The compound with the carbamate link and ethylene substituent on the phenyl ring inhibited proliferation in these models by 70-90% without cytotoxic effects. The compound did not affect the viability of the immortalized fibroblast cell line Bj-5ta. The compound was also able to enhance the action of doxorubicin and temozolomide by about 20%. According to the molecular modeling data, the probable receptor target for the synthesized compound was the A2AR adenosine receptor. Conclusions: The results obtained on the ethylenediurea analogs with ethyl substituent in the aromatic ring are promising for the development of novel anticancer therapeutics.

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