Development of pyrimidine-cinnamamide hybrids as potential anticancer agents: A rational design approach

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15310%2F22%3A73616090" target="_blank" >RIV/61989592:15310/22:73616090 - isvavai.cz</a>
Result on the web
<a href="https://www.sciencedirect.com/science/article/pii/S0022286022012509" target="_blank" >https://www.sciencedirect.com/science/article/pii/S0022286022012509</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1016/j.molstruc.2022.133594" target="_blank" >10.1016/j.molstruc.2022.133594</a>

Result language
angličtina
Original language name
Development of pyrimidine-cinnamamide hybrids as potential anticancer agents: A rational design approach
Original language description
Pyrimidine is a privileged scaffold and part of many anti-cancer drugs, whereas cinnamamides are present in many natural products. The present work reports the rational design and synthesis of 26 novel pyrimidine and cinnamamide hybrid analogs with further optimization in the core structure. The synthesized derivatives were tested against K-562 (chronic myeloid leukemia), MV4-11 (acute myeloid leukemia), G361 (malignant melanoma), and HCC827 (lung adenocarcinoma) cell lines. Compounds 10j, 10m, 10r, and 10t displayed low micromolar potency against leukemia cell lines. 10m and 10r were the most potent analogs against G361 and HCC827 cell lines. Subsequently, structure-activity relationship study was carried out and revealed the nitro substitution was unfavorable for the activity. Cellular effects of compounds 10j and 10t were studied in the most sensitive cell line K562. The compounds arrested the cell cycle in G2/M phases and induced caspase-independent cell death.
Czech name
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Czech description
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Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
10403 - Physical chemistry

Project
Result was created during the realization of more than one project. More information in the Projects tab.
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Publication year
2022
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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