TY - JOUR
T1 - Synthesis of Novel Lipophilic Polyamines via Ugi Reaction and Evaluation of Their Anticancer Activity
AU - Nichugovskiy, Artemiy
AU - Maksimova, Varvara
AU - Trapeznikova, Ekaterina
AU - Eshtukova-Shcheglova, Elizaveta
AU - Ivanov, Igor
AU - Yakubovskaya, Marianna
AU - Kirsanov, Kirill
AU - Cheshkov, Dmitry
AU - Tron, Gian Cesare
AU - Maslov, Mikhail
N1 - Publisher Copyright:
© 2022 by the authors.
PY - 2022/10
Y1 - 2022/10
N2 - Natural polyamines (PAs) are involved in the processes of proliferation and differentiation of cancer cells. Lipophilic synthetic polyamines (LPAs) induce the cell death of various cancer cell lines. In the current paper, we have demonstrated a new method for synthesis of LPAs via the multicomponent Ugi reaction and subsequent reduction of amide groups by PhSiH3. The anticancer activity of the obtained compounds was evaluated in the A-549, MCF7, and HCT116 cancer cell lines. For the first time, it was shown that the anticancer activity of LPAs with piperazine fragments is comparable with that of aliphatic LPAs. The presence of a diglyceride fragment in the structure of LPAs appears to be a key factor for the manifestation of high anticancer activity. The findings of the study strongly support further research in the field of LPAs and their derivatives.
AB - Natural polyamines (PAs) are involved in the processes of proliferation and differentiation of cancer cells. Lipophilic synthetic polyamines (LPAs) induce the cell death of various cancer cell lines. In the current paper, we have demonstrated a new method for synthesis of LPAs via the multicomponent Ugi reaction and subsequent reduction of amide groups by PhSiH3. The anticancer activity of the obtained compounds was evaluated in the A-549, MCF7, and HCT116 cancer cell lines. For the first time, it was shown that the anticancer activity of LPAs with piperazine fragments is comparable with that of aliphatic LPAs. The presence of a diglyceride fragment in the structure of LPAs appears to be a key factor for the manifestation of high anticancer activity. The findings of the study strongly support further research in the field of LPAs and their derivatives.
KW - anticancer activity
KW - lipophilic polyamines
KW - multicomponent Ugi reaction
KW - polyamines
UR - http://www.scopus.com/inward/record.url?scp=85139812746&partnerID=8YFLogxK
U2 - 10.3390/molecules27196218
DO - 10.3390/molecules27196218
M3 - Article
SN - 1420-3049
VL - 27
JO - Molecules
JF - Molecules
IS - 19
M1 - 6218
ER -
