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Molecular design and synthesis of new heterobivalent compounds based on chlorambucil and colchicine

Evgeniya Vladimirovna Nurieva 1
Evgeniya Vladimirovna Nurieva
, 
Nikolay Alekseevich Zefirov 1, 2
Nikolay Alekseevich Zefirov
, 
Nele Fritsch 3
Nele Fritsch
, 
Elena Rudol'fovna Milaeva 1, 2
Elena Rudol'fovna Milaeva
, 
Sergei A Kuznetsov 3
Sergei A Kuznetsov
, 
Ol'ga Nikolaevna Zefirova 1, 2
Ol'ga Nikolaevna Zefirova
10.1016/j.mencom.2020.11.005
Published 2020-11-03
Communication , Volume 30, Issue 6, 706-708
5
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Nurieva E. V. et al. Molecular design and synthesis of new heterobivalent compounds based on chlorambucil and colchicine // Mendeleev Communications. 2020. Vol. 30. No. 6. pp. 706-708.
GOST all authors (up to 50) Copy
Nurieva E. V., Zefirov N. A., Fritsch N., Milaeva E. R., Kuznetsov S. A., Zefirova O. N. Molecular design and synthesis of new heterobivalent compounds based on chlorambucil and colchicine // Mendeleev Communications. 2020. Vol. 30. No. 6. pp. 706-708.
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TY - JOUR
DO - 10.1016/j.mencom.2020.11.005
UR - https://mendcomm.colab.ws/publications/10.1016/j.mencom.2020.11.005
TI - Molecular design and synthesis of new heterobivalent compounds based on chlorambucil and colchicine
T2 - Mendeleev Communications
AU - Nurieva, Evgeniya Vladimirovna
AU - Zefirov, Nikolay Alekseevich
AU - Fritsch, Nele
AU - Milaeva, Elena Rudol'fovna
AU - Kuznetsov, Sergei A
AU - Zefirova, Ol'ga Nikolaevna
PY - 2020
DA - 2020/11/03
PB - Mendeleev Communications
SP - 706-708
IS - 6
VL - 30
ER -
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@article{2020_Nurieva,
author = {Evgeniya Vladimirovna Nurieva and Nikolay Alekseevich Zefirov and Nele Fritsch and Elena Rudol'fovna Milaeva and Sergei A Kuznetsov and Ol'ga Nikolaevna Zefirova},
title = {Molecular design and synthesis of new heterobivalent compounds based on chlorambucil and colchicine},
journal = {Mendeleev Communications},
year = {2020},
volume = {30},
publisher = {Mendeleev Communications},
month = {Nov},
url = {https://mendcomm.colab.ws/publications/10.1016/j.mencom.2020.11.005},
number = {6},
pages = {706--708},
doi = {10.1016/j.mencom.2020.11.005}
}
MLA
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Nurieva, Evgeniya Vladimirovna, et al. “Molecular design and synthesis of new heterobivalent compounds based on chlorambucil and colchicine.” Mendeleev Communications, vol. 30, no. 6, Nov. 2020, pp. 706-708. https://mendcomm.colab.ws/publications/10.1016/j.mencom.2020.11.005.

Keywords

adamantane
chlorambucil
colchicine
dual target profile
heterobivalent compounds
lung carcinoma A549
tubulin
twin drugs

Abstract

Two new heterobivalent molecules were designed by linking a DNA-alkylating agent chlorambucil with tubulin-targeting compound colchicine or its adamantyl containing C(7)-derivative. Target compounds were synthesized via acid coupling with N-deacetylcolchicine. According to preliminary biotests, both conjugates caused microtubule depolymerization and strong tubulin clustering, and colchicine–chlorambucil conjugate was found to be one order of magnitude more potent and to exhibit some selectivity to A549 carcinoma cells.

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