Abstract
A number of analogs of tubuloclustin, N-[7-(2-adamantyloxy)-7-oxoheptanoyl]-N-deacetylcolchicine, were obtained. In these analogs, the colchicine moiety is formally replaced by the cyclohexane, adamantane, and 2-methoxyestradiol moieties (the steroid is attached through the hydroxy group at the C(17) atom). MTT assays revealed that the conjugates obtained are much less cytotoxic against A549 lung carcinoma cells than the lead compound.
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Based on the materials of the First Russian Conference on Medicinal Chemistry (“MedChem Russia-2013”) with International Participation (September 8–12, 2013, Moscow).
Published in Russian in Izvestiya Akademii Nauk. Seriya Khimicheskaya, No. 5, pp. 1126–1129, May, 2014.
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Zefirova, O.N., Glazkova, Y.S., Nurieva, E.V. et al. Synthesis and biological testing of tubuloclustin analogs containing alicyclic groups and 2-methoxyestradiol moiety. Russ Chem Bull 63, 1126–1129 (2014). https://doi.org/10.1007/s11172-014-0559-x
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DOI: https://doi.org/10.1007/s11172-014-0559-x