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Synthesis, antiproliferative and antibacterial evaluation of C-ring modified colchicine analogues.

Synthesis, antiproliferative and antibacterial evaluation of C-ring modified colchicine analogues.

European journal of medicinal chemistry (2014-12-02)

Adam Huczyński, Jacek Rutkowski, Katarzyna Popiel, Ewa Maj, Joanna Wietrzyk, Joanna Stefańska, Urszula Majcher, Franz Bartl

摘要

A series of 10 amine derivatives of colchicine have been obtained with high yields by modification at C(10)-OCH3 position of C-ring and characterized by spectroscopic methods. In vitro cytotoxicity has been evaluated against four human tumour cell lines (HL-60, HL-60/vinc, LoVo, LoVo/DX), as well as antibacterial activity against clinical isolates of methicillin-resistant Staphylococcus aureus (MRSA) and Staphylococcus epidermidis (MRSE). From among the compounds tested the most active is colchicine derivative 2h with bis(2-methoxyethyl)amine substituent which is active in nanomolar to submicromolar concentrations and is several times more cytotoxic than cisplatin and doxorubicin. This compound is also effective against the methicillin-resistant Staphylococci strains.

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