Journal of Biological Inorganic Chemistry p. 139 - 149 (2019)
Update date:2022-08-11
Topics:
Mbaba, Mziyanda
de la Mare, Jo-Anne
Sterrenberg, Jason N.
Kajewole, Deborah
Maharaj, Shantal
Edkins, Adrienne L.
Isaacs, Michelle
Hoppe, Heinrich C.
Khanye, Setshaba D.
Abstract: A series of tailored novobiocin–ferrocene conjugates was prepared in moderate yields and investigated for in vitro anticancer and antiplasmodial activity against the MDA-MB-231 breast cancer line and Plasmodium falciparum 3D7 strain, respectively. While the target compounds displayed moderate anticancer activity against the breast cancer cell line with IC50 values in the mid-micromolar range, compounds 10a–c displayed promising antiplasmodial activity as low as 0.889?μM. Furthermore, the most promising compounds were tested for inhibitory effects against a postulated target, heat shock protein 90 (Hsp90). Graphical abstract: A selection of tailored novobiocin derivatives bearing the organometallic ferrocene unit were synthesized and characterized by common spectroscopic techniques. The target compounds were investigated for in vitro anticancer and antimalarial activity against the MDA-MB-231 breast cancer cell line and Plasmodium falciparum 3D7 strain, respectively.[Figure not available: see fulltext.].
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