Polygodial and Ophiobolin A Analogues for Covalent Crosslinking of Anticancer Targets




Maslivetc, Vladimir
Laguera, Breana
Chandra, Sunena
Dasari, Ramesh
Olivier, Wesley
Smith, Jason A.
Bissember, Alex C.
Masi, Marco
Evidente, Antonio
Mathieu, Veronique

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Multidisciplinary Digital Publishing Institute


In a search of small molecules active against apoptosis-resistant cancer cells, including glioma, melanoma, and non-small cell lung cancer, we previously prepared α,β- and γ,δ-unsaturated ester analogues of polygodial and ophiobolin A, compounds capable of pyrrolylation of primary amines and demonstrating double-digit micromolar antiproliferative potencies in cancer cells. In the current work, we synthesized dimeric and trimeric variants of such compounds in an effort to discover compounds that could crosslink biological primary amine containing targets. We showed that such compounds retain the pyrrolylation ability and possess enhanced single-digit micromolar potencies toward apoptosis-resistant cancer cells. Target identification studies of these interesting compounds are underway.



anticancer activity, apoptosis resistance, ophiobolin A, polygodial, wittig reaction, Chemistry and Biochemistry


Maslivetc, V., Laguera, B., Chandra, S., Dasari, R., Olivier, W. J., Smith, J. A., Bissember, A. C., Masi, M., Evidente, A., Mathieu, V., & Kornienko, A. (2021). Polygodial and Ophiobolin A analogues for covalent crosslinking of anticancer targets. International Journal of Molecular Sciences, 22(20), 11256.


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