Isoxazole-pyrimidine derivatives as TACC3 inhibitors: A novel modality to targeted cancer therapy.

Deniz Lengerli¹, Özge Akbulut Çalışkan², Kübra Çalışkan¹, Özge Saatci², Chaemin Lim³, Sridhar Vempati³, Burcu Çalışkan¹, Özgür Şahin², Erden Banoglu⁴

¹Gazi University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, 06560 Ankara, Turkey.

²Department of Drug Discovery and Biomedical Sciences, University of South Carolina, Columbia, SC 29208, USA.

³A2A Pharmaceuticals, Inc., 1185 Avenue of the Americas, New York, NY 10036, USA.

⁴Gazi University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, 06560 Ankara, Turkey. Electronic address: banoglu@gazi.edu.tr.

PubMed DOI

Abstract

Inhibiting the function of transforming acidic coiled-coil 3 (TACC3) offers a promising therapeutic approach for various cancers, such as breast, ovarian, and lung cancers.Our previous work introduced BO-264 as a novel chemotype for inhibiting TACC3 function, though it exhibited relatively low metabolic stability. In this study, sixty-two compounds were designed and synthesized to modify the struc…

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