Design, synthesis and biological evaluation of a novel non-Gemini analog of UVB1 and crystal structure of its complex with the vitamin D receptor.

• Tác giả: Yagamare Fall, Generosa Gómez, Uxía Gómez-Bouzó, Carole Peluso-Iltis, Natacha Rochel, Hugo Santalla, Lieve Verlinden, Annemieke Verstuyf
• Ngôn ngữ: eng
• Thông tin xuất bản: United States : Bioorganic chemistry , 2025
• Bộ sưu tập: NCBI
• ID: 717090

Tóm tắt

We synthesized UG-650, a novel non-Gemini analog of UVB1 that combines structural features of UVB1 and MC 1288. The evaluation of the bioactivities indicates that UG-650 dose-dependently inhibited MCF-7 cell proliferation. In comparison to calcitriol, slightly lower concentrations of UG-650 were needed to achieve equivalent levels of proliferation inhibition. Structural analysis revealed that the analog forms additional interactions stabilizing VDR active form.