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Abstract Total syntheses of 6 BE-43547A2 analogues modified at O35 and C15 sites are reported. Late stage oxidation of 15-deoxy-BE-43547A2 delivered 15-epi-BE-43547A2, which verified the proposition that the C15 is… Click to show full abstract
Abstract Total syntheses of 6 BE-43547A2 analogues modified at O35 and C15 sites are reported. Late stage oxidation of 15-deoxy-BE-43547A2 delivered 15-epi-BE-43547A2, which verified the proposition that the C15 is an active site for late stage oxidation. The N35 and C15-F of analogues 1b and 1d were synthesized. Cellular level tests indicated O35 is a prohibitive site for modification and substitution of the OH at C15 with F or trim of the OH both led to a dramatic loss of activity. Compound 1e showed comparable inhibitory level towards Panc-1 cells, which indicated that the OH at C15 are permissive site for further modifications.
Journal Title: Tetrahedron
Year Published: 2019
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