Design and synthesis of diazine-based panobinostat analogues for HDAC8 inhibition

• Sivaraman Balasubramaniam,
• Sajith Vijayan,
• Liam V. Goldman,
• Xavier A. May,
• Kyra Dodson,
• Sweta Adhikari,
• Fatima Rivas,
• Davita L. Watkins and
• Shana V. Stoddard

Beilstein J. Org. Chem. 2020, 16, 628–637, doi:10.3762/bjoc.16.59

• the positive control consisted of HDAC8 without inhibitor added. The substrate concentration was 5 µM, and HDAC8 concentration per well was 4 ng/µL. The reaction was initiated by addition of enzyme. The fluorogenic substrate was excited at 360 nm and the emission signal was detected at 460 nm using a

Development of a fluorogenic small substrate for dipeptidyl peptidase-4

• Futa Ogawa,
• Masanori Takeda,
• Kanae Miyanaga,
• Keita Tani,
• Ryuji Yamazawa,
• Kiyoshi Ito,
• Atsushi Tarui,
• Kazuyuki Sato and
• Masaaki Omote

Beilstein J. Org. Chem. 2017, 13, 2690–2697, doi:10.3762/bjoc.13.267

• by converting 2,4-disubstituted aniline 1 to the non-fluorescent dipeptide analogue H-Gly-Pro-1 for the use as a fluorogenic substrate for dipeptidyl peptidase-4 (DPP-4). The progress of the enzymatic hydrolysis of H-Gly-Pro-1 with DPP-4 was monitored by fluorometric determination of 1 released into

• the reaction medium. The results suggest that 1 could be used as fluorophore in OFF–ON-type fluorogenic probes. Keywords: dipeptidyl peptidase-4; fluorogenic substrate; fluorometry; small fluorescent molecule; Introduction Fluorescent organic probes have become indispensable for bio-imaging or

• for DPP-4. The experimental strategy is summarized in Scheme 1; non-fluorescent H-Gly-Pro-1 is hydrolysed specifically by DPP-4 to release 1, enabling fluorometric measurements. Synthesis of the fluorogenic substrate for DPP-4 The synthesis of H-Gly-Pro-1 is shown in Scheme 2. In the synthesis, N

SF002-96-1, a new drimane sesquiterpene lactone from an Aspergillus species, inhibits survivin expression

• Silke Felix,
• Louis P. Sandjo,
• Till Opatz and
• Gerhard Erkel

Beilstein J. Org. Chem. 2013, 9, 2866–2876, doi:10.3762/bjoc.9.323

• for 5 h. (D) Induction of apoptosis by SF002-96-1 as measured by caspase-3 activity. Colo 320 cells were treated without (control) and with different concentrations of SF002-96-1 for 5 h. After lysis of the cells, 20 µM Ac-DEVD-AMC was added as fluorogenic substrate. AMC released from Ac-DEVD-AMC was