8.8 Hz, 1H), 5.46 (d, J = 1.5 Hz, 1H), 3.52 (s, 1H), 3.44 (s, 1H), 3.16 (d, J = 5.3 Hz, 2H), 3.08 (s, 1H),
2.94 (d, 1H), 2.89 – 2.52 (m, 3H), 2.44 (t, J = 5.6 Hz, 1H), 2.42 (s, 2H), 2.43 – 2.10 (m, 5H), 1.99 –
1.85 (m, 2H), 1.80 – 1.71 (m, 1H), 1.62 – 1.53 (m, 1H), 0.93 (t, J = 7.1 Hz, 3H). 13C NMR (DMSO-
d6) δ 202.90, 178.87, 167.23, 155.21, 142.02, 135.11, 130.98, 129.47, 128.40, 125.20, 121.55, 109.92,
99.98, 76.00, 51.98, 40.60, 40.43, 40.27, 40.10, 39.93, 39.41, 38.81, 31.78, 28.02, 25.57, 14.09
UPLC−MS calculated for C36H38N8O5 [M]+: 662.29; found 663.30.
6-Acetyl-8-cyclopentyl-2-((5-(4-(((3R,3aS,9aR,10aS,10bS,E)-6,9a-dimethyl-2-oxo-
2,3,3a,4,5,8,9,9a,10a,10b-decahydrooxireno[2',3':9,10]cyclodeca[1,2-b]furan-3-yl)methyl)piperazin-
1-yl)pyridin-2-yl)amino)-5-methylpyrido[2,3-d]pyrimidin-7(8H)-one (6)
To a solution of parthenolide (25 mg, 0.100 mmol), triethylamine in methanol (2 mL) was
added palbociclib (45 mg, 0.100 mmol) and the mixture was stirred for 48 h. Then the mixture was
concentrated in vacuo and purified by prep HPLC (Yield 16 mg, 23%). 1H NMR (DMSO-d6) δ 10.08
(d, 1H), 8.95 (s, 1H), 8.05 (dd, J = 3.0, 1H), 7.84 (t, J = 9.7 Hz, 1H), 7.51 – 7.41 (m, 1H), 5.86 – 5.78
(m, 1H), 3.98 (t, J = 9.1 Hz, 1H), 3.17 (d, J = 5.1 Hz, 4H), 3.06 (t, J = 4.8 Hz, 1H), 2.89 – 2.78 (m,
2H), 2.65 (dd, J = 7.6, 2H), 2.42 (s, 3H), 2.31 (s, 4H), 2.19 (d, 4H), 2.02 (t, 2H), 1.82 (d, 6H), 1.61 (d,
6H), 1.20 (s, 3H). 13C NMR (DMSO-d6) δ 175.82, 134.70, 125.12, 81.84, 68,28, 65.79, 61.59, 59.14,
48.24, 45.22, 40.99, 40,61, 40.27, 40.10, 39.93, 39.59, 36.50, 29.08, 24.18, 17.33, 17.01UPLC−MS
calculated for C39H49N7O5 [M]+: 695.38; found 696.38.
4-(2,6-dichlorobenzamido)-N-(1-((2',5-dioxo-4,5-dihydro-3H-spiro[furan-2,3'-indolin]-4-
yl)methyl)piperidin-4-yl)-1H-pyrazole-3-carboxamide (7)
To a solution of 4-methylene-3,4-dihydro-5H-spiro[furan-2,3'-indoline]-2',5-dione (16 mg,
0.074 mmol), triethylamine in methanol (2 mL) was added AT7519 (31 mg, 0.074 mmol) and the
mixture was stirred for 48 h. Then the mixture was concentrated in vacuo and purified by prep HPLC
1
(Yield 8 mg, 18%). H NMR (DMSO-d6) δ 10.76 (d, 1H), 10.27 (d, 1H), 10.16 (d, J = 8.6 Hz, 1H),
8.43 – 8.22 (m, 2H), 7.70 – 7.42 (m, 3H), 7.28 – 6.87 (m, 3H), 6.86 – 6.69 (m, 1H), 3.58 – 3.43 (m,
2H), 3.24 (s, 2H), 2.94 – 2.61 (m, 2H), 2.43 – 2.05 (m, 2H), 2.04 – 1.83 (m, 2H), 1.80 – 1.37 (m, 4H).
13C NMR (DMSO-d6) δ 178.50, 173.77, 163.12, 159.87, 141.15, 134.86, 131.40, 130.85, 130.76,
130.62, 128.53, 127.94, 124.52, 123.97, 123.34, 122.14, 120.97, 120.93, 109.12, 74.04, 60.14, 51.82,
This article is protected by copyright. All rights reserved