Table 3.

In vitro antiproliferative activities of celastrol derivatives 1–14 against normal cell line (LO2) and selectivity index.

Compounds	IC50 for LO2 (µM)a	Selectivity indexb
		BEL-7402	AGS	HCT-116	HepG-2	MGC-803	A549
1	0.46 ± 0.05	0.68	0.98	0.98	0.74	1.24	0.14
2	0.39 ± 0.03	0.67	1.22	1.22	0.52	1.34	0.09
3	0.43 ± 0.04	0.68	1.23	1.10	0.68	1.59	0.14
4	1.28 ± 0.30	2.17	2.98	2.67	0.13	4.00	<0.01
5	0.48 ± 0.07	0.39	1.33	0.91	0.04	1.23	<0.00
6	0.71 ± 0.09	0.96	1.73	0.76	0.10	1.78	<0.01
7	0.73 ± 0.17	0.63	1.74	1.26	0.22	1.92	0.18
8	0.61 ± 0.09	0.85	1.69	1.17	0.46	1.53	0.12
9	0.67 ± 0.07	1.14	1.56	1.43	0.26	1.63	0.21
10	0.64 ± 0.09	0.79	1.64	1.31	0.68	1.60	0.20
11	1.63 ± 0.24	1.23	1.20	1.22	0.54	3.54	0.30
12	4.56 ± 0.79	0.84	2.17	1.65	<0.05	4.18	<0.05
13	0.38 ± 0.04	0.49	1.19	0.67	0.22	1.12	0.05
14	0.71 ± 0.11	0.86	1.92	1.11	0.56	1.82	0.19
celastrol	0.47 ± 0.19	0.59	1.21	1.09	0.38	1.34	0.09

^aIC₅₀: concentration that inhibits 50%.

^bSI: selective index (IC₅₀ against normal cells/IC₅₀ against tumour cells).