Table 1.

Structure activity relationships of cinchona alkaloid‐derived autophagy inhibitors. IC₅₀ data represents the ability to inhibit autophagy induced by amino acid starvation using EBSS and is mean ± SD of three independent experiments. 2=Autoquin.

Entry	#	R	R1	R2	R3	R4	IC50 [μm]
1	2	OMe	p‐F‐C6H4	H	H	H	0.56±0.15
2	7 a	OMe	p‐Cl‐C6H4	H	H	H	2.44±1.01
3	7 b	OMe	p‐Me‐C6H4	H	H	H	2.31±0.07
4	7 c	OMe	Ph	H	H	H	>10
5	7 d	OMe	m‐Br‐C6H4	H	H	H	7.48±0.70
6	7 e	OMe	m‐Cl‐C6H4	H	H	H	5.70±0.39
7	7 f	OMe	m‐Cl‐p‐F‐C6H3	H	H	H	>10
8	9 a	OMe	H	p‐F‐C6H4	H	H	>10
9	9 b	OMe	H	m‐Cl‐C6H4	H	H	>10
10	9 c	OMe	H	m‐Cl‐p‐F‐C6H3	H	H	5.40±2.40
11	9 d	OMe	H	Ph	H	H	>10
12	8 a	H	p‐F‐C6H4	H	H	H	1.62±0.19
13	8 b	H	p‐Cl‐C6H4	H	H	H	Toxic
14	8 c	H	p‐Me‐C6H4	H	H	H	>10
15	8 d	H	Ph	H	H	H	>10
16	8 e	H	m‐Br‐C6H4	H	H	H	>10
17	8 f	H	m‐Cl‐C6H4	H	H	H	5.43±0.13
18	8 g	H	m‐Cl‐p‐F‐C6H4	H	H	H	>10
19	10 a	H	H	H	p‐F‐C6H4	H	>10
20	10 b	H	H	H	p‐Cl‐C6H4	H	2.52±0.32
21	10 c	H	H	H	m‐Br‐C6H4	H	>10
22	11 a	OMe	p‐F‐C6H4	H	H	H	3.30±1.60
23	11 b	OMe	p‐Cl‐C6H4	H	H	H	2.70±1.30
24	11 c	OMe	p‐Me‐C6H4	H	H	H	>10
25	11 d	OMe	Ph	H	H	H	>10
26	11 e	OMe	m‐Br‐C6H4	H	H	H	2.72±1.31
27	11 f	OMe	m‐Cl‐C6H4	H	H	H	na
28	11 g	OMe	m‐Cl‐p‐F‐C6H3	H	H	H	na
29	12 a	H	p‐F‐C6H4	H	H	H	>10
30	12 b	H	p‐Cl‐C6H4	H	H	H	5.84±1.30
31	12 c	H	p‐Me‐C6H4	H	H	H	>10
32	12 d	H	Ph	H	H	H	>10
33	12 e	H	m‐Br‐C6H4	H	H	H	>10
34	13 a	H	H	H	p‐F‐C6H4	H	>10
35	13 b	H	H	H	p‐Cl‐C6H4	H	na
36	13 c	H	H	H	Ph	H	>10
37	16 a	OMe	H	H	H	p‐F‐C6H4	>10
38	16 b	OMe	H	H	H	p‐Cl‐C6H4	>10
39	16 c	OMe	H	H	H	p‐NO2‐C6H4	3.87±0.69
40	16 d	OMe	H	H	H	p‐CF3‐C6H4	3.52±0.69
41	16 e	OMe	H	H	H	p‐NHBoc‐C6H4	>10
42	16 f	OMe	H	H	H	4‐py	>10
43	16 g	OMe	H	H	H	m‐F‐C6H4	>10
44	16 h	OMe	H	H	H	m‐F‐p‐F‐C6H4	>10
45	16 i	OMe	H	H	H	3,5‐di‐F‐ C6H4	>10
46	16 j	OMe	H	H	H	m‐Cl‐p‐F‐C6H4	>10
47	16 k	OMe	H	H	H	3,4‐di‐OMe‐ C6H4	>10
48	16 l	OMe	H	H	H	3,5‐di‐OMe‐ C6H4	>10
49	14	OMe	H	H	H	‐Br	>10