Table 1.

Structures, binding affinity and anti-pancreatic cancer activities of PDEδ inhibitors.

Compd.	R1	R2	PDEδa (KD, nmol/L)	Mia PaCa-2b (IC50, μmol/L)
23a	H	Ph	1670 ± 260	46 ± 14
23b	H	2,3-Dihydro-1H-inden-5-yl	1538 ± 166	3.6 ± 2.1
23c	H	Naphthalen-1-ylmethyl	2186 ± 385	4.8 ± 1.2
23d	H	Cyclohexyl	1699 ± 178	64 ± 8.1
23e	H	Cyclopentyl	1543 ± 244	>100
36a	Ph	2-F-Benzyl	1311 ± 219	16 ± 0.10
36b	Ph	4-Cl-Benzyl	328 ± 59	4.3 ± 2.1
36c	Ph	2-Br-Benzyl	485 ± 35	12 ± 0.60
36d	Ph	3-Br-Benzyl	690 ± 198	4.9 ± 1.4
36e	Ph	1H-Imidazole-4-ylmethyl	1657 ± 436	>100
36f	Ph	Thiophen-2-ylmethyl	1475 ± 197	15 ± 5.4
36g	Ph	Thiophen-3-ylmethyl	1240 ± 106	17 ± 8.3
36h	Ph	Pyridin-2-ylmethyl	1373 ± 317	46 ± 21
36i	Ph	Pyridin-4-ylmethyl	1482 ± 18	55 ± 2.8
36j	Ph	Quinolin-6-ylmethyl	1343 ± 36	12 ± 4.0
36k	Ph	Quinolin-3-ylmethyl	1328 ± 32	13 ± 2.8
36l	Ph	Cyclohexylmethyl	127 ± 16	6.7 ± 1.7
36m	Ph	Cyclopentylmethyl	159 ± 29	18 ± 1.5
36n	Ph	Cyclobutylmethyl	393 ± 27	19 ± 4.0
36o	Ph	Cyclopropylmethyl	1125 ± 140	26 ± 1.6
9	/	/	1471 ± 246	>100
2	/	/	34 ± 4	>100

^aTested by fluorescent anisotropy assay.

^bTested by the CCK8 method.