e.g. Filippa Pettersson or Cancer Res. 75(6) , 1102-12, (2015) or 10.1002/anie.201600521

Inhibitors of cyclic AMP phosphodiesterase. 1. Analogs of cilostamide and anagrelide

GH Jones, MC Venuti, R Alvarez, JJ Bruno…

Index: Jones; Venuti; Alvarez; Bruno; Berks; Prince Journal of Medicinal Chemistry, 1987 , vol. 30, # 2 p. 295 - 303

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Citation Number: 46

Abstract

Evaluation of a series of lactam heterocyclic analogues of cilostamide (2) as inhibitors of cyclic AMP phosphodiesterase derived from both human platelets and rat heart in comparison with their corresponding methoxy-substituted heterocycles has revealed that the N-cyclohexyl-N-methyl-4-oxybutyramide side chain of 2 is an important lipophilic and/or steric pharmacophore. Attachment of this side chain to the parent heterocycle of the potent ...

N-Methylcyclohexanamine Structure

N-Methylcyclohe...

~%

Lixazinone Structure

5-Hydroxy-2-nitrobenzaldehyde Structure

5-Hydroxy-2-nit...

~%

Lixazinone Structure

ethyl 4-((3-formyl-4-nitrophenyl)oxy)butyrate Structure

ethyl 4-((3-for...

~%

Lixazinone Structure

ethyl 2-((5-(4-(cyclohexyl(methyl)amino)-4-oxobutoxy)-2-nitrobenzyl)amino)acetate Structure

ethyl 2-((5-(4-...

~%

Lixazinone Structure

4-(3-FORMYL-4-NITRO-PHENOXY)-BUTYRIC ACID Structure

4-(3-FORMYL-4-N...

~%

Lixazinone Structure

4-(3-formyl-4-nitrophenoxy)butanoyl chloride Structure

4-(3-formyl-4-n...

~%

Lixazinone Structure

6-Methoxy-2(3H)-benzothiazolone Structure

6-Methoxy-2(3H)...

~94%

2(3H)-Benzothiazolone,6-hydroxy-(9CI) Structure

2(3H)-Benzothia...

2-Amino-6-methoxybenzothiazole Structure

2-Amino-6-metho...

~%

2(3H)-Benzothiazolone,6-hydroxy-(9CI) Structure

2(3H)-Benzothia...

Benzenethiol,2-amino-5-methoxy- Structure

Benzenethiol,2-...

~%

7-hydroxy-4H-1,4-benzothiazin-3-one Structure

7-hydroxy-4H-1,...

2,3-diamino-2-methylpropanoic acid dihydrochloride Structure

2,3-diamino-2-m...

~54%

(2-Amino-5-methoxyphenyl)methanol Structure

(2-Amino-5-meth...

N/A Structure

~%

Cilostamide Structure

N-Methylcyclohexanamine Structure

N-Methylcyclohe...

~%

Cilostamide Structure

5-Hydroxy-2-nitrobenzaldehyde Structure

5-Hydroxy-2-nit...

~%

Cilostamide Structure

ethyl 4-((3-formyl-4-nitrophenyl)oxy)butyrate Structure

ethyl 4-((3-for...

~%

Cilostamide Structure

N-cyclohexyl-N-methyl-4-[3-(2-carboxyvinyl)-4-nitrophenoxy]butyramide Structure

N-cyclohexyl-N-...

~%

Cilostamide Structure

4-(3-FORMYL-4-NITRO-PHENOXY)-BUTYRIC ACID Structure

4-(3-FORMYL-4-N...

~%

Cilostamide Structure

4-(3-formyl-4-nitrophenoxy)butanoyl chloride Structure

4-(3-formyl-4-n...

~%

Cilostamide Structure

N-Cyclohexyl-N-methyl-4-(3-formyl-4-nitrophenyl)-oxybutyramide Structure

N-Cyclohexyl-N-...

~%

Cilostamide Structure

Inhibitors of cyclic AMP phosphodiesterase. 4. Synthesis and...

[Venuti, Michael C.; Alvarez, Robert; Bruno, John J.; Strosberg, Arthur M.; Gu, Leo; et al. Journal of Medicinal Chemistry, 1988 , vol. 31, # 11 p. 2145 - 2152]

Inhibitors of cyclic AMP phosphodiesterase. 4. Synthesis and...

[Venuti, Michael C.; Alvarez, Robert; Bruno, John J.; Strosberg, Arthur M.; Gu, Leo; et al. Journal of Medicinal Chemistry, 1988 , vol. 31, # 11 p. 2145 - 2152]