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1.
Bioorg Med Chem ; 24(5): 1136-41, 2016 Mar 01.
Article in English | MEDLINE | ID: mdl-26850376

ABSTRACT

Two classes of modified analogs of 4-(thiazol-5-yl)benzoic acid-type CK2 inhibitors were designed. The azabenzene analogs, pyridine- and pyridazine-carboxylic acid derivatives, showed potent protein kinase CK2 inhibitory activities [IC50 (CK2α)=0.014-0.017µM; IC50 (CK2α')=0.0046-0.010µM]. Introduction of a 2-halo- or 2-methoxy-benzyloxy group at the 3-position of the benzoic acid moiety maintained the potent CK2 inhibitory activities [IC50 (CK2α)=0.014-0.016µM; IC50 (CK2α')=0.0088-0.014µM] and led to antiproliferative activities [CC50 (A549)=1.5-3.3µM] three to six times higher than those of the parent compound.


Subject(s)
Benzoic Acid/chemistry , Benzoic Acid/pharmacology , Protein Kinase Inhibitors/chemistry , Protein Kinase Inhibitors/pharmacology , Casein Kinase II/antagonists & inhibitors , Casein Kinase II/metabolism , Cell Line, Tumor , Cell Proliferation/drug effects , Humans , Models, Molecular , Structure-Activity Relationship , Thiazoles/chemistry , Thiazoles/pharmacology
2.
Biol Pharm Bull ; 38(1): 30-8, 2015.
Article in English | MEDLINE | ID: mdl-25744455

ABSTRACT

Previously, we reported that cationic nanoparticles (NP) composed of diamine-type cholesteryl-3-carboxamide (OH-Chol, N-(2-(2-hydroxyethylamino)ethyl)cholesteryl-3-carboxamide) and Tween 80 could deliver small interfering RNA (siRNA) with high transfection efficiency into tumor cells. In this study, we synthesized new diamine-type cationic cholesteryl carbamate (OH-C-Chol, cholesteryl (2-((2-hydroxyethyl)amino)ethyl)carbamate) and triamine-type carbamate (OH-NC-Chol, cholesteryl (2-((2-((2-hydroxyethyl)amino)ethyl)amino)ethyl)carbamate), and prepared cationic nanoparticles composed of OH-C-Chol or OH-NC-Chol with Tween 80 (NP-C and NP-NC, respectively), as well as cationic liposomes composed of OH-C-Chol or OH-NC-Chol with 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE) (LP-C and LP-NC, respectively) for evaluation of their possible use as siRNA delivery vectors. LP-C and LP-NC/siRNA complexes (lipoplexes) exhibited larger gene silencing effects than NP-C and NP-NC/siRNA complexes (nanoplexes), respectively, in human breast tumor MCF-7 cells, although the NP-C nanoplex showed high association with the cells. In particular, LP-NC lipoplex could induce strong gene suppression, even at a concentration of 5 nM siRNA. From these results, cationic liposomes composed of OH-NC-Chol and DOPE may have potential as gene vectors for siRNA transfection to tumor cells.


Subject(s)
Cholesterol/analogs & derivatives , Cholesterol/chemistry , Nanoparticles/chemistry , RNA, Small Interfering/chemistry , Animals , Carbamates/chemistry , Female , Humans , Liposomes , Luciferases, Firefly/genetics , MCF-7 Cells , Mice, Inbred BALB C , Nanoparticles/administration & dosage , Neoplasms/metabolism , Phosphatidylethanolamines/chemistry , Polysorbates/chemistry , RNA, Small Interfering/administration & dosage
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