In this work, iminothiazolidin-4-one derivatives were explored as selective GSK-3β inhibitors. Molecular docking analysis was carried to design a series of compounds, which were synthesized using substituted thiourea, 2-bromoacetophenones and benzaldehydes. Out of the twenty five compounds synthesized during this work, the in vitro evaluation against GSK-3 led to the identification of nine compounds with activity in lower nano-molar range (2–85 nM). Further, in vitro evaluation against CDK-2 showed five compounds to be selective towards GSK-3
Abstract: Exploring the affinity-pocket binding moiety of a 2-aminothiazole (S)-proline-amide-urea s...
An in silico screening procedure was performed to select new inhibitors of glycogen synthase kinase ...
Abstract: In order to discover novel MEK inhibitors, a series of 3-(benzothiazol-2-yl) coumarin deri...
Compound 5 was selected from our in-house library as a suitable starting point for the rational desi...
4 p.-4 fig.-1 tab.Glycogen synthase kinase 3 (GSK-3) has become known for its multifactorial involve...
A series of isoxazol-indolin-2-one was designed for GSK-3β inhibitors as novel anticancer agents bas...
Compound 5 was selected from our in-house library as a suitable starting point for the rational desi...
In this PhD thesis, I have focused my attention on drug design, chemical optimization and biological...
Glycogen synthase kinase 3 (GSK-3) is a serine/threonine protein kinase that mediates the addition o...
Glycogen Synthase Kinase 3-\u3b2 (GSK-3\u3b2) and Casein Kinase 1-\u3b4 (CK-1\u3b4) are both highly ...
International audienceAn efficient synthetic strategy was developed to modulate the structure of the...
This thesis describes the synthesis and biological evaluation of some medicinally important hybrid c...
For the first time, the in silico design, screening, and in vitro validation of potent GSK-3β type-I...
A series of novel 3-benzisoxazolyl-4-indolyl-maleimides were synthesized and evaluated for their GSK...
Background: Cancer is a major cause of death all over the globe. Controlling cell division byinhibit...
Abstract: Exploring the affinity-pocket binding moiety of a 2-aminothiazole (S)-proline-amide-urea s...
An in silico screening procedure was performed to select new inhibitors of glycogen synthase kinase ...
Abstract: In order to discover novel MEK inhibitors, a series of 3-(benzothiazol-2-yl) coumarin deri...
Compound 5 was selected from our in-house library as a suitable starting point for the rational desi...
4 p.-4 fig.-1 tab.Glycogen synthase kinase 3 (GSK-3) has become known for its multifactorial involve...
A series of isoxazol-indolin-2-one was designed for GSK-3β inhibitors as novel anticancer agents bas...
Compound 5 was selected from our in-house library as a suitable starting point for the rational desi...
In this PhD thesis, I have focused my attention on drug design, chemical optimization and biological...
Glycogen synthase kinase 3 (GSK-3) is a serine/threonine protein kinase that mediates the addition o...
Glycogen Synthase Kinase 3-\u3b2 (GSK-3\u3b2) and Casein Kinase 1-\u3b4 (CK-1\u3b4) are both highly ...
International audienceAn efficient synthetic strategy was developed to modulate the structure of the...
This thesis describes the synthesis and biological evaluation of some medicinally important hybrid c...
For the first time, the in silico design, screening, and in vitro validation of potent GSK-3β type-I...
A series of novel 3-benzisoxazolyl-4-indolyl-maleimides were synthesized and evaluated for their GSK...
Background: Cancer is a major cause of death all over the globe. Controlling cell division byinhibit...
Abstract: Exploring the affinity-pocket binding moiety of a 2-aminothiazole (S)-proline-amide-urea s...
An in silico screening procedure was performed to select new inhibitors of glycogen synthase kinase ...
Abstract: In order to discover novel MEK inhibitors, a series of 3-(benzothiazol-2-yl) coumarin deri...