Design, Synthesis and Evaluation of Small Molecules as ALK5 Inhibitors - Couverture souple

Karpoormath, Rajshekhar ; Noolvi, Malleshappa N.; Patel, Harun M.

9783659479922: Design, Synthesis and Evaluation of Small Molecules as ALK5 Inhibitors

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ISBN 10 : 3659479926 ISBN 13 : 9783659479922

Editeur : LAP LAMBERT Academic Publishing, 2018

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A new series of imidazo[2,1-b][1,3,4]thiadiazoles were synthesized as transforming growth factor-β (TGF- β) type I receptor (also known as activin receptor-like kinase 5 or ALK5) inhibitors. These compounds were evaluated for their ALK5 inhibitory activity in an enzyme assay and their TGF-β -induced Smad2/3 phosphorylation inhibitory activity in a cell-based assay. One of the compound from this series displayed prominent ALK5 inhibition (IC50 = 0.0012 �M) and elective inhibition (91%) against the P38α kinase at 10 �M. The binding mode of this compound by XP docking studies showed that it ﬁts well into the active site cavity of ALK5 by forming broad and tight interactions. Lipinski’s rule and in silico ADME pharmacokinetic parameters are within the acceptable range defined for human use, thereby indicating their potential as a drug-like molecules.

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�diteur: LAP LAMBERT Academic Publishing
Date d'�dition: 2018
Langue: anglais
ISBN 10: 3659479926
ISBN 13: 9783659479922
Reliure: Broch�
Nombre de pages: 52
Coordonn�es du fabricant: non disponible
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Design, Synthesis and Evaluation of Small Molecules as ALK5 Inhibitors

Rajshekhar Karpoormath

Edit� par LAP LAMBERT Academic Publishing Nov 2018, 2018

ISBN 10 : 3659479926 ISBN 13 : 9783659479922

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Taschenbuch. Etat : Neu. This item is printed on demand - it takes 3-4 days longer - Neuware -A new series of imidazo[2,1-b][1,3,4]thiadiazoles were synthesized as transforming growth factor-beta (TGF- beta) type I receptor (also known as activin receptor-like kinase 5 or ALK5) inhibitors. These compounds were evaluated for their ALK5 inhibitory activity in an enzyme assay and their TGF-beta -induced Smad2/3 phosphorylation inhibitory activity in a cell-based assay. One of the compound from this series displayed prominent ALK5 inhibition (IC50 = 0.0012 �M) and elective inhibition (91%) against the P38 kinase at 10 �M. The binding mode of this compound by XP docking studies showed that it fits well into the active site cavity of ALK5 by forming broad and tight interactions. Lipinski's rule and in silico ADME pharmacokinetic parameters are within the acceptable range defined for human use, thereby indicating their potential as a drug-like molecules. 52 pp. Englisch. N� de r�f. du vendeur 9783659479922

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Design, Synthesis and Evaluation of Small Molecules as ALK5 Inhibitors

Karpoormath, Rajshekhar/ Noolvi, Malleshappa N./ Patel, Harun M.

Edit� par LAP LAMBERT Academic Publishing, 2018

ISBN 10 : 3659479926 ISBN 13 : 9783659479922

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Paperback. Etat : Brand New. 52 pages. 8.66x5.91x0.12 inches. In Stock. N� de r�f. du vendeur 3659479926

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Design, Synthesis and Evaluation of Small Molecules as ALK5 Inhibitors

Rajshekhar Karpoormath|Malleshappa N. Noolvi|Harun M. Patel

Edit� par LAP LAMBERT Academic Publishing, 2018

ISBN 10 : 3659479926 ISBN 13 : 9783659479922

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Kartoniert / Broschiert. Etat : New. Dieser Artikel ist ein Print on Demand Artikel und wird nach Ihrer Bestellung fuer Sie gedruckt. Autor/Autorin: Karpoormath RajshekharDr. R. Karpoormath is professor at the faculty in the Dis. of Pharmaceutical Sciences, University of KwaZulu-Natal, Durban, South Africa. His research interests are: target based drug design (HIV, Cancer and TB). N� de r�f. du vendeur 260575183

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Design, Synthesis and Evaluation of Small Molecules as ALK5 Inhibitors

Rajshekhar Karpoormath

Edit� par LAP LAMBERT Academic Publishing Nov 2018, 2018

ISBN 10 : 3659479926 ISBN 13 : 9783659479922

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Taschenbuch. Etat : Neu. This item is printed on demand - Print on Demand Titel. Neuware -A new series of imidazo[2,1-b][1,3,4]thiadiazoles were synthesized as transforming growth factor-� (TGF- �) type I receptor (also known as activin receptor-like kinase 5 or ALK5) inhibitors. These compounds were evaluated for their ALK5 inhibitory activity in an enzyme assay and their TGF-� -induced Smad2/3 phosphorylation inhibitory activity in a cell-based assay. One of the compound from this series displayed prominent ALK5 inhibition (IC50 = 0.0012 �M) and elective inhibition (91%) against the P38� kinase at 10 �M. The binding mode of this compound by XP docking studies showed that it �ts well into the active site cavity of ALK5 by forming broad and tight interactions. Lipinski's rule and in silico ADME pharmacokinetic parameters are within the acceptable range defined for human use, thereby indicating their potential as a drug-like molecules.VDM Verlag, Dudweiler Landstra�e 99, 66123 Saarbr�cken 52 pp. Englisch. N� de r�f. du vendeur 9783659479922

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Design, Synthesis and Evaluation of Small Molecules as ALK5 Inhibitors

Rajshekhar Karpoormath

Edit� par LAP LAMBERT Academic Publishing, 2018

ISBN 10 : 3659479926 ISBN 13 : 9783659479922

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Taschenbuch. Etat : Neu. nach der Bestellung gedruckt Neuware - Printed after ordering - A new series of imidazo[2,1-b][1,3,4]thiadiazoles were synthesized as transforming growth factor-beta (TGF- beta) type I receptor (also known as activin receptor-like kinase 5 or ALK5) inhibitors. These compounds were evaluated for their ALK5 inhibitory activity in an enzyme assay and their TGF-beta -induced Smad2/3 phosphorylation inhibitory activity in a cell-based assay. One of the compound from this series displayed prominent ALK5 inhibition (IC50 = 0.0012 �M) and elective inhibition (91%) against the P38 kinase at 10 �M. The binding mode of this compound by XP docking studies showed that it fits well into the active site cavity of ALK5 by forming broad and tight interactions. Lipinski's rule and in silico ADME pharmacokinetic parameters are within the acceptable range defined for human use, thereby indicating their potential as a drug-like molecules. N� de r�f. du vendeur 9783659479922

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