Synopsis
A new series of imidazo[2,1-b][1,3,4]thiadiazoles 5(a-g), 6(a-g), 9(a-i) and 12(a-h) were synthesized. Among them, 23 compounds 5a, 5b, 5e, 5d, 5f, 5g, 6a, 6b, 6c, 6d, 6e, 9b, 9d, 9f, 9g, 9h, 9i, 12b, 12c, 12d, 12e, 12g, and 12h were evaluated at National Cancer Institute for single dose in vitro primary cytotoxicity assay. Compound 5b, 5e, 6c, 6d, 6e, 12c, 12d and 12e were further screened for 5-log dose molar range as they have shown prominent cell growth inhibition at 10-5 M concentration against variety of cell lines. Compound 5e shows significant inhibition against Leukemia HL-60 cell line with GI50 of 0.0285 µM and highest selectivity towards the Leukemic Cancer cell line (selectivity ratio of 7.96) it also shows prominent ALK5 inhibition (IC50 = 0.0263 µM) and elective inhibition (91%) against KDR at10 µM. The binding mode of compound 5e by SP docking studies shows 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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Design and Synthesis of ALK5 Inhibitors
Edité par
LAP LAMBERT Academic Publishing Dez 2015, 2015
ISBN 10 : 3659815438
ISBN 13 : 9783659815430
Neuf
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Vendeur : BuchWeltWeit Ludwig Meier e.K., Bergisch Gladbach, Allemagne
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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 5(a-g), 6(a-g), 9(a-i) and 12(a-h) were synthesized. Among them, 23 compounds 5a, 5b, 5e, 5d, 5f, 5g, 6a, 6b, 6c, 6d, 6e, 9b, 9d, 9f, 9g, 9h, 9i, 12b, 12c, 12d, 12e, 12g, and 12h were evaluated at National Cancer Institute for single dose in vitro primary cytotoxicity assay. Compound 5b, 5e, 6c, 6d, 6e, 12c, 12d and 12e were further screened for 5-log dose molar range as they have shown prominent cell growth inhibition at 10-5 M concentration against variety of cell lines. Compound 5e shows significant inhibition against Leukemia HL-60 cell line with GI50 of 0.0285 µM and highest selectivity towards the Leukemic Cancer cell line (selectivity ratio of 7.96) it also shows prominent ALK5 inhibition (IC50 = 0.0263 µM) and elective inhibition (91%) against KDR at10 µM. The binding mode of compound 5e by SP docking studies shows 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. 100 pp. Englisch. N° de réf. du vendeur 9783659815430
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Design and Synthesis of ALK5 Inhibitors
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LAP LAMBERT Academic Publishing, 2015
ISBN 10 : 3659815438
ISBN 13 : 9783659815430
Neuf
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Etat : New. Dieser Artikel ist ein Print on Demand Artikel und wird nach Ihrer Bestellung fuer Sie gedruckt. Autor/Autorin: Patel HarunDr. Harun M. Patel was born on 5th September 1983. He received Gold Medal in graduation and post graduation. Completed his doctoral study at Punjab Technical University-Jalndhar as Young Scientist (DST). Recently completed. N° de réf. du vendeur 158876907
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Design and Synthesis of ALK5 Inhibitors
Edité par
LAP LAMBERT Academic Publishing Dez 2015, 2015
ISBN 10 : 3659815438
ISBN 13 : 9783659815430
Neuf
Taschenbuch
Vendeur : buchversandmimpf2000, Emtmannsberg, BAYE, Allemagne
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Taschenbuch. Etat : Neu. Neuware -A new series of imidazo[2,1-b][1,3,4]thiadiazoles 5(a-g), 6(a-g), 9(a-i) and 12(a-h) were synthesized. Among them, 23 compounds 5a, 5b, 5e, 5d, 5f, 5g, 6a, 6b, 6c, 6d, 6e, 9b, 9d, 9f, 9g, 9h, 9i, 12b, 12c, 12d, 12e, 12g, and 12h were evaluated at National Cancer Institute for single dose in vitro primary cytotoxicity assay. Compound 5b, 5e, 6c, 6d, 6e, 12c, 12d and 12e were further screened for 5-log dose molar range as they have shown prominent cell growth inhibition at 10-5 M concentration against variety of cell lines. Compound 5e shows significant inhibition against Leukemia HL-60 cell line with GI50 of 0.0285 µM and highest selectivity towards the Leukemic Cancer cell line (selectivity ratio of 7.96) it also shows prominent ALK5 inhibition (IC50 = 0.0263 µM) and elective inhibition (91%) against KDR at10 µM. The binding mode of compound 5e by SP docking studies shows 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.Books on Demand GmbH, Überseering 33, 22297 Hamburg 100 pp. Englisch. N° de réf. du vendeur 9783659815430
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Design and Synthesis of ALK5 Inhibitors
Edité par
LAP LAMBERT Academic Publishing, 2015
ISBN 10 : 3659815438
ISBN 13 : 9783659815430
Neuf
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Vendeur : AHA-BUCH GmbH, Einbeck, Allemagne
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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 5(a-g), 6(a-g), 9(a-i) and 12(a-h) were synthesized. Among them, 23 compounds 5a, 5b, 5e, 5d, 5f, 5g, 6a, 6b, 6c, 6d, 6e, 9b, 9d, 9f, 9g, 9h, 9i, 12b, 12c, 12d, 12e, 12g, and 12h were evaluated at National Cancer Institute for single dose in vitro primary cytotoxicity assay. Compound 5b, 5e, 6c, 6d, 6e, 12c, 12d and 12e were further screened for 5-log dose molar range as they have shown prominent cell growth inhibition at 10-5 M concentration against variety of cell lines. Compound 5e shows significant inhibition against Leukemia HL-60 cell line with GI50 of 0.0285 µM and highest selectivity towards the Leukemic Cancer cell line (selectivity ratio of 7.96) it also shows prominent ALK5 inhibition (IC50 = 0.0263 µM) and elective inhibition (91%) against KDR at10 µM. The binding mode of compound 5e by SP docking studies shows 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 réf. du vendeur 9783659815430
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Design and Synthesis of ALK5 Inhibitors
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ISBN 10 : 3659815438
ISBN 13 : 9783659815430
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Taschenbuch. Etat : Neu. Design and Synthesis of ALK5 Inhibitors | Harun Patel (u. a.) | Taschenbuch | 100 S. | Englisch | 2015 | LAP LAMBERT Academic Publishing | EAN 9783659815430 | Verantwortliche Person für die EU: BoD - Books on Demand, In de Tarpen 42, 22848 Norderstedt, info[at]bod[dot]de | Anbieter: preigu. N° de réf. du vendeur 104039030
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Design and Synthesis of ALK5 Inhibitors
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ISBN 13 : 9783659815430
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