Design and Synthesis of ALK5 Inhibitors
Language: English
Published by LAP LAMBERT Academic Publishing Dez 2015, 2015
- Softcover
- New
Seller: BuchWeltWeit Ludwig Meier e.K., Bergisch Gladbach, GermanyBuchWeltWeit Ludwig Meier e.K.
AbeBooks seller since January 11, 2012
Condition: New
£ 47.77
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Add to basketItem description from seller
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.…
Seller Inventory # 9783659815430
- Title
- Design and Synthesis of ALK5 Inhibitors
- Author
- Harun Patel
- Publisher
- LAP LAMBERT Academic Publishing Dez 2015
- Publication year
- 2015
- Condition
- Neu
- Binding
- Taschenbuch
- Language
- English
- ISBN 10
- 3659815438
- ISBN 13
- 9783659815430
- Item weight
- 167 grams
- Dimensions
- 220x150x6 mm
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About the Author
"About the title" may belong to another edition of this title.
BuchWeltWeit Ludwig Meier e.K.
Bergisch Gladbach, Germany
AbeBooks seller since January 11, 2012
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BuchWeltWeit Ludwig Meier e.K.
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