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Quinazoline antifolate thymidylate synthase inhibitors: heterocyclic benzoyl ring modifications.
The synthesis is described of a series of C2-methyl-N10-alkylquinazoline-based antifolates in which the p-aminobenzoate ring is replaced by the heterocycles thiophene, thiazole, thiadiazole,Expand
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Quinazoline antifolate thymidylate synthase inhibitors: alkyl, substituted alkyl, and aryl substituents in the C2 position.
Modification of the potent thymidylate synthase (TS) inhibitor N-[4-[N-[(2-amino-3,4-dihydro-4-oxo-6-quinazolinyl)methyl]-N-prop-2- ynylamino]benzoyl]-L-glutamic acid (1a) has led to the synthesis ofExpand
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‘Chords of freedom’: Commemoration, ritual and British transatlantic slavery
CONTENTS List of illustrations Acknowledgements Introduction One Frames of Remembrance: Benjamin Robert Haydon and The Anti-Slavery Convention, 1840 Two Literary Memorials: Clarkson's History and TheExpand
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Apparent role of melatonin and prolactin in initiating winter fur growth in mink.
A study was conducted to determine the effects of exogenous melatonin and bromocriptine (CB-154), an inhibitor of prolactin synthesis and secretion, on the induction of winter fur growth in mink.Expand
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Balancing hERG affinity and absorption in the discovery of AZD5672, an orally active CCR5 antagonist for the treatment of rheumatoid arthritis.
Modifications to a series of potent and selective substituted 1-(3,3-diphenylpropyl)-piperidine phenylacetamide CCR5 antagonists were explored with the aim of reducing affinity at the hERG cardiacExpand
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Modulators of the human CCR5 receptor. Part 2: SAR of substituted 1-(3,3-diphenylpropyl)-piperidinyl phenylacetamides.
SAR and DMPK studies led to the identification of substituted N-alkyl-N-[1-(3,3-diphenylpropyl)piperidin-4-yl]-2-phenylacetamides as potent and orally bioavailable ligands for the human CCR5Expand
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Quinazoline antifolate thymidylate synthase inhibitors: benzoyl ring modifications in the C2-methyl series.
The synthesis of nine new 2-methyl-10-propargylquinazoline antifolates with substituents in the p-aminobenzoyl ring is described. In general the synthetic route involved the coupling of theExpand
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Modulators of the human CCR5 receptor. Part 3: SAR of substituted 1-[3-(4-methanesulfonylphenyl)-3-phenylpropyl]-piperidinyl phenylacetamides.
SAR and PK studies led to the identification of N-(1-{(3R)-3-(3,5-difluorophenyl)-3-[4-methanesulfonylphenyl] propyl}piperidin-4-yl)-N-ethyl-2-[4-methanesulfonylphenyl]acetamide as a highly potentExpand
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VLSI and rule-based systems
TLDR
Many AI applications today employ some form of if-then rule-based programming. Expand
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A High-Level Recognizer for Schematic Diagrams
TLDR
This recognizer uses high-level knowledge stored in a global, modifiable database. Expand
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