Structure-activity relationship of pyrrolyl diketo acid derivatives as dual inhibitors of HIV-1 integrase and reverse transcriptase ribonuclease H domain

Journal of Medicinal Chemistry

Volumn 58, Issue 4, 2015, Pages 1915-1928

  Cuzzucoli Crucitti, Giuliana ^a   Métifiot, Mathieu ^b   Pescatori, Luca ^a   Messore, Antonella ^a   Madia, Valentina Noemi ^a   Pupo, Giovanni ^a   Saccoliti, Francesco ^a   Scipione, Luigi ^a   Tortorella, Silvano ^a   Esposito, Francesca ^c   Corona, Angela ^c   Cadeddu, Marta ^c   Marchand, Christophe ^b   Pommier, Yves ^b   Tramontano, Enzo ^c   Costi, Roberta ^a   Di Santo, Roberto ^a  

^a SAPIENZA UNIVERSITY OF ROME   (Italy)

^b NATIONAL CANCER INSTITUTE   (United States)

^c UNIVERSITY OF CAGLIARI   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

1 [1 (4 FLUOROBENZOYL) 1H PYRROL 2 YL] 2 HYDROXY 3 (1H 1,2,4 TRIAZOL 3 YL)PROP 2 EN 1 ONE; 2 AMINO 4 [1 (4 FLUOROBENZOYL) 4 PHENYL 1H PYRROL 3 YL] 4 OXOHEXA 2,5 DIENOIC ACID; 4 [1 (4 FLUOROBENZOYL) 1H PYRROL 2 YL] 2 HYDROXY 4 OXOHEXA 2,5 DIENOIC ACID; 4 [1 (4 FLUOROBENZYL) 1H PYRROL 3 YL] 2 HYDROXY 4 OXOBUT 2 ENOIC ACID; 4 [1 (4 FLUOROBENZYL) 4 PHENYL 1H PYRROL 3 YL] 2 HYDROXY 3 METHYL 4 OXOBUT 2 ENOIC ACID; 4 [1 (4 FLUOROBENZYL) 4 PHENYL 1H PYRROL 3 YL] 2 HYDROXY 4 OXOBUT 2 ENOIC ACID; 6 [1 (4 FLUOROBENZOYL) 1H PYRROL 3 YL] 2 HYDROXY 4 OXOHEXA 2,5 DIENOIC ACID; 6 [1 (4 FLUOROBENZOYL) 4 PHENYL 1H PYRROL 2 YL] 2 HYDROXY 4 OXOHEXA 2,5 DIENOIC ACID; 6 [1 (4 FLUOROBENZOYL) 4 PHENYL 1H PYRROL 3 YL] 2 HYDROXY 4 OXOHEXA 2,5 DIENOIC ACID; 6 [1 BENZYL 4 (4 FLUOROBENZOYL) 1H PYRROL 2 YL] 2 HYDROXY 4 OXOHEXA 2,5 DIENOIC ACID; 6 [4 (4 FLUOROBENZOYL) 1 METHYL 1H PYRROL 2 YL] 2 HYDROXY 4 OXOHEXA 2,5 DIENOIC ACID; 6 [4 (4 FLUOROBENZOYL) 1 PHENYL 1H PYRROL 2 YL] 2 HYDROXY 4 OXOHEXA 2,5 DIENOIC ACID; ANTI HUMAN IMMUNODEFICIENCY VIRUS AGENT; ESTER 6 [1 (4 FLUOROBENZYL) 1H PYRROL 3 YL] 2 HYDROXY 4 OXOHEXA 2,5 DIENOATE; ETHYL 2 AMINO 4 [1 (4 FLUOROBENZYL) 4 PHENYL 1H PYRROL 3 YL] 4 OXOBUT 2 ENOATE; ETHYL 4 [1 (4 FLUOROBENZYL) 1H PYRROL 2 YL] 2 HYDROXY 4 OXOHEXA 2,5 DIENOATE; ETHYL 4 [1 (4 FLUOROBENZYL) 1H PYRROL 3 YL] 2 HYDROXY 4 OXOBUT 2 ENOATE; ETHYL 4 [1 (4 FLUOROBENZYL) 4 PHENYL 1H PYRROL 2 YL] 2 HYDROXY 4 OXOHEXA 2,5 DIENOATE; ETHYL 4 [1 (4 FLUOROBENZYL) 4 PHENYL 1H PYRROL 3 YL] 2 HYDROXY 3 METHYL 4 OXOBUT 2 ENOATE; ETHYL 4 [1 (4 FLUOROBENZYL) 4 PHENYL 1H PYRROL 3 YL] 2 HYDROXY 4 OXOBUT 2 ENOATE; ETHYL 6 [1 (4 FLUOROBENZYL) 4 PHENYL 1H PYRROL 2 YL] 2 HYDROXY 4 OXOHEXA 2,5 DIENOATE; ETHYL 6 [1 (4 FLUOROBENZYL) 4 PHENYL 1H PYRROL 3 YL] 2 HYDROXY 4 OXOHEXA 2,5 DIENOATE; ETHYL 6 [1 BENZYL) 4 (4 FLUOROBENZOYL) 1H PYRROL 2 YL] 2 HYDROXY 4 OXOBUT 2,5 DIENOATE; ETHYL 6 [4 (4 FLUOROBENZYL) 1 METHYL 1H PYRROL 2 YL] 2 HYDROXY 4 OXOHEXA 2,5 DIENOATE; ETHYL 6 [4 (4 FLUOROBENZYL) 1 PHENYL 1H PYRROL 2 YL] 2 HYDROXY 4 OXOHEXA 2,5 DIENOATE; INTEGRASE INHIBITOR; RNA DIRECTED DNA POLYMERASE INHIBITOR; UNCLASSIFIED DRUG; INTEGRASE; P31 INTEGRASE PROTEIN, HUMAN IMMUNODEFICIENCY VIRUS 1; PYRROLE DERIVATIVE; RIBONUCLEASE H; RNA DIRECTED DNA POLYMERASE;

ANTIVIRAL ACTIVITY; ARTICLE; BIOLOGICAL ACTIVITY; CHEMOTHERAPY; CYTOTOXICITY; DRUG IDENTIFICATION; DRUG POTENCY; DRUG SCREENING; DRUG SYNTHESIS; PROTEIN DOMAIN; STRUCTURE ACTIVITY RELATION; ANTAGONISTS AND INHIBITORS; CHEMICAL STRUCTURE; CHEMISTRY; DOSE RESPONSE; DRUG EFFECTS; ENZYMOLOGY; HUMAN IMMUNODEFICIENCY VIRUS; METABOLISM; MICROBIAL SENSITIVITY TEST; PROTEIN TERTIARY STRUCTURE; SYNTHESIS; VIRUS REPLICATION;

DOSE-RESPONSE RELATIONSHIP, DRUG; HIV; HIV INTEGRASE; HIV INTEGRASE INHIBITORS; HIV REVERSE TRANSCRIPTASE; MICROBIAL SENSITIVITY TESTS; MOLECULAR STRUCTURE; PROTEIN STRUCTURE, TERTIARY; PYRROLES; REVERSE TRANSCRIPTASE INHIBITORS; RIBONUCLEASE H; STRUCTURE-ACTIVITY RELATIONSHIP; VIRUS REPLICATION;

EID: 84923882396     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm501799k     Document Type: Article

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