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Titolo:
SYNTHESIS OF A NONNUCLEOSIDE REVERSE-TRANSCRIPTASE INHIBITOR IN THE ALKENYLDIARYLMETHANE (ADAM) SERIES WITH OPTIMIZED POTENCY AND THERAPEUTIC INDEX
Autore:
CUSHMAN M; CASIMIROGARCIA A; WILLIAMSON K; RICE WG;
Indirizzi:
PURDUE UNIV,SCH PHARM & PHARMACAL SCI,DEPT MED CHEM & MOL PHARMACOL WLAFAYETTE IN 47907 NCI,LAB ANTIVIRAL DRUG MECHANISMS,SAIC FREDERICK,FREDERICK CANC RES &DEV CTR FREDERICK MD 21702
Titolo Testata:
Bioorganic & medicinal chemistry letters
fascicolo: 2, volume: 8, anno: 1998,
pagine: 195 - 198
SICI:
0960-894X(1998)8:2<195:SOANRI>2.0.ZU;2-X
Fonte:
ISI
Lingua:
ENG
Soggetto:
VIRUS TYPE-1 HIV-1; BIOLOGICAL EVALUATION; SELECTIVE-INHIBITION; DERIVATIVES; NNRTIS; INFECTIONS; RESISTANCE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
17
Recensione:
Indirizzi per estratti:
Citazione:
M. Cushman et al., "SYNTHESIS OF A NONNUCLEOSIDE REVERSE-TRANSCRIPTASE INHIBITOR IN THE ALKENYLDIARYLMETHANE (ADAM) SERIES WITH OPTIMIZED POTENCY AND THERAPEUTIC INDEX", Bioorganic & medicinal chemistry letters, 8(2), 1998, pp. 195-198

Abstract

A novel alkenyldiarylmethane (ADAM) analog has been synthesized with enhanced potency as an anti-HIV agent. The new compound (ADAM II) inhibits the cytopathic effect of HIV-1(RF) in CEM-SS cells with an EC50 of 13 nM, while it shows cytotoxicity with a CC50 of 31.6 mu M, providing a therapeutic index of 2430. ADAM II is a non-nucleoside reverse transcriptase inhibitor, displaying an IC50 of 0.3 mu M with poly(rC) oligo(dG) as the template/primer. (C) 1998 Elsevier Science Ltd. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 30/09/20 alle ore 09:26:52