[Design, synthesis and evaluation of novel 2H-1, 4-benzodiazepine-2-ones as inhibitors of HIV-1 transcription].
Publication
, Journal Article
Tang, Y-B; Zhang, C-M; Fang, C; Hu, C; Huang, L; Chen, C-H; Xiao, Z-Y
Published in: Yao Xue Xue Bao
June 2011
HIV-1 trans-activator of transcription (Tat) plays a critical role in HIV-1 transcription. Based on the beta-turn motif present in HIV-1 Tat, a series of novel benzodiazepine analogs were designed as beta-turn mimetics and prepared from p-chloro-nitrobenzene/2-phenylacetonitrile, p-toluidine/benzoyl chloride, or (Z)-7-nitro-5-phenyl-1H-benzo[e][1, 4]diazepin-2(3H)-one (nitrazepam) through different synthetic routes. Preliminary biological evaluation indicated that compound 30 exhibited inhibitory activity on HIV-1 tat-mediated LTR transcription with EC50 of 25.0 micromol x L(-1) and showed no obvious cytotoxic effects on TZM-BI cells under the concentration of 100 micromol x L(-1).
Duke Scholars
Published In
Yao Xue Xue Bao
ISSN
0513-4870
Publication Date
June 2011
Volume
46
Issue
6
Start / End Page
688 / 694
Location
China
Related Subject Headings
- tat Gene Products, Human Immunodeficiency Virus
- Transcription, Genetic
- Pharmacology & Pharmacy
- Humans
- HIV-1
- HIV Long Terminal Repeat
- Cell Line, Tumor
- Benzodiazepinones
Citation
APA
Chicago
ICMJE
MLA
NLM
Tang, Y.-B., Zhang, C.-M., Fang, C., Hu, C., Huang, L., Chen, C.-H., & Xiao, Z.-Y. (2011). [Design, synthesis and evaluation of novel 2H-1, 4-benzodiazepine-2-ones as inhibitors of HIV-1 transcription]. Yao Xue Xue Bao, 46(6), 688–694.
Tang, Yan-Boi, Chuan-Ming Zhang, Cheng Fang, Chun Hu, Li Huang, Chin-Ho Chen, and Zhi-Yan Xiao. “[Design, synthesis and evaluation of novel 2H-1, 4-benzodiazepine-2-ones as inhibitors of HIV-1 transcription].” Yao Xue Xue Bao 46, no. 6 (June 2011): 688–94.
Tang Y-B, Zhang C-M, Fang C, Hu C, Huang L, Chen C-H, et al. [Design, synthesis and evaluation of novel 2H-1, 4-benzodiazepine-2-ones as inhibitors of HIV-1 transcription]. Yao Xue Xue Bao. 2011 Jun;46(6):688–94.
Tang, Yan-Boi, et al. “[Design, synthesis and evaluation of novel 2H-1, 4-benzodiazepine-2-ones as inhibitors of HIV-1 transcription].” Yao Xue Xue Bao, vol. 46, no. 6, June 2011, pp. 688–94.
Tang Y-B, Zhang C-M, Fang C, Hu C, Huang L, Chen C-H, Xiao Z-Y. [Design, synthesis and evaluation of novel 2H-1, 4-benzodiazepine-2-ones as inhibitors of HIV-1 transcription]. Yao Xue Xue Bao. 2011 Jun;46(6):688–694.
Published In
Yao Xue Xue Bao
ISSN
0513-4870
Publication Date
June 2011
Volume
46
Issue
6
Start / End Page
688 / 694
Location
China
Related Subject Headings
- tat Gene Products, Human Immunodeficiency Virus
- Transcription, Genetic
- Pharmacology & Pharmacy
- Humans
- HIV-1
- HIV Long Terminal Repeat
- Cell Line, Tumor
- Benzodiazepinones