Styrylquinazoline derivatives as HIV-1 integrase inhibitors.
Styrylquinazoline derivatives were prepared by Perkin condensation and evaluated for inhibitory activity against HIV-1 integrase. Among them, compound 5c containing a free catechol ring was the most potent (IC(50)=0.8 +/- 1.9 microM)and showed 6-fold more potency than the corresponding styrylquinoline compound (IC(50) = 130.7 +/- 8.6 microM).
Lee
Jae Yeol
JY
Medicinal Chemistry Research Center, Korea Institute of Science & Technology, Cheongryang, Seoul, Korea. yslee@kist.re.kr
Park
Jang Hyun
JH
Lee
Sook Ja
SJ
Park
Hokoon
H
Lee
Yong Sup
YS
D019428:HIV Integrase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D015497:HIV-1 / Q000201:enzymology*; D006801:Humans; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D009841:Oligonucleotides / Q000737:chemistry; D011799:Quinazolines / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D019428:HIV Integrase Inhibitors; D007202:Indicators and Reagents; D009841:Oligonucleotides; D011799:Quinazolines