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Styrylquinazoline derivatives as HIV-1 integrase inhibitors
Jae Yeol Lee1, Jang Hyun Park, Sook Ja Lee
1Medicinal Chemistry Research Center, Korea Institute of Science & Technology, Cheongryang, Seoul, Korea. yslee@kist.re.kr
Archiv Der Pharmazie
|September 5, 2002
Abstract:
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).