synthesis of quinolin-2-one alkaloid derivatives and their inhibitory activities against hiv-1 reverse transcriptasequinolin-2-one生物碱衍生物的合成及其对hiv - 1逆转录酶抑制活动.pdf

Molecules 2011, 16, 7649-7661; doi:10.3390/molecule OPEN ACCESS molecules ISSN 1420-3049 /journal/molecules Article Synthesis of Quinolin-2-one Alkaloid Derivatives and Their Inhibitory Activities against HIV-1 Reverse Transcriptase Pi Cheng 1,3,*, Qiong Gu 2, Wei Liu 1, Jian-Feng Zou 1, Yang-Yong Ou 3, Zhong-Yong Luo 3 and Jian-Guo Zeng 1,3,* 1 National Research Center of Engineering Technology For Utilization of Functional Ingredients From Botanicals, College of Horticulture and Landscape Architecture, Hunan Agricultural University, Changsha 410128, Hunan, China; E-Mails: lwhncs618@163.com (W.L.); zoujf2005@163.com (J.-F.Z.) 2 School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou 510006, Guangdong, China; E-Mail: guqiong@ (Q.G.) 3 Hunan Engineering Research Center of Botanical Extract, Changsha410128, Hunan, China; E-Mails: oyy713@163.com (Y.-Y.O.); zhongyongluo@ (Z.-Y.L.) * Authors to whom correspondence should be addressed; E-Mails: picheng55@126.com (P.C.); ginkgo@ (J.-G.Z.); Tel.: +86-731-8468-6560; Fax: +86-731-8468-6560. Received: 16 June 2011; in revised form: 4 August 2011 / Accepted: 20 August 2011 / Published: 7 September 2011 Abstract: Based on an established common pharmacophore of HIV-1 non-nucleoside reverse transcriptase inhibitors (NNTTIs), a series of quinolin-2-one derivatives were synthesized and assayed for their in vitro activities against HIV-1 reverse transcriptase (RT) for the first time. Some of the tested compounds were active against HIV-1 RT.