中国科技论文在线

上传时间

2004年12月28日

【期刊论文】Anti-AIDS Agents. Part 36:1 17-Carboxylated Steroids as Potential Anti-HIV Agents

夏鹏， Peng Xia， a， †， Zheng-Yu Yang， b， Yi Xia， Yun-Qing Zheng， L. Mark Cosentino c and Kuo-Hsiung Lee b*

Bioorganic & Medicinal Chemistry 7(1999)1907-1911，-0001，（）：

-1年11月30日

摘要

ith EC50 and therapeutic index values of 0.8μM and 300, respectively.

28浏览
0点赞
0收藏
0分享
330下载
0

引用

上传时间

2004年12月28日

【期刊论文】Synthesis and Bioactivity of 4,10-Dimethyl-pyridino[2,3-h]quinolin-2(1H)-one-9-carboxylic Acid and Its Esters

夏鹏， Qian Zhang， a， Ying Chen， Yun Qing Zheng， Peng Xia， *， Yi Xia， b， Zheng Yu Yang， Kenneth F. Bastow， Susan L. Morris-Natschke b and Kuo-Hsiung Lee b

Bioorganic & Medicinal Chemistry 11(2003)1031-1034，-0001，（）：

-1年11月30日

摘要

4, 10-Dimethyl-pyridino[2,3-h]quinolin-2(1H)-one-9-carboxylic acid (1) was synthesized by a new approach via the key intermediate 7-[1-aza-2-(dimethylamino) vinyl]-4-methylquinolin-2(1H)-one (4). Compound 1 and its esters were evaluated in cytotoxicity and anti-HIV assays. The 9-carboxyl (1s)-endo-(-)-borneol ester (9) showed marginal cytotoxic activity in CAK1-1, HOS, KB, and HCT-8 cells.

42浏览
0点赞
0收藏
0分享
264下载
0

引用

上传时间

2004年12月28日

【期刊论文】Anti-AIDS agents. Part 56: Synthesis and anti-HIV activity of 7-thia-di-O-(-)-camphanoyl-(+)-cis-khellactone (7-thia-DCK) analogs☆

夏鹏， Ying Chen， a， Qian Zhang， Beina Zhang， Peng Xia， *， Yi Xia， b， Zheng-Yu Yang， Nicole Kilgore， c， Carl Wild， Susan L. Morris-Natschke b and Kuo-Hsiung Lee b

Bioorganic & Medicinal Chemistry 12(2004)6383-6387，-0001，（）：

-1年11月30日

摘要

Two thia-DCK analogs (3a, b) were synthesized and evaluated for inhibition of HIV-1 replication in H9 lymphocytes. Compound 3a showed potent anti-HIV activity with an EC50 value of 0.14μM and a therapeutic index of 1110. However, the corresponding 6-tert-butyl-substituted compound (3b) showed no suppression. The bioassay results indicated that thia-DCK analogs merit attention as potential HIV-1 inhibitors.

42浏览
0点赞
0收藏
0分享
233下载
0

引用

上传时间

2004年12月28日

【期刊论文】Anti-AIDS Agents Part 41:† Synthesis and Anti-HIV Activity of 3', 4'-di-o-(-)-camphanoyl-(+)-cis-khellactone (DCK) Lactam Analogues

夏鹏， Zheng-Yu Yang， a， Yi Xia， Peng Xia， Arnold Brossi， L. Mark Cosentino b and Kuo-Hsiung Lee a， *

Bioorganic & Medicinal Chemistry Letters 10(2000)1003-1005，-0001，（）：

-1年11月30日

摘要

DCK lactam analogues were synthesized and evaluated for anti-HIV activity against HIV-1 replication in H9 lymphocyte cells. 4-Methyl-DCK lactam (11a) exhibited potent anti-HIV activity with EC50 and therapeutic index values of 0.00024μM and 119,333, respectively.

41浏览
0点赞
0收藏
0分享
184下载
0

引用

上传时间

2004年12月28日

【期刊论文】ANTI-AIDS AGENTS 31.1 SYNTHESIS AND ANTI-HIV ACTIVITY OF 4-SUBSTITUTED 3', 4'-DI-O-(-)-CAMPHANOYL-(+)-Cis-KHELLACTONE (DCK) THIOLACTONE ANALOGS

夏鹏， Zheng-Yu Yang， a， Yi Xia， Peng Xia， L. Mark Cosentino， b and Kuo-Hsiung Lee a*

Bioorganic & Medicinal Chemistry Letters 8(1998)1483-1486，-0001，（）：

-1年11月30日

摘要

Four DCK-thiolactone analogs (3-6) Were synthesized asymmetrically and evaluated for anti-HIV activity against HIV-1 replication in H9 lymphocyte cells. Based on the functionality on the thiolactone-coumarin nucleus, activity was in the order: methyl＞H＞propyl＞benzyl. 4-Methyl-3',4'-di-O-(-)-camphanoyl-(+)-cis-khelthiolactone (4) exhibited extremely potent anti-HIV activity with EC50 and therapeutic index values of 0.00718μM and＞21,300, respectively.

37浏览
0点赞
0收藏
0分享
175下载
0

引用