Literature DB >> 14552777

Synthesis of a highly active new anti-HIV agent 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine.

Kazuhiro Haraguchi1, Shingo Takeda, Hiromichi Tanaka, Takao Nitanda, Masanori Baba, G E Dutschman, Yung-Chi Cheng.   

Abstract

Compounds having methyl, vinyl, and ethynyl groups at the 4'-position of stavudine (d4T: 2',3'-didehydro-3'-deoxythymidine) were synthesized. The compounds were assayed for their ability to inhibit the replication of HIV in cell culture. The 4'-ethynyl analogue (15) was found to be more potent and less toxic than the parent compound stavudine.

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Year:  2003        PMID： 14552777     DOI： 10.1016/j.bmcl.2003.07.009

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  15 in total

1.  Determinants of individual variation in intracellular accumulation of anti-HIV nucleoside analog metabolites.

Authors:  Elijah Paintsil; Ginger E Dutschman; Rong Hu; Susan P Grill; Chuan-Jen Wang; Wing Lam; Fang-Yong Li; Musie Ghebremichael; Veronika Northrup; Yung-Chi Cheng
Journal:  Antimicrob Agents Chemother       Date:  2010-11-15       Impact factor: 5.191

2.  Intracellular metabolism and persistence of the anti-human immunodeficiency virus activity of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel thymidine analog.

Authors:  Elijah Paintsil; Ginger E Dutschman; Rong Hu; Susan P Grill; Wing Lam; Masanori Baba; Hiromichi Tanaka; Yung-Chi Cheng
Journal:  Antimicrob Agents Chemother       Date:  2007-08-27       Impact factor: 5.191

Review 3.  From the chemistry of epoxy-sugar nucleosides to the discovery of anti-HIV agent 4'-ethynylstavudine-Festinavir.

Authors:  Kazuhiro Haraguchi; Shingo Takeda; Yutaka Kubota; Hiroki Kumamoto; Hiromichi Tanaka; Takayuki Hamasaki; Masanori Baba; Elijah Paintsil; Yung-Chi Cheng
Journal:  Curr Pharm Des       Date:  2013       Impact factor: 3.116

4.  Anti-human immunodeficiency virus type 1 activity and resistance profile of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine in vitro.

Authors:  Takao Nitanda; Xin Wang; Hiroki Kumamoto; Kazuhiro Haraguchi; Hiromichi Tanaka; Yung-Chi Cheng; Masanori Baba
Journal:  Antimicrob Agents Chemother       Date:  2005-08       Impact factor: 5.191

5.  The Nucleoside Analog BMS-986001 Shows Greater In Vitro Activity against HIV-2 than against HIV-1.

Authors:  Robert A Smith; Dana N Raugi; Vincent H Wu; Sally S Leong; Kate M Parker; Mariah K Oakes; Papa Salif Sow; Selly Ba; Moussa Seydi; Geoffrey S Gottlieb
Journal:  Antimicrob Agents Chemother       Date:  2015-09-21       Impact factor: 5.191

6.  Anti-human immunodeficiency virus type 1 activity of novel 6-substituted 1-benzyl-3-(3,5-dimethylbenzyl)uracil derivatives.

Authors:  Paula Ordonez; Takayuki Hamasaki; Yohei Isono; Norikazu Sakakibara; Masahiro Ikejiri; Tokumi Maruyama; Masanori Baba
Journal:  Antimicrob Agents Chemother       Date:  2012-01-30       Impact factor: 5.191

7.  Comparison of the phosphorylation of 4'-ethynyl 2',3'-dihydro-3'-deoxythymidine with that of other anti-human immunodeficiency virus thymidine analogs.

Authors:  Chih-Hung Hsu; Rong Hu; Ginger E Dutschman; Guangwei Yang; Preethi Krishnan; Hiromichi Tanaka; Masanori Baba; Yung-Chi Cheng
Journal:  Antimicrob Agents Chemother       Date:  2007-03-12       Impact factor: 5.191

8.  Novel 4'-substituted stavudine analog with improved anti-human immunodeficiency virus activity and decreased cytotoxicity.

Authors:  Ginger E Dutschman; Susan P Grill; Elizabeth A Gullen; Kazuhiro Haraguchi; Shingo Takeda; Hiromichi Tanaka; Masanori Baba; Yung-Chi Cheng
Journal:  Antimicrob Agents Chemother       Date:  2004-05       Impact factor: 5.191

9.  Impact of novel human immunodeficiency virus type 1 reverse transcriptase mutations P119S and T165A on 4'-ethynylthymidine analog resistance profile.

Authors:  Guangwei Yang; Elijah Paintsil; Ginger E Dutschman; Susan P Grill; Chuan-Jen Wang; Jimin Wang; Hiromichi Tanaka; Takayuki Hamasaki; Masanori Baba; Yung-Chi Cheng
Journal:  Antimicrob Agents Chemother       Date:  2009-08-24       Impact factor: 5.191

10.  Retention of metabolites of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel anti-human immunodeficiency virus type 1 thymidine analog, in cells.

Authors:  Xin Wang; Hiromichi Tanaka; Masanori Baba; Yung-chi Cheng
Journal:  Antimicrob Agents Chemother       Date:  2009-05-26       Impact factor: 5.191
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