Synthesis of novel L-N-MCd4T as a potent anti-HIV agent

被引：22
|
作者：
Park, Ah-Young
Moon, Hyung Ryong [1 ]
Kim, Kyung Ran
Chun, Moon Woo
Jeong, Lak Shin
机构：
[1] Pusan Natl Univ, Coll Pharm, Med Chem Lab, Pusan 609735, South Korea
[2] Pusan Natl Univ, Res Inst Drug Dev, Pusan 609735, South Korea
[3] Seoul Natl Univ, Coll Pharm, Seoul 151742, South Korea
[4] Ewha Womans Univ, Coll Pharm, Med Chem Lab, Seoul 120750, South Korea
来源：
ORGANIC & BIOMOLECULAR CHEMISTRY | 2006年 / 4卷 / 22期
关键词：
D O I：
10.1039/b612537a
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
L-N-MCd4T (1) has been synthesized as a potent anti-HIV agent starting from (R)-epichlorohydrin using tandem alkylation, chemoselective reduction of ester in the presence of lactone functional group, RCM reaction and Mitsunobu reaction as key steps and was found to be a very potent anti-HIV-1 (EC50 = 6.76 mu g mL(-1)) agent without cytotoxicity up to 100 mu g mL(-1), indicating that the anti-HIV-1 activity found is similar to that of ddI (EC50 = 4.95 mu g mL(-1)), which is used clinically for the treatment of AIDS patients.
引用
收藏
页码：4065 / 4067
页数：3
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