Highly Suppressing Wild-Type HIV-1 and Y181C Mutant HIV-1 Strains by 10-Chloromethyl-11-demethyl-12-oxo-calanolide A with Druggable Profile

Xue H; Lu XF; Zheng PR; Liu L; Han CY; Hu JP; Liu ZJ; Ma T; Li Y; Wang L; Chen ZW; Liu G

首页> 外文期刊>Journal of Medicinal Chemistry >Highly Suppressing Wild-Type HIV-1 and Y181C Mutant HIV-1 Strains by 10-Chloromethyl-11-demethyl-12-oxo-calanolide A with Druggable Profile

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Highly Suppressing Wild-Type HIV-1 and Y181C Mutant HIV-1 Strains by 10-Chloromethyl-11-demethyl-12-oxo-calanolide A with Druggable Profile

机译：高度抑制野生型HIV-1和Y181C突变型HIV-1菌株的10-氯甲基-11-demethyl-12-oxo-calanolide A具有可吸收性

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We herein report a new compound: 10-chloromethyl-11-demethyl-12-oxo-calanolide A (20, EC50 = 7.4 nM, St = 1417), which demonstrates a druggable profile with 32.7% oral bioavailability in rat, tolerated oral single dose toxicity in mice, and especially the feature of highly efficient suppression of the wild-type HIV-1 and Y181C mutant HIV-1 at an EC50 = 7.4 nM and EC50 = 0.46 nM, respectively.

机译：我们在此报告了一种新化合物：10-氯甲基-11-脱甲基-12-氧代-calanolide A（20，EC50 = 7.4 nM，St = 1417），该化合物在大鼠中具有可口服的32.7％的生物利用度，可耐受口服单药剂量对小鼠的毒性，特别是在EC50 = 7.4 nM和EC50 = 0.46 nM时，高效抑制野生型HIV-1和Y181C突变体HIV-1的特征。

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来源
《Journal of Medicinal Chemistry》 |2010年第3期|共5页
作者
Xue H; Lu XF; Zheng PR; Liu L; Han CY; Hu JP; Liu ZJ; Ma T; Li Y; Wang L; Chen ZW; Liu G;
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正文语种 eng
中图分类药学;
关键词
IMMUNODEFICIENCY-VIRUS TYPE-1; INHIBITORY NATURAL-PRODUCTS; REVERSE-TRANSCRIPTASE; (+)-CALANOLIDE; CALANOLIDE; ANALOGS; SENSITIVITY; GAMMA;

机译：免疫缺陷病毒-1型;抑制类天然产物;逆转录酶;（+）-卡拉内酯;卡拉内酯;类似物;敏感性;γ;

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1. Highly Suppressing Wild-Type HIV-1 and Y181C Mutant HIV-1 Strains by 10-Chloromethyl-11-demethyl-12-oxo-calanolide A with Druggable Profile [J] . Xue H, Lu XF, Zheng PR, Journal of Medicinal Chemistry . 2010,第3期

机译：高度抑制野生型HIV-1和Y181C突变型HIV-1菌株的10-氯甲基-11-demethyl-12-oxo-calanolide A具有可吸收性
2. First discovery of a potential carbonate prodrug of NNRTI drug candidate RDEA427 with submicromolar inhibitory activity against HIV-1 K103N/Y181C double mutant strain [J] . Huang Boshi, Liu Xinhao, Tian Ye, Bioorganic and Medicinal Chemistry Letters . 2018,第8期

机译：第一次发现具有亚麻摩尔抑制活性对HIV-1K103N / Y181C双突变菌株的亚麻摩尔抑制活性的碳酸NNRTI药物候选RDEA427的第一次发现
3. Discovery of Wild-Type and Y181C Mutant Non-nucleoside HIV-1 Reverse Transcriptase Inhibitors Using Virtual Screening with Multiple Protein Structures [J] . Nichols SE, Domaoal RA, Thakur VV, Journal of chemical information and modeling . 2009,第5期

机译：使用多蛋白结构的虚拟筛选发现野生型和Y181C突变型非核苷HIV-1逆转录酶抑制剂。
4. Detection of Differentially Expressed Genes in Wild Type HIV-1 Vpr and Two HIV-1 Mutant Vprs [C] . Bandana Barman, Anirban Mukhopadhyay International Conference on Frontiers of Intelligent Computing : Theory and Applications . 2014

机译：在野生型HIV-1VPR和两个HIV-1突变VPRS中检测差异表达基因
5. Part I: Synthesis of Cyclobutyl Nucleoside Analogs That Mimic AZT for Inhibition of the K65R HIV-1 Reverse Transcriptase Mutant. Part II: Synthesis and Evaluation of Truncated Triptolide Analogs to Suppress Chronic Inflammation [D] . Bluemling, Gregory Richard 2011

机译：第一部分：模拟AZT抑制K65R HIV-1逆转录酶突变体的环丁基核苷类似物的合成。第二部分：截短雷公藤甲素类似物的合成和评估，以抑制慢性炎症
6. Human immunodeficiency virus 1 (HIV-1)-specific reverse transcriptase (RT) inhibitors may suppress the replication of specific drug-resistant (E138K)RT HIV-1 mutants or select for highly resistant (Y181C--C181I)RT HIV-1 mutants. [O] . J Balzarini, A Karlsson, V V Sardana, 1994

机译：人类免疫缺陷病毒1（HIV-1）特异性逆转录酶（RT）抑制剂可抑制特定抗药性（E138K）RT HIV-1突变体的复制或选择高抗药性（Y181C- C181I）RT HIV-1突变体。
7. Human immunodeficiency virus 1 (HIV-1)-specific reverse transcriptase (RT) inhibitors may suppress the replication of specific drug-resistant (E138K)RT HIV-1 mutants or select for highly resistant (Y181C-->C181I)RT HIV-1 mutants [O] . Balzarini, Jan, Karlsson, A, Sardana, V V, 1994

机译：人类免疫缺陷病毒1（HIV-1）特异性逆转录酶（RT）抑制剂可抑制特定抗药性（E138K）RT HIV-1突变体的复制或选择高抗药性（Y181C-> C181I）RT HIV-1突变体

Highly Suppressing Wild-Type HIV-1 and Y181C Mutant HIV-1 Strains by 10-Chloromethyl-11-demethyl-12-oxo-calanolide A with Druggable Profile

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