Literature DB >> 20050672

Highly suppressing wild-type HIV-1 and Y181C mutant HIV-1 strains by 10-chloromethyl-11-demethyl-12-oxo-calanolide A with druggable profile.

Hai Xue1, Xiaofan Lu, Purong Zheng, Li Liu, Chunyan Han, Jinping Hu, Zijie Liu, Tao Ma, Yan Li, Lin Wang, Zhiwei Chen, Gang Liu.   

Abstract

We herein report a new compound: 10-chloromethyl-11-demethyl-12-oxo-calanolide A (20, EC(50) = 7.4 nM, SI = 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 EC(50) = 7.4 nM and EC(50) = 0.46 nM, respectively.

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Year:  2010        PMID: 20050672     DOI: 10.1021/jm901653e

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  6 in total

1.  F18, a novel small-molecule nonnucleoside reverse transcriptase inhibitor, inhibits HIV-1 replication using distinct binding motifs as demonstrated by resistance selection and docking analysis.

Authors:  Xiaofan Lu; Li Liu; Xu Zhang; Terrence Chi Kong Lau; Stephen Kwok Wing Tsui; Yuanxi Kang; Purong Zheng; Bojian Zheng; Gang Liu; Zhiwei Chen
Journal:  Antimicrob Agents Chemother       Date:  2011-10-28       Impact factor: 5.191

Review 2.  Two decades of recent advances of Ugi reactions: synthetic and pharmaceutical applications.

Authors:  Manar Ahmed Fouad; Hamida Abdel-Hamid; Mohammed Salah Ayoup
Journal:  RSC Adv       Date:  2020-11-23       Impact factor: 4.036

Review 3.  Therapeutic potential of coumarins as antiviral agents.

Authors:  Mohd Zaheen Hassan; Hasnah Osman; Mohamed Ashraf Ali; Mohamed Jawed Ahsan
Journal:  Eur J Med Chem       Date:  2016-07-25       Impact factor: 6.514

Review 4.  Pharmacological perspectives and molecular mechanisms of coumarin derivatives against virus disease.

Authors:  Zhoupeng Li; Dehui Kong; Yongsheng Liu; Mingkai Li
Journal:  Genes Dis       Date:  2021-04-20

5.  Metabolism of F18, a Derivative of Calanolide A, in Human Liver Microsomes and Cytosol.

Authors:  Xiangmeng Wu; Qinghao Zhang; Jiamei Guo; Yufei Jia; Ziqian Zhang; Manman Zhao; Yakun Yang; Baolian Wang; Jinping Hu; Li Sheng; Yan Li
Journal:  Front Pharmacol       Date:  2017-07-19       Impact factor: 5.810

Review 6.  Naturally Occurring Calanolides: Occurrence, Biosynthesis, and Pharmacological Properties Including Therapeutic Potential.

Authors:  Lutfun Nahar; Anupam Das Talukdar; Deepa Nath; Sushmita Nath; Aman Mehan; Fyaz M D Ismail; Satyajit D Sarker
Journal:  Molecules       Date:  2020-10-28       Impact factor: 4.411

  6 in total

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