BMS-707035 - CAS 729607-74-3
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Not Intended for Therapeutic Use. For research use only.
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BMS-707035 is a specific HIV-I integrase (IN) inhibitor with IC50 of 15 nM.
Publictions citing BOC Sciences Products
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1.HIV-1 integrase inhibitors: an emerging clinical reality.
Dayam R1, Al-Mawsawi LQ, Neamati N. Drugs R D. 2007;8(3):155-68.
From the discovery of HIV-1 integrase (IN) inhibitors using enzyme-based assays in 1992, it has taken 15 years to achieve success in human clinical trials. Currently available antiretroviral drugs set high clinical standards in efficacy and long-term safety for upcoming novel HIV/AIDS therapeutic agents. The results from advanced stages of human clinical trials with IN inhibitors indicate a promising future for these compounds as a novel class of antiretroviral drugs. Success and failure of previously discovered antiretroviral drugs have taught us that there are no magic bullets in eradicating HIV. However, approval of drugs selectively targeting IN has long been awaited. There is once again a surge of interest in the field focusing on clinical development of IN inhibitors. Here, we summarise the current status of IN inhibitors under clinical development. These agents include S-1360, GSK-364735, L-870,810, L-870,812, MK-0518, GS-9137, L-900564, GS-9224, and BMS-707035.
2.Anti-infectives: clinical progress of HIV-1 integrase inhibitors.
Al-Mawsawi LQ1, Al-Safi RI, Neamati N. Expert Opin Emerg Drugs. 2008 Jun;13(2):213-25. doi: 10.1517/14728214.13.2.213 .
BACKGROUND: HIV-1 integrase (IN) represents a therapeutically advantageous viral target to treat HIV/AIDS in the clinic. Over a decade of progress in the field has resulted in IN inhibitor chemical classes that display specificity for strand transfer catalysis of the enzyme, thus blocking viral DNA integration into host cell nuclear DNA, an essential step for viral infectivity.
3.3-Hydroxy-6,7-dihydropyrimido[2,1-c][1,4]oxazin-4(9H)-ones as new HIV-1 integrase inhibitors WO2011046873 A1.
Cotelle P1. Expert Opin Ther Pat. 2011 Nov;21(11):1799-804. doi: 10.1517/13543776.2011.624272. Epub 2011 Oct 6.
Since the discovery of raltegravir, the first FDA-approved integrase inhibitor, Merck and other pharmaceutical companies have continued their research programs in order to introduce novel molecules as second generation integrase inhibitors. Elvitegravir (Japan Tobacco/Gilead) and dolutegravir (Shionogi/GlaxoSmithKline) are in advanced stages of clinical development. Bristol-Myers Squibb has developed molecules leading to BMS-707035, which was stopped at the Phase II clinical trial stage. Herein is presented the last patent from this company where, in particular, new 3-hydroxy-6,7-dihydropyrimido[2,1-c][1,4]oxazin-4(9H)-ones are synthesized and their biological properties given.
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CAS 729607-74-3 BMS-707035

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