کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1363814 981522 2006 11 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Modification at the C9 position of the marine natural product isoaaptamine and the impact on HIV-1, mycobacterial, and tumor cell activity
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Modification at the C9 position of the marine natural product isoaaptamine and the impact on HIV-1, mycobacterial, and tumor cell activity
چکیده انگلیسی

As part of an investigation to generate optimized drug leads from marine natural pharmacophores for the treatment of neoplastic and infectious diseases, a series of novel isoaaptamine analogs were prepared by coupling acyl halides to the C9 position of isoaaptamine (2) isolated from the Aaptos sponge. This library of new semisynthetic products was evaluated for biological activity against HIV-1, Mtb, AIDS-OI, tropical parasitic diseases, and cancer. Compound 4 showed potent activity against HIV-1 (EC50 0.47 μg/mL), compound 19 proved to possess remarkable activity against Mycobacterium intracellulare with an IC50 and MIC value of 0.15 and 0.31 μg/mL, while compounds 4 and 17 possessed anti-leishmanial activity with IC50 values of 0.1 and 0.4 μg/mL, respectively. Compounds 16 and 17 showed antimalarial activity with EC50 values of 230 and 240 ng/mL, respectively, and compound 14 exhibited an EC50 of 0.05 μM against the Leukemia cell line K-562.

A series of isoaaptamine analogs were prepared at the C9 position of isoaaptamine (2) and were evaluated for their biological activity against HIV-1, Mtb, AIDS-OI, tropical parasitic diseases, and cancer.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 14, Issue 24, 15 December 2006, Pages 8495–8505
نویسندگان
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