کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10582749 | 981101 | 2011 | 8 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Design, synthesis, and biological evaluation of N-acetyl-S-(p-chlorophenylcarbamoyl)cysteine and its analogs as a novel class of anticancer agents
دانلود مقاله + سفارش ترجمه
دانلود مقاله ISI انگلیسی
رایگان برای ایرانیان
کلمات کلیدی
PBSEWGEDGFBSN-acetyl-l-cysteineTFANACDPBSTHFIC50(3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) - (3- (4،5-dimethylthiazol-2-yl) -2،5-diphenyltetrazolium bromide)BSA - BSADMSO - DMSOMTT - MTTbovine serum albumin - آلبومین سرم گاوTrifluoroacetic acid - اسید TrifluoroaceticTetrahydrofuran - تتراهیدروفورانCell cycle distribution - توزیع چرخه سلولیApoptosis - خزان یاختهایDimethyl sulfoxide - دیمتیل سولفواکسیدStructure activity relationship - رابطه فعالیت ساختاریfetal bovine serum - سرم جنین گاوSynthesis - سنتزDulbecco’s phosphate buffered saline - فسفات باسیل نمک DulbeccoPhosphate buffered saline - فسفات بافر شورPhosphatidylserine - فسفاتیدیلسرینAnticancer activity - فعالیت ضد سرطانPropidium iodide - پروتئین یدیدhigh performance liquid chromatography - کروماتوگرافی مایع با کارایی بالاHPLC - کروماتوگرافی مایعی کاراelectron withdrawing group - گروه اخراج الکترونelectron donating group - گروه اهدا الکترون
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
N-Acetyl-S-(p-chlorophenylcarbamoyl)cysteine (NACC) was identified as a metabolite of sulofenur. Sulofenur was demonstrated to have broad activity against solid tumors in preclinical studies but exhibited disappointing clinical responses due to its high protein binding related adverse effects. NACC exhibited low protein binding and excellent activity against a sulofenur sensitive human colon cancer cell line. In this study, analogs of NACC were synthesized and evaluated with four human cancer cell lines. Two of the NACC analogs showed excellent activity against two human melanoma cell lines, while NACC remains the most potent of the series. All three compounds were more potent than dacarbazine, which is used extensively in treating melanoma. NACC was shown to induce apoptosis without affecting the cell cycle. Further, NACC exhibited low toxicity against monkey kidney cells. The selective anticancer activity, low toxicity, an unknown yet but unique anticancer mechanism and ready obtainability through synthesis make NACC and its analogs promising anticancer agents.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 19, Issue 1, 1 January 2011, Pages 287-294
Journal: Bioorganic & Medicinal Chemistry - Volume 19, Issue 1, 1 January 2011, Pages 287-294
نویسندگان
Wei Chen, Teresa Seefeldt, Alan Young, Xiaoying Zhang, Xiangming Guan,