التفاصيل البيبلوغرافية
| العنوان: |
Direct Synthesis of 2‐Acyl Acridines Using Aldimines and Anthranils: Evaluation of Cytotoxicity and Anti‐Inflammatory Activity. |
| المؤلفون: |
Kim, Saegun, Kundu, Amit, Chun, Rina, Han, Sang Hoon, Pandey, Ashok Kumar, Yoo, Sungin, Park, Junghyun, Kim, Hyung Sik, Ku, Jin‐Mo, Kim, In Su |
| المصدر: |
Asian Journal of Organic Chemistry; Oct2018, Vol. 7 Issue 10, p2069-2075, 7p |
| مصطلحات موضوعية: |
ACRIDINES, ALDIMINES, ANTHRANIL |
| مستخلص: |
Rhodium (III)‐catalyzed C−H aminations of aldimines with anthranils followed by intramolecular cyclization are described. These transformations facilitate the efficient generation of 2‐acyl acridines, which are important motifs found in bioactive natural products and pharmaceuticals. All synthesized 2‐acyl acridines were first screened for cytotoxic activity against human renal carcinoma cells (CAKI‐1 and 786‐O) and human breast carcinoma cells (MCF‐7). Compound 3 z showed the most potent cytotoxic activity, which is stronger than that of doxorubicin against CAKI‐1 and 786‐O cells. In addition, compounds that exhibited potent cytotoxicities were selected for further in vitro anti‐inflammatory activity testing using interleukin‐6 (IL‐6) with lipopolysaccharide (LPS)‐induced RAW264.7 cells. Notably, compounds (3 k, 3 n, 3 s and 3 x–3 z) were found to exhibit inhibitory activities that are about two‐ to three‐times more potent than that of the anti‐inflammatory drug dexamethasone. Rhodium (III)‐catalyzed C−H aminations of aldimines with anthranils followed by intramolecular cyclization are described. All synthesized 2‐acyl acridines were screened for cytotoxic activity against human renal carcinoma cells (CAKI‐1 and 786‐O) and human breast carcinoma cells (MCF‐7). In addition, selected compounds were further evaluated for in vitro anti‐inflammatory activity using interleukin‐6 (IL‐6) with lipopolysaccharide (LPS)‐induced RAW264.7 cells. [ABSTRACT FROM AUTHOR] |
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| قاعدة البيانات: |
Complementary Index |
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