期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 30, 期 16, 页码 -出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2020.127304
关键词
Chalcone; Acetamides; Cytotoxicity; Jones reagent; Growth inhibition; Human cancer cell lines
资金
- Council of Scientific and Industrial Research (CSIR), New Delhi, India [DST-SERB/EEQ/2017/095]
A new series of 1,2,3-triazole tethered chalcone acetamide derivatives (7a-c & 8a-r) have been synthesized in excellent yields and their structures were determined by analytical and spectral (FT-IR, H-1 NMR, C-13 NMR HRMS) studies. The newly synthesized derivatives were evaluated for their cytotoxic activity against four human cancer cell lines, such as HeLa (Human cervical cancer), A549 (Human alveolar adenocarcinoma), MCF-7 (Human breast adenocarcinoma) and SKNSH (Human brain cancer). Among them, compound 7c exhibited good anti-proliferation activity with HeLa (IC50 7.41 + 0.8 mu M), SKNSH (IC50 8.68 + 1.1 mu M), MCF-7 (IC50 9.76 + 1.3 mu M) and MDA-MB-231, while compounds 7a and 7b showed promising anti-proliferation against above four human cancer cell lines with IC50 7.95-11.62 mu M, respectively, compared with the standard drug Doxorubicin. We explored the probable key active site and binding mode interactions in HDAC8 (PDB ID:3SFH) and EHMT2 (PDB ID:3K5K) proteins. The docking results are complementary to the experimental observations.
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