title: Design, synthesis and evaluation of antitumor activity of new rotundic acid acylhydrazone derivatives.
abstract: In light of the important antitumor activity of acylhydrazone compounds and based on our previous study, 18 new rotundic acid (RA) acylhydrazone derivatives were synthesized. All of the compounds were characterized by their spectroscopic data. The antiproliferative activity of the compounds was evaluated in vitro via the MTT method in three tumor cell lines, including A-375 (human malignant melanoma cells), SPC-A1 (human lung adenocarcinoma) and NCI-H446 (small cell lung cancer). The results showed that the antiproliferative activity of all of the compounds on the NCI-H446 cell line did not increase compared to RA, however, most of the derivatives exhibited higher activity against the A375 and SPC-A1 cell lines as compared to RA. Importantly, the antiproliferative activities of compounds 5a and 5b were the highest among the compounds, with IC(50) values <10 μM. Collectively, compounds 5a and 5b may act as potential anti-tumor agents in the future.
authors.forename: Yu-Fang
authors.initials: YF
authors.lastname: He
authors.forename: Min-Lun
authors.initials: ML
authors.lastname: Nan
authors.forename: Yu-Wei
authors.initials: YW
authors.lastname: Zhao
authors.forename: Wen-Yi
authors.initials: WY
authors.lastname: Sun
authors.forename: Wei
authors.initials: W
authors.lastname: Li
authors.forename: Quan-Cheng
authors.initials: QC
authors.lastname: Zhao
mesh_terms: D000230:Adenocarcinoma / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D006801:Humans; D006835:Hydrazones; D008175:Lung Neoplasms / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D008545:Melanoma / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D055752:Small Cell Lung Carcinoma / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D014315:Triterpenes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D006835:Hydrazones; D014315:Triterpenes; C572089:rotundic acid