Synthesis and bioactivity of 5-substituted-2-furoyl diacylhydazide derivatives with aliphatic chain.
A series of 5-substituted-2-furoyl diacylhydazide derivatives with aliphatic chain were designed and synthesized. Their structures were characterized by IR, 1H NMR, elemental analysis, and X-ray single crystal diffraction. The anti-tumor bioassay revealed that some title compounds exhibited promising activity against the selected cancer cell lines, especially against the human promyelocytic leukemic cells (HL-60). Their fungicidal tests indicated that most of the title compounds showed significant anti-fungal activity. The preliminary structure-activity relationship showed that the aliphatic chain length and differences in the R2 group had obvious effects on the anti-tumor and anti-fungal activities. The bioassay results demonstrated that the title compounds hold great promise as novel lead compounds for further drug discovery.
Guangdong Province Key Laboratory of Microbial Signals and Disease Control, Department of Plant Pathology, College of Natural Resources and Environment, South China Agricultural University, Guangzhou 510642, China. ziningcui@scau.edu.cn.
Zining
Z
Cui
Department of Pesticide Science, Plant Protection College, Shenyang Agricultural University, Shenyang 110866, China. xinghai30@163.com.
Xinghai
X
Li
State Key Laboratory for Biology of Plant Diseases and Insect Pests, Institute of Plant Protection, Chinese Academy of Agricultural Sciences, Beijing 100193, China. ftian@ippcaas.cn.
Fang
F
Tian
State Key Laboratory for Biology of Plant Diseases and Insect Pests, Institute of Plant Protection, Chinese Academy of Agricultural Sciences, Beijing 100193, China. yanxjcau@gmail.com.
Xiaojing
X
Yan
D000818:Animals; D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects; D002460:Cell Line; D018360:Crystallography, X-Ray; D005658:Fungi / Q000187:drug effects; D018922:HL-60 Cells; D006801:Humans; D006834:Hydrazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D007306:Insecticides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D007814:Larva / Q000187:drug effects; D008968:Molecular Conformation; D013329:Structure-Activity Relationship
D000935:Antifungal Agents; D000970:Antineoplastic Agents; D006834:Hydrazines; D007306:Insecticides; C029424:hydrazine