Heterocycle-functional gramine analogues: solvent- and catalyst-free synthesis and their inhibition activities against cell proliferation.
A series of novel gramine analogues were designed and synthesized via a convenient three-component reaction, and which were evaluated for their inhibition activities against cell proliferation. Their structures were confirmed by satisfactory spectra analyses mainly including (1)H NMR, and ESI-MS analyses. The preliminary assays indicated that some of the newly synthesized compounds displayed significantly good inhibition activities against human lung cancer (NCI-H460), hepatocellular liver carcinoma (HepG2), gastric cancer (SGC-7901 and BGC-823) cell lines compared with the control 5-Fluorouracil (5-FU), which might be developed as novel lead scaffold for potential anticancer agents.
National Biopesticide Engineering Research Center, Hubei Academy of Agricultural Sciences, No. 6 Nanhu Yaoyuan, Wuhan 430064, PR China. keshaoyong@163.com
Shaoyong
S
Ke
Liqiao
L
Shi
Xiufang
X
Cao
Qingyu
Q
Yang
Ying
Y
Liang
Ziwen
Z
Yang
D000470:Alkaloids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002384:Catalysis; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D060326:Chemistry Techniques, Synthetic; D006571:Heterocyclic Compounds / Q000737:chemistry*; D006801:Humans; D026121:Indole Alkaloids; D020128:Inhibitory Concentration 50
D000470:Alkaloids; D000970:Antineoplastic Agents; D006571:Heterocyclic Compounds; D026121:Indole Alkaloids; C007884:gramine