In this study,a novel series of cordycepin derivatives with benzenesulfonamido groups at the 6-position of the purine ring were synthesized and their antitumor activity was evaluated.We revealed the structural moietie...In this study,a novel series of cordycepin derivatives with benzenesulfonamido groups at the 6-position of the purine ring were synthesized and their antitumor activity was evaluated.We revealed the structural moieties of the cordycepin analogs that were required for antitumor activity.Among all the target compounds,those with 4-methyl and 4-nitro substituents on the benzene ring displayed better activity than the lead compound in antiproliferative activity experiments using MDA-MB-231 and A549 cells.However,compounds with 4-methoxybenzene and 2-oxoindoline groups and ethylene spacers displayed more significant activity than the lead compound in antiproliferative activity experiments using He La cells.In particular,a compound with a 4-bromo substituent and an ethylene spacer displayed very high inhibitory activity against the proliferation of MDA-MB-231,A549,and He La cells,suggesting that it had the potential for further development and application.展开更多
基金Research Basic Ability Enhancement Project of Young and Middle-aged Teachers in Guangxi Universities(Grant No.2019KY0166)the Project of Guangxi University for Nationalities(Grant No.2018MDYB006,2018XJGY46)。
文摘In this study,a novel series of cordycepin derivatives with benzenesulfonamido groups at the 6-position of the purine ring were synthesized and their antitumor activity was evaluated.We revealed the structural moieties of the cordycepin analogs that were required for antitumor activity.Among all the target compounds,those with 4-methyl and 4-nitro substituents on the benzene ring displayed better activity than the lead compound in antiproliferative activity experiments using MDA-MB-231 and A549 cells.However,compounds with 4-methoxybenzene and 2-oxoindoline groups and ethylene spacers displayed more significant activity than the lead compound in antiproliferative activity experiments using He La cells.In particular,a compound with a 4-bromo substituent and an ethylene spacer displayed very high inhibitory activity against the proliferation of MDA-MB-231,A549,and He La cells,suggesting that it had the potential for further development and application.
