Fluoroalkyl derivatives of two biologically active oligopeptides [(m-CF3)Tyr(1)]-Leu-enkephalin, [(m-C2F4Cl)Tyr(1)]-Leu-enkephalin and [(m-COCF2Cl)Tyr(2)]-melanocyte-stimulating hormone releasing hormone have been syn...Fluoroalkyl derivatives of two biologically active oligopeptides [(m-CF3)Tyr(1)]-Leu-enkephalin, [(m-C2F4Cl)Tyr(1)]-Leu-enkephalin and [(m-COCF2Cl)Tyr(2)]-melanocyte-stimulating hormone releasing hormone have been synthesized. Studies on the activities of these peptides are underway.展开更多
A series of novel gossypol derivatives were synthesized and screened for their in vitro anti-HIV- 1I activity. The results showed that replacing the aldehyde groups of gossypol with certain oligopeptides and Dglucosam...A series of novel gossypol derivatives were synthesized and screened for their in vitro anti-HIV- 1I activity. The results showed that replacing the aldehyde groups of gossypol with certain oligopeptides and Dglucosamine not only reduced the cytotoxicity of gossypol derivatives but also enhanced their antiviral activity against HIV-1. Interestingly, D-glucosamine derivative of gossypol that lacked the COONa group also exhibited the same potent anti-HIV-1 activity as oligopeptide derivatives with the COONa group. These compounds blocked the entry of HIV-1ⅢB into target cell. which was similar to T20. Furthermore, the molecular docking analysis rationalized their anti-HIV-1 activity. The results also implied that certain oligopeptides and D-glucosamine were important moities to prepare gossypol derivatives as HIV- 1 entry inhibitors besides certain amino acids.展开更多
基金Project supported by the National Natural Science Foundation of China.
文摘Fluoroalkyl derivatives of two biologically active oligopeptides [(m-CF3)Tyr(1)]-Leu-enkephalin, [(m-C2F4Cl)Tyr(1)]-Leu-enkephalin and [(m-COCF2Cl)Tyr(2)]-melanocyte-stimulating hormone releasing hormone have been synthesized. Studies on the activities of these peptides are underway.
基金the National Natural Science Foundation of China(No.30770228)for financial support
文摘A series of novel gossypol derivatives were synthesized and screened for their in vitro anti-HIV- 1I activity. The results showed that replacing the aldehyde groups of gossypol with certain oligopeptides and Dglucosamine not only reduced the cytotoxicity of gossypol derivatives but also enhanced their antiviral activity against HIV-1. Interestingly, D-glucosamine derivative of gossypol that lacked the COONa group also exhibited the same potent anti-HIV-1 activity as oligopeptide derivatives with the COONa group. These compounds blocked the entry of HIV-1ⅢB into target cell. which was similar to T20. Furthermore, the molecular docking analysis rationalized their anti-HIV-1 activity. The results also implied that certain oligopeptides and D-glucosamine were important moities to prepare gossypol derivatives as HIV- 1 entry inhibitors besides certain amino acids.
