Eight new water-soluble amino acid conjugates 6 a-h of chlorin p6 ethers(5 a-d) were synthesized and preliminarily investigated for their in vitro PDT antitumor activity and structure-activity relationship(SAR). The r...Eight new water-soluble amino acid conjugates 6 a-h of chlorin p6 ethers(5 a-d) were synthesized and preliminarily investigated for their in vitro PDT antitumor activity and structure-activity relationship(SAR). The results showed that all compounds exhibited much higher phototoxicity against tumor cells than talaporfin. SAR analysis indicated that PDT antitumor effect enhanced with the increase of carbon chain length of alkoxyl ether bonds at 3~1-position, and L-aspartic acid was superior to L-glutamic acid. In particular, the IC_50 values of most phototoxic compound 6 d were 0.20 mmol/L against A549 cell and0.41υmmol/L against B16-F10 cell, which individually represented 31-and 24-fold increase of antitumor potency compared to talaporfin, suggesting that it was a promising candidate photosensitizer(PS) for PDT applications due to its strong absorption at long wavelength, high phototoxicity, low dark cytotoxicity and good water-solubility.展开更多
Iodiconazole is a novel antifungal agent that was developed in its racemic form. In order to investigate the ef- fects of the chiral center on the antifungal activity, R- and S-isomers of iodiconazole were prepared on...Iodiconazole is a novel antifungal agent that was developed in its racemic form. In order to investigate the ef- fects of the chiral center on the antifungal activity, R- and S-isomers of iodiconazole were prepared on the basis of the asymmetric Sharpless epoxidation. （S）-Iodiconazole was proved to have better antifungal activity than the （R）- isomer. The binding modes of the two isomers with lanosterol 14~z-demethylase were clarified by molecular dock- ing.展开更多
Based on the EMMS model, the local slip velocity between gas and solid is systematically analyzed and a theoretical correlation of local slip velocity with local voidage for a downer is derived as follows:U_s(r)/U_t=D...Based on the EMMS model, the local slip velocity between gas and solid is systematically analyzed and a theoretical correlation of local slip velocity with local voidage for a downer is derived as follows:U_s(r)/U_t=D^(8/7)(1-ε_mt)^(-2/7)[(1-ε(r)/(ε(r))]^(8/7)]ε(r)(47/14)((ε(r)-ε_(mt))/ε(r)) Using this correlation, the local gas-solid slip velocity in a downer is calculated. The calculated results are well consistent with experimental data. In addition, the variation of the local slip velocity with its corresponding solid holdup is also dis-cussed.展开更多
基金supported by grants from the National Natural Science Foundation of China (Nos. 81172950 and 81671739)the Project of Science and Technology Commission of Shanghai (No. 11431920401)the College Students’ Innovation Ability Training Project of Second Military Medical University (No. MS2017040)
文摘Eight new water-soluble amino acid conjugates 6 a-h of chlorin p6 ethers(5 a-d) were synthesized and preliminarily investigated for their in vitro PDT antitumor activity and structure-activity relationship(SAR). The results showed that all compounds exhibited much higher phototoxicity against tumor cells than talaporfin. SAR analysis indicated that PDT antitumor effect enhanced with the increase of carbon chain length of alkoxyl ether bonds at 3~1-position, and L-aspartic acid was superior to L-glutamic acid. In particular, the IC_50 values of most phototoxic compound 6 d were 0.20 mmol/L against A549 cell and0.41υmmol/L against B16-F10 cell, which individually represented 31-and 24-fold increase of antitumor potency compared to talaporfin, suggesting that it was a promising candidate photosensitizer(PS) for PDT applications due to its strong absorption at long wavelength, high phototoxicity, low dark cytotoxicity and good water-solubility.
基金the National Natural Science Foundation of China，Shanghai Municipal Health Bureau
文摘Iodiconazole is a novel antifungal agent that was developed in its racemic form. In order to investigate the ef- fects of the chiral center on the antifungal activity, R- and S-isomers of iodiconazole were prepared on the basis of the asymmetric Sharpless epoxidation. （S）-Iodiconazole was proved to have better antifungal activity than the （R）- isomer. The binding modes of the two isomers with lanosterol 14~z-demethylase were clarified by molecular dock- ing.
基金supports from the National Program of Basic Research(No.G1999022103)Key Project of the National Natural Science Foundation of China(No.29936090)are gratefully acknowledged.
文摘Based on the EMMS model, the local slip velocity between gas and solid is systematically analyzed and a theoretical correlation of local slip velocity with local voidage for a downer is derived as follows:U_s(r)/U_t=D^(8/7)(1-ε_mt)^(-2/7)[(1-ε(r)/(ε(r))]^(8/7)]ε(r)(47/14)((ε(r)-ε_(mt))/ε(r)) Using this correlation, the local gas-solid slip velocity in a downer is calculated. The calculated results are well consistent with experimental data. In addition, the variation of the local slip velocity with its corresponding solid holdup is also dis-cussed.
