Anticancer Effect of Chlorambucil Enhanced by Chiral Phthalidyl Promoiety

Zhang, Long3; Cheng, Yisa1,2; Liu, Ying-Guo1,2; Chen, Xingkuan4; Liu, Hongmei3

2022-12-01

10.1002/cbdv.202201025

CHEMISTRY & BIODIVERSITY   影响因子和分区

1612-1872

1612-1880

Phthalidyl promoiety has been used in several drugs, but they were all marketed in racemic form. The pharmaceutical effects of each enantiomer have not been clearly demonstrated. In this project, an anticancer chemotherapy drug, chlorambucil, was modified as enantiopure phthalidyl prodrugs. The enantiomers, together with phthalidyl unit and their racemic mixture, were then subject to the in vivo bioactivity tests against B16F10 melanoma cells. It was found that proper chirality within the promoiety had noticeably better in vivo pharmacological effects than the parent drug, the enantiomer and racemic mixture. This merit perhaps could be extended from the phthalidyl prodrugs to other chirality containing prodrugs.

chiral promoieties antitumor activity phthalidyl prodrugs pharmaceutical enhancement phthalidyl promoieties

SCI

英语

第一 ; 通讯

National Natural Science Foundation of China[22101266] ; International Postdoctoral Exchange Fellowship Program[YJ20210304] ; China Postdoctoral Science Foundation[2022M722865] ; Jiangsu Department of Science and Technology[BE2020647] ; Social Development Project of Xuzhou Department of Science and Technology[KC20079] ; Open Fund of Guangdong Provincial Key Laboratory of Functional Supramolecular Coordination Materials and Applications[2020B08] ; Fundamental Research Funds["11620416","202201020559"]

Biochemistry & Molecular Biology ; Chemistry

Biochemistry & Molecular Biology ; Chemistry, Multidisciplinary

WOS:000894621900001

WILEY-V C H VERLAG GMBH

ENVIRONMENT/ECOLOGY

Web of Science

1.Zhengzhou Univ, Affiliated Hosp 1, Zhengzhou 450001, Peoples R China
2.Zhengzhou Univ, Henan Inst Adv Technol, Zhengzhou 450001, Peoples R China
3.Southern Univ Sci & Technol, Dept Biomed Engn, Shenzhen 518055, Guangdong, Peoples R China
4.Jinan Univ, Dept Chem, Guangdong Prov Key Lab Funct Supramol Coordinat Ma, Guangzhou 510632, Guangdong, Peoples R China

Zhang, Long,Cheng, Yisa,Liu, Ying-Guo,et al. Anticancer Effect of Chlorambucil Enhanced by Chiral Phthalidyl Promoiety[J]. CHEMISTRY & BIODIVERSITY,2022,20(1).

Zhang, Long,Cheng, Yisa,Liu, Ying-Guo,Chen, Xingkuan,&Liu, Hongmei.(2022).Anticancer Effect of Chlorambucil Enhanced by Chiral Phthalidyl Promoiety.CHEMISTRY & BIODIVERSITY,20(1).

Zhang, Long,et al."Anticancer Effect of Chlorambucil Enhanced by Chiral Phthalidyl Promoiety".CHEMISTRY & BIODIVERSITY 20.1(2022).