Synthesis and Cytotoxic Activity of Novel Ergosterol Peroxide Derivatives with Acrylate or Propionate Side Chain

被引：3
|
作者：
Bu, Ming [1 ]
Zhang, Zhiguo [2 ]
Li, Gang [3 ]
Xie, Chunhua [2 ]
Du, Xiaohui [1 ]
Ma, Guofang [1 ]
Li, Hongling [4 ]
机构：
[1] Qiqihar Med Univ, Coll Pharm, Qiqihar, Peoples R China
[2] Qiqihar Med Univ, Dept Pharm, Affiliated Hosp 2, Qiqihar, Peoples R China
[3] Qiqihar Med Univ, Res Inst Med Pharm, Qiqihar, Peoples R China
[4] Qiqihar Med Univ, Dept Psychiat, Qiqihar 161006, Peoples R China
来源：
NATURAL PRODUCT COMMUNICATIONS | 2022年 / 17卷 / 12期
关键词：
natural products modification; synthesis; ergosterol peroxide derivatives; anticancer activity; drug discovery; STEROIDAL; 5-ALPHA; 8-ALPHA-ENDOPEROXIDE DERIVATIVES; BIOLOGICAL EVALUATION; CELL-GROWTH; ANTICANCER; TETRAHYDROCURCUMIN;
D O I：
10.1177/1934578X221143634
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of novel ergosterol peroxide derivatives with acrylate or propionate side chain were synthesized. All compounds 3a-n were evaluated for their cytotoxicity against four kinds of human carcinoma cell lines (HepG2, MCF-7, HCT-116, and A549). Most of the derivatives displayed stronger cytotoxicity than ergosterol peroxide parent. Among them, compound 3h with the highest potency against HepG2 cell line (IC50 = 2.70 mu M), which was 7.47-fold more efficacious than ergosterol peroxide. The results suggested that the introduction of acrylate or propionate side chain at C-3 position of ergosterol peroxide is beneficial to enhance its cytotoxic activity. Compound 3h has potential to become a novel anti-tumor agent through further structural modification.
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页数：9
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