Benzofuran;
Piperazine;
IPSO substitution;
Necrosis;
In vivo efficacy;
INHIBITORS;
SCAFFOLD;
DESIGN;
D O I:
10.1016/j.bmcl.2023.129425
中图分类号:
R914 [药物化学];
学科分类号:
100701 ;
摘要:
This work describes about the synthesis and evaluation of substituted benzofuran piperazines as potential anticancer agents. The synthesized candidates have been evaluated for their cell proliferation inhibition properties in six murine and human cancer cell lines. In vitro evaluation of apoptosis and cell cycle analysis with the lead candidate 1.19 reveals that necrosis might be an important pathway for the candidate compounds to cause cell death. Further, in vivo evaluation of the lead compound shows that this candidate is well tolerated in healthy mice. Additionally, an in vivo anticancer efficacy study in mice using a MDA-MB-231 xenograft model with the lead compound provides good anti-cancer efficacy.
机构:
Northeast Agr Univ, Dept Vet Med, Harbin 150030, Heilongjiang, Peoples R China
Heilongjiang Key Lab Anim Dis Control & Pharmaceu, Harbin 150030, Heilongjiang, Peoples R ChinaNortheast Agr Univ, Dept Vet Med, Harbin 150030, Heilongjiang, Peoples R China
Jin Bo
Tao Ye
论文数: 0引用数: 0
h-index: 0
机构:
Jilin Univ, Sch Pharmaceut Sci, Changchun 130021, Jilin, Peoples R ChinaNortheast Agr Univ, Dept Vet Med, Harbin 150030, Heilongjiang, Peoples R China
Tao Ye
Yang Hongliang
论文数: 0引用数: 0
h-index: 0
机构:
Northeast Agr Univ, Dept Vet Med, Harbin 150030, Heilongjiang, Peoples R China
Heilongjiang Key Lab Anim Dis Control & Pharmaceu, Harbin 150030, Heilongjiang, Peoples R ChinaNortheast Agr Univ, Dept Vet Med, Harbin 150030, Heilongjiang, Peoples R China
机构:
Nanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Peoples R ChinaNanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Peoples R China
Lv, Peng-Cheng
Li, Huan-Qiu
论文数: 0引用数: 0
h-index: 0
机构:
Nanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Peoples R ChinaNanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Peoples R China
Li, Huan-Qiu
Sun, Juan
论文数: 0引用数: 0
h-index: 0
机构:
Nanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Peoples R ChinaNanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Peoples R China
Sun, Juan
Zhou, Yang
论文数: 0引用数: 0
h-index: 0
机构:
Nanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Peoples R ChinaNanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Peoples R China
Zhou, Yang
Zhu, Hai-Liang
论文数: 0引用数: 0
h-index: 0
机构:
Nanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Peoples R ChinaNanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Peoples R China
机构:
Islamic Univ Madinah, Fac Sci, Dept Chem, Madinah 42351, Saudi ArabiaIslamic Univ Madinah, Fac Sci, Dept Chem, Madinah 42351, Saudi Arabia
Abolibda, Tariq Z.
El-Sayed, Abdel-Aziz A. A.
论文数: 0引用数: 0
h-index: 0
机构:
Islamic Univ Madinah, Fac Sci, Biol Dept, Madinah 42351, Saudi ArabiaIslamic Univ Madinah, Fac Sci, Dept Chem, Madinah 42351, Saudi Arabia
El-Sayed, Abdel-Aziz A. A.
Farag, Basant
论文数: 0引用数: 0
h-index: 0
机构:
Zagazig Univ, Fac Sci, Dept Chem, Zagazig 44519, EgyptIslamic Univ Madinah, Fac Sci, Dept Chem, Madinah 42351, Saudi Arabia
Farag, Basant
Zaki, Magdi E. A.
论文数: 0引用数: 0
h-index: 0
机构:
Imam Mohammed Ibn Saud Islamic Univ IMSIU, Fac Sci, Dept Chem, Riyadh 11623, Saudi ArabiaIslamic Univ Madinah, Fac Sci, Dept Chem, Madinah 42351, Saudi Arabia
Zaki, Magdi E. A.
Alrehaily, Abdulwahed
论文数: 0引用数: 0
h-index: 0
机构:
Islamic Univ Madinah, Fac Sci, Biol Dept, Madinah 42351, Saudi ArabiaIslamic Univ Madinah, Fac Sci, Dept Chem, Madinah 42351, Saudi Arabia
Alrehaily, Abdulwahed
Elbadawy, Hossein M.
论文数: 0引用数: 0
h-index: 0
机构:
Taibah Univ, Coll Pharm, Dept Pharmacol & Toxicol, Madinah 41477, Saudi ArabiaIslamic Univ Madinah, Fac Sci, Dept Chem, Madinah 42351, Saudi Arabia
Elbadawy, Hossein M.
Al-Shahri, Ahmad A.
论文数: 0引用数: 0
h-index: 0
机构:
Islamic Univ Madinah, Fac Noble Hadith, Dept Jurisprudence Sunnah & Its Sources, Madinah 41477, Saudi ArabiaIslamic Univ Madinah, Fac Sci, Dept Chem, Madinah 42351, Saudi Arabia
Al-Shahri, Ahmad A.
Alsenani, Saleh R.
论文数: 0引用数: 0
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机构:
Islamic Univ Madinah, Fac Sci, Biol Dept, Madinah 42351, Saudi ArabiaIslamic Univ Madinah, Fac Sci, Dept Chem, Madinah 42351, Saudi Arabia
Alsenani, Saleh R.
Gomha, Sobhi M.
论文数: 0引用数: 0
h-index: 0
机构:
Islamic Univ Madinah, Fac Sci, Dept Chem, Madinah 42351, Saudi ArabiaIslamic Univ Madinah, Fac Sci, Dept Chem, Madinah 42351, Saudi Arabia
机构:
Nanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Peoples R ChinaNanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Peoples R China
Lv, Peng-Cheng
Wang, Kai-Rui
论文数: 0引用数: 0
h-index: 0
机构:
Nanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Peoples R ChinaNanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Peoples R China
Wang, Kai-Rui
Li, Qing-Shan
论文数: 0引用数: 0
h-index: 0
机构:
Nanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Peoples R ChinaNanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Peoples R China
Li, Qing-Shan
Chen, Jin
论文数: 0引用数: 0
h-index: 0
机构:
Nanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Peoples R ChinaNanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Peoples R China
Chen, Jin
Sun, Juan
论文数: 0引用数: 0
h-index: 0
机构:
Nanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Peoples R ChinaNanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Peoples R China
Sun, Juan
Zhu, Hai-Liang
论文数: 0引用数: 0
h-index: 0
机构:
Nanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Peoples R ChinaNanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Peoples R China