In this study, we investigated the anticancer activity of novel carbazoyl hydrazine derivatives as inhibitors of Proviral Integration site for Moloney murine leukemia virus kinase 1 (Pim-1) in liver cancer cells in vitro. The obtained compounds were characterized using 1H NMR, 13C NMR, HRMS, and FTIR. Through computer-assisted screening, antitumor activity testing, and Pim-1 inhibitory activity testing, most of the compounds exhibited significant inhibitory activity against liver cancer cell lines. Among them, compound N'-(2-(9H-carbazol-9-yl) acetyl)-4-fluorobenzohydrazide (4r) demonstrated a remarkable anticancer effect by inducing G2/M phase cell cycle arrest and apoptosis. It was identified as a highly efficient lead compound in our screening process. Overall, our study provides valuable insights into the anticancer activity of novel carbazoyl hydrazine derivatives as Pim1 inhibitors in liver cancer cells. The identified lead compound 4r demonstrates promising potential for further exploration and development in future studies for liver cancer treatment.
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Beijing Univ Chem Technol, Coll Life Sci & Technol, Beijing 100029, Peoples R ChinaBeijing Univ Chem Technol, Coll Life Sci & Technol, Beijing 100029, Peoples R China
Xu, Jiwei
Shen, Cheng
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Natl Inst Biol Sci, Beijing 102206, Peoples R China
Chinese Acad Med Sci, Grad Sch, Peking Union Med Coll, Beijing, Peoples R ChinaBeijing Univ Chem Technol, Coll Life Sci & Technol, Beijing 100029, Peoples R China
Shen, Cheng
Xie, Yuting
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Natl Inst Biol Sci, Beijing 102206, Peoples R ChinaBeijing Univ Chem Technol, Coll Life Sci & Technol, Beijing 100029, Peoples R China
Xie, Yuting
Qiu, Boxiang
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Beijing Univ Chem Technol, Coll Life Sci & Technol, Beijing 100029, Peoples R ChinaBeijing Univ Chem Technol, Coll Life Sci & Technol, Beijing 100029, Peoples R China
Qiu, Boxiang
Ren, Xintong
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Natl Inst Biol Sci, Beijing 102206, Peoples R ChinaBeijing Univ Chem Technol, Coll Life Sci & Technol, Beijing 100029, Peoples R China
Ren, Xintong
Zhou, Yu
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Natl Inst Biol Sci, Beijing 102206, Peoples R ChinaBeijing Univ Chem Technol, Coll Life Sci & Technol, Beijing 100029, Peoples R China
Zhou, Yu
Li, Gudong
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Beijing Univ Chem Technol, Coll Life Sci & Technol, Beijing 100029, Peoples R ChinaBeijing Univ Chem Technol, Coll Life Sci & Technol, Beijing 100029, Peoples R China
Li, Gudong
Zheng, Guojun
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Beijing Univ Chem Technol, Coll Life Sci & Technol, Beijing 100029, Peoples R ChinaBeijing Univ Chem Technol, Coll Life Sci & Technol, Beijing 100029, Peoples R China
Zheng, Guojun
Huang, Niu
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Natl Inst Biol Sci, Beijing 102206, Peoples R China
Tsinghua Univ, Tsinghua Inst Multidisciplinary Biomed Res, Beijing 102206, Peoples R ChinaBeijing Univ Chem Technol, Coll Life Sci & Technol, Beijing 100029, Peoples R China
机构:
Fudan Univ, Sch Pharm, Dept Med Chem, 826 Zhangheng Rd, Shanghai 201203, Peoples R ChinaFudan Univ, Sch Pharm, Dept Med Chem, 826 Zhangheng Rd, Shanghai 201203, Peoples R China
Huang, Ke
Jiang, Lulu
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Fudan Univ, Sch Pharm, Dept Med Chem, 826 Zhangheng Rd, Shanghai 201203, Peoples R ChinaFudan Univ, Sch Pharm, Dept Med Chem, 826 Zhangheng Rd, Shanghai 201203, Peoples R China
Jiang, Lulu
Liang, Ronghui
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Jinan Univ, Biomed Translat Res Inst, Guangzhou 510632, Guangdong, Peoples R ChinaFudan Univ, Sch Pharm, Dept Med Chem, 826 Zhangheng Rd, Shanghai 201203, Peoples R China
Liang, Ronghui
Li, Huiti
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Fudan Univ, Sch Pharm, Dept Med Chem, 826 Zhangheng Rd, Shanghai 201203, Peoples R ChinaFudan Univ, Sch Pharm, Dept Med Chem, 826 Zhangheng Rd, Shanghai 201203, Peoples R China
Li, Huiti
Ruan, Xiaoxue
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Fudan Univ, Sch Pharm, Dept Med Chem, 826 Zhangheng Rd, Shanghai 201203, Peoples R ChinaFudan Univ, Sch Pharm, Dept Med Chem, 826 Zhangheng Rd, Shanghai 201203, Peoples R China
Ruan, Xiaoxue
Shan, Changliang
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Jinan Univ, Biomed Translat Res Inst, Guangzhou 510632, Guangdong, Peoples R China
Nankai Univ, State Key Lab Med Chem Biol, Coll Pharm, Tianjin 300350, Peoples R ChinaFudan Univ, Sch Pharm, Dept Med Chem, 826 Zhangheng Rd, Shanghai 201203, Peoples R China
Shan, Changliang
Ye, Deyong
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Fudan Univ, Sch Pharm, Dept Med Chem, 826 Zhangheng Rd, Shanghai 201203, Peoples R ChinaFudan Univ, Sch Pharm, Dept Med Chem, 826 Zhangheng Rd, Shanghai 201203, Peoples R China
Ye, Deyong
Zhou, Lu
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Fudan Univ, Sch Pharm, Dept Med Chem, 826 Zhangheng Rd, Shanghai 201203, Peoples R ChinaFudan Univ, Sch Pharm, Dept Med Chem, 826 Zhangheng Rd, Shanghai 201203, Peoples R China