Naturally based pyrazoline derivatives as aminopeptidase N, VEGFR2 and MMP9 inhibitors: design, synthesis and molecular modeling
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作者:
Batran, Rasha Z.
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Natl Res Ctr, Pharmaceut & Drug Ind Res Inst, Chem Nat Cpds Dept, Cairo 12622, EgyptNatl Res Ctr, Pharmaceut & Drug Ind Res Inst, Chem Nat Cpds Dept, Cairo 12622, Egypt
Batran, Rasha Z.
[1
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Ahmed, Eman Y.
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Natl Res Ctr, Pharmaceut & Drug Ind Res Inst, Chem Nat Cpds Dept, Cairo 12622, EgyptNatl Res Ctr, Pharmaceut & Drug Ind Res Inst, Chem Nat Cpds Dept, Cairo 12622, Egypt
Ahmed, Eman Y.
[1
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Awad, Hanem M.
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Natl Res Ctr, Tanning Mat & Leather Technol Dept, Cairo 12622, EgyptNatl Res Ctr, Pharmaceut & Drug Ind Res Inst, Chem Nat Cpds Dept, Cairo 12622, Egypt
Awad, Hanem M.
[2
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Latif, Nehad A. Abdel
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Natl Res Ctr, Pharmaceut & Drug Ind Res Inst, Chem Nat Cpds Dept, Cairo 12622, EgyptNatl Res Ctr, Pharmaceut & Drug Ind Res Inst, Chem Nat Cpds Dept, Cairo 12622, Egypt
Latif, Nehad A. Abdel
[1
]
机构:
[1] Natl Res Ctr, Pharmaceut & Drug Ind Res Inst, Chem Nat Cpds Dept, Cairo 12622, Egypt
[2] Natl Res Ctr, Tanning Mat & Leather Technol Dept, Cairo 12622, Egypt
Aminopeptidase N (APN) is regarded as an attractive target for cancer treatment due to its overexpression in various types of malignancies and its close association with cancer angiogenesis, metastasis and invasion. Herein the authors describe the design, synthesis and biological evaluation of some naturally based pyrazoline derivatives. Among these compounds, the diphenylpyrazole carbothioamide 8 showed significant activity and selectivity index (SI = 4.7) on breast (MCF-7) human cancer cell line and was capable of inhibiting APN with pIC50 value of 4.8, comparable to the reference standard. Further evaluation of derivative 8 against VEGFR2 and MMP9 as biomarkers for angiogenesis and invasion showed that the selected compound had an inhibitory activity on both proteins with pIC50 values of 6.7 and 6.4, respectively. Additionally, the migration ability of cells following treatment with the diphenylpyrazole derivative decreased to record a percentage wound closure of 57.77 for compound 8versus 97.03 for the control. The promising derivative arrested cell growth at the G1 phase inducing early and late apoptosis. Finally, docking and ADMET in silico studies were performed. New naturally based pyrazoline derivatives were investigated as anti-breast cancer agents targeting APN, VEGFR2 and MMP9. The effects on wound healing, cell cycle and apoptosis were evaluated. Docking and ADMET studies were performed as well.
机构:
Al Azhar Univ, Fac Pharm Girls, Dept Pharmaceut Med Chem & Drug Design, Cairo, Egypt
Egyptian Russian Univ, Fac Pharm, Dept Pharmaceut Chem, Cairo, EgyptAl Azhar Univ, Fac Pharm Girls, Dept Pharmaceut Med Chem & Drug Design, Cairo, Egypt
Soliman, Dalia H.
Nafie, Mohamed S.
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Suez Canal Univ, Fac Sci, Dept Chem, Biochem Program, Ismailia 41522, EgyptAl Azhar Univ, Fac Pharm Girls, Dept Pharmaceut Med Chem & Drug Design, Cairo, Egypt
机构:
School of Pharmacy, East China University of Science & TechnologySchool of Pharmacy, East China University of Science & Technology
Guo-Rui Gao
Meng-Yuan Li
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机构:
Division of Anti-tumor Pharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences
Pharmacology and Safety Evaluation Key Laboratory of Tibetan Medicine in Qinghai Province, Northwest Institute of Plateau Biology, Chinese Academy of SciencesSchool of Pharmacy, East China University of Science & Technology
Meng-Yuan Li
Yong-Cong Lv
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Department of Medicinal Chemistry, Shanghai Institute of Materia Medica, Chinese Academy of SciencesSchool of Pharmacy, East China University of Science & Technology
Yong-Cong Lv
Su-Fen Cao
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School of Pharmacy, East China University of Science & TechnologySchool of Pharmacy, East China University of Science & Technology
Su-Fen Cao
Lin-Jiang Tong
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Division of Anti-tumor Pharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of SciencesSchool of Pharmacy, East China University of Science & Technology
Lin-Jiang Tong
Li-Xin Wei
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Pharmacology and Safety Evaluation Key Laboratory of Tibetan Medicine in Qinghai Province, Northwest Institute of Plateau Biology, Chinese Academy of SciencesSchool of Pharmacy, East China University of Science & Technology
Li-Xin Wei
Jian Ding
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Division of Anti-tumor Pharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of SciencesSchool of Pharmacy, East China University of Science & Technology
Jian Ding
Hua Xie
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Division of Anti-tumor Pharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of SciencesSchool of Pharmacy, East China University of Science & Technology
Hua Xie
Wen-Hu Duan
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机构:
School of Pharmacy, East China University of Science & Technology
Department of Medicinal Chemistry, Shanghai Institute of Materia Medica, Chinese Academy of SciencesSchool of Pharmacy, East China University of Science & Technology
机构:
Anhui Med Univ, Sch Pharm, Hefei 230032, Peoples R ChinaAnhui Med Univ, Sch Pharm, Hefei 230032, Peoples R China
Tong, Xu
Chen, Rui
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Anhui Med Univ, Sch Pharm, Hefei 230032, Peoples R ChinaAnhui Med Univ, Sch Pharm, Hefei 230032, Peoples R China
Chen, Rui
Zhang, Tong-Tian
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Anhui Med Univ, Sch Pharm, Hefei 230032, Peoples R ChinaAnhui Med Univ, Sch Pharm, Hefei 230032, Peoples R China
Zhang, Tong-Tian
Han, Yan
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Anhui Med Univ, Sch Pharm, Hefei 230032, Peoples R ChinaAnhui Med Univ, Sch Pharm, Hefei 230032, Peoples R China
Han, Yan
Tang, Wen-Jian
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Anhui Med Univ, Sch Pharm, Hefei 230032, Peoples R ChinaAnhui Med Univ, Sch Pharm, Hefei 230032, Peoples R China
Tang, Wen-Jian
Liu, Xin-Hua
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Anhui Med Univ, Sch Pharm, Hefei 230032, Peoples R China
Nanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Jiangsu, Peoples R ChinaAnhui Med Univ, Sch Pharm, Hefei 230032, Peoples R China
机构:
Menoufia Univ, Chem Dept, Shibin Al Kawm, EgyptAl Azhar Univ, Fac Pharm Boys, Pharmaceut Med Chem & Drug Design Dept, Al Mukhayam Al Daem Str,6th Dist, Cairo 11765, Egypt
Abdel-Rahman, Adel A-H
Omar, Asmaa M.
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Menoufia Univ, Chem Dept, Shibin Al Kawm, EgyptAl Azhar Univ, Fac Pharm Boys, Pharmaceut Med Chem & Drug Design Dept, Al Mukhayam Al Daem Str,6th Dist, Cairo 11765, Egypt
Omar, Asmaa M.
Alswah, Mohamed
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Al Azhar Univ, Fac Pharm, Pharmaceut Organ Chem Dept, Cairo, EgyptAl Azhar Univ, Fac Pharm Boys, Pharmaceut Med Chem & Drug Design Dept, Al Mukhayam Al Daem Str,6th Dist, Cairo 11765, Egypt
Alswah, Mohamed
Saleh, Nashwa M.
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Al Azhar Univ, Dept Chem, Girls Branch, Cairo, EgyptAl Azhar Univ, Fac Pharm Boys, Pharmaceut Med Chem & Drug Design Dept, Al Mukhayam Al Daem Str,6th Dist, Cairo 11765, Egypt
机构:
Beijing Univ Technol, Coll Life Sci & Bioengn, Beijing Key Lab Environm & Viral Oncol, Pingleyuan St 100, Beijing 100124, Peoples R ChinaBeijing Univ Technol, Coll Life Sci & Bioengn, Beijing Key Lab Environm & Viral Oncol, Pingleyuan St 100, Beijing 100124, Peoples R China
Sun, Wuji
Hu, Shengquan
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Beijing Univ Technol, Coll Life Sci & Bioengn, Beijing Key Lab Environm & Viral Oncol, Pingleyuan St 100, Beijing 100124, Peoples R ChinaBeijing Univ Technol, Coll Life Sci & Bioengn, Beijing Key Lab Environm & Viral Oncol, Pingleyuan St 100, Beijing 100124, Peoples R China
Hu, Shengquan
Fang, Shubiao
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Tong Yi Tang Pharmaceut Co Ltd, Suian Ind Pk Zhangpu Cty, Qingdao 363200, Fujian, Peoples R ChinaBeijing Univ Technol, Coll Life Sci & Bioengn, Beijing Key Lab Environm & Viral Oncol, Pingleyuan St 100, Beijing 100124, Peoples R China
Fang, Shubiao
Yan, Hong
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Beijing Univ Technol, Coll Life Sci & Bioengn, Beijing Key Lab Environm & Viral Oncol, Pingleyuan St 100, Beijing 100124, Peoples R ChinaBeijing Univ Technol, Coll Life Sci & Bioengn, Beijing Key Lab Environm & Viral Oncol, Pingleyuan St 100, Beijing 100124, Peoples R China
机构:
Sungkyunkwan Univ, Dept Chem, Suwon 16419, South KoreaSungkyunkwan Univ, Dept Chem, Suwon 16419, South Korea
Salimi, Abbas
Lim, Jong Hyeon
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Sungkyunkwan Univ, Dept Chem, Suwon 16419, South KoreaSungkyunkwan Univ, Dept Chem, Suwon 16419, South Korea
Lim, Jong Hyeon
Jang, Jee Hwan
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Sungkyunkwan Univ, Sch Mat Sci & Engn, Suwon 16419, South Korea
Ucaretron Inc, 3508,40,Simin Daero 365 Beon Gil, Anyang Si 3508, Gyeonggi Do, South KoreaSungkyunkwan Univ, Dept Chem, Suwon 16419, South Korea
Jang, Jee Hwan
Lee, Jin Yong
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Sungkyunkwan Univ, Dept Chem, Suwon 16419, South KoreaSungkyunkwan Univ, Dept Chem, Suwon 16419, South Korea