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Original Research

Novel HDAC/Tubulin Dual Inhibitor: Design, Synthesis and Docking Studies of α-Phthalimido-Chalcone Hybrids as Potential Anticancer Agents with Apoptosis-Inducing Activity

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Pages 3111-3130 | Published online: 03 Aug 2020

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Mai A. E. Mourad, Ayman Abo Elmaaty, Islam Zaki, Ahmed A. E. Mourad, Amal Hofni, Ahmed E. Khodir, Esam M. Aboubakr, Ahmed Elkamhawy, Eun Joo Roh & Ahmed A. Al-Karmalawy. (2023) Novel topoisomerase II/EGFR dual inhibitors: design, synthesis and docking studies of naphtho[2′,3′:4,5]thiazolo[3,2-a]pyrimidine hybrids as potential anticancer agents with apoptosis inducing activity. Journal of Enzyme Inhibition and Medicinal Chemistry 38:1.
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Wenjing Liu, Min He, Yongjun Li, Zhiyun Peng & Guangcheng Wang. (2022) A review on synthetic chalcone derivatives as tubulin polymerisation inhibitors. Journal of Enzyme Inhibition and Medicinal Chemistry 37:1, pages 9-38.
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Articles from other publishers (21)

Yingjie Cui, Jing Zhang & Guifang Zhang. (2024) The Potential Strategies for Overcoming Multidrug Resistance and Reducing Side Effects of Monomer Tubulin Inhibitors for Cancer Therapy. Current Medicinal Chemistry 31:14, pages 1874-1895.
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Sukhmeet Kaur, Jasneet Kaur, Amit Anand, Kirandeep Kaur & Vishal Choudhary. (2024) Chalcones: Effective Agents for Fighting Cancer Across Multiple Cell Lines. ChemistrySelect 9:9.
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Jing Nie, Huina Wu, Yepeng Luan & Jiyong Wu. (2024) The Development of HDAC and Tubulin Dual-Targeting Inhibitors for Cancer Therapy. Mini-Reviews in Medicinal Chemistry 24:5, pages 480-490.
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Mohammad Mahboubi-Rabbani, Rosa Zarei, Mehdi Baradaran, Maryam Bayanati & Afshin Zarghi. (2024) Chalcones as Potential Cyclooxygenase-2 Inhibitors: A Review. Anti-Cancer Agents in Medicinal Chemistry 24:2, pages 77-95.
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Aliki Drakontaeidi & Eleni Pontiki. (2023) A Review on Molecular Docking on HDAC Isoforms: Novel Tool for Designing Selective Inhibitors. Pharmaceuticals 16:12, pages 1639.
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Reham A. Mohamed-Ezzat, Benson M. Kariuki & Aladdin M. Srour. (2023) Synthesis, crystal structure and in vitro anti-proliferative activity of 2-[(4-acetylphenyl)carbamoyl]phenyl acetate . Acta Crystallographica Section E Crystallographic Communications 79:11, pages 999-1002.
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Jiahui Yang, Jianmei Lv, Shuxian Cheng, Tingyu Jing, Tenghao Meng, Dezhen Huo, Xin Ma & Ran Wen. (2023) Recent Progresses in Chalcone Derivatives as Potential Anticancer Agents. Anti-Cancer Agents in Medicinal Chemistry 23:11, pages 1265-1283.
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Vijay K. Patel, Ekta Shirbhate, Priya Tiwari, Rakesh Kore, Ravichandran Veerasamy, Achal Mishra & Harish Rajak. (2023) Multi-targeted HDAC Inhibitors as Anticancer Agents: Current Status and Future Prospective. Current Medicinal Chemistry 30:24, pages 2762-2795.
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Fernando Ferreira Leite, Natália Ferreira de Sousa, Bruno Hanrry Melo de Oliveira, Gabrielly Diniz Duarte, Maria Denise Leite Ferreira, Marcus Tullius Scotti, José Maria Barbosa Filho, Luís Cezar Rodrigues, Ricardo Olímpio de Moura, Francisco Jaime Bezerra Mendonça-Junior & Luciana Scotti. (2023) Anticancer Activity of Chalcones and Its Derivatives: Review and In Silico Studies. Molecules 28:10, pages 4009.
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Mohammed M. Amin, Gamal El-Din A. Abuo-Rahma, Montaser Sh. A. Shaykoon, Adel A. Marzouk, Mohammed A.S. Abourehab, Roshdy E. Saraya, Mohamed Badr, Ahmed M. Sayed & Eman A.M. Beshr. (2023) Design, synthesis, cytotoxic activities, and molecular docking of chalcone hybrids bearing 8-hydroxyquinoline moiety with dual tubulin/EGFR kinase inhibition. Bioorganic Chemistry 134, pages 106444.
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Amr Ahmed WalyEldeen, Salwa Sabet, Haidan M. El-Shorbagy, Ismail A. Abdelhamid & Sherif Abdelaziz Ibrahim. (2023) Chalcones: Promising therapeutic agents targeting key players and signaling pathways regulating the hallmarks of cancer. Chemico-Biological Interactions 369, pages 110297.
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Pavithra Palanikarasu, Remya Ramachandran Surajambika & Natarajan Ramalakshmi. (2022) Chalcones and Flavones as Multifunctional Anticancer Agents- A Comprehensive Review. Current Bioactive Compounds 18:10.
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María Ovejero-Sánchez, Gloria Asensio-Juárez, Myriam González, Pilar Puebla, Miguel Vicente-Manzanares, Rafael Pélaez, Rogelio González-Sarmiento & Ana Belén Herrero. (2022) Panobinostat Synergistically Enhances the Cytotoxicity of Microtubule Destabilizing Drugs in Ovarian Cancer Cells. International Journal of Molecular Sciences 23:21, pages 13019.
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Huajian Zhu, Yuchen Tan, Chen He, Yang Liu, Yiping Duan, Wenjian Zhu, Tiandong Zheng, Dahong Li, Jinyi Xu, Dong-Hua Yang, Zhe-Sheng Chen & Shengtao Xu. (2022) Discovery of a Novel Vascular Disrupting Agent Inhibiting Tubulin Polymerization and HDACs with Potent Antitumor Effects. Journal of Medicinal Chemistry 65:16, pages 11187-11213.
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Tarfah Al-Warhi, Adil Aldhahrani, Fayez Althobaiti, Eman Fayad, Ola A. Abu Ali, Sarah Albogami, Ali H. Abu Almaaty, Amgad I. M. Khedr, Syed Nasir Abbas Bukhari & Islam Zaki. (2022) Design, Synthesis and Cytotoxic Activity Evaluation of Newly Synthesized Amides-Based TMP Moiety as Potential Anticancer Agents over HepG2 Cells. Molecules 27:12, pages 3960.
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Navanath Kumbhar, Snehal Nimal, Sagar Barale, Subodh Kamble, Rohit Bavi, Kailas Sonawane & Rajesh Gacche. (2022) Identification of novel leads as potent inhibitors of HDAC3 using ligand-based pharmacophore modeling and MD simulation. Scientific Reports 12:1.
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Rama Rao Malla, Satyalakshmi Siragam, Vasudha Dadi & Balachandrika Seetini. (2022) Natural Chalcones and Their Derivatives Target the Tumor Microenvironment in Colon Cancer. Critical Reviews in Immunology 42:6, pages 27-39.
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Yingge Wang, Moran Sun, Yuyang Wang, Jinling Qin, Yixin Zhang, Yingyue Pang, Yongfang Yao, Hua Yang & Yongtao Duan. (2021) Discovery of novel tubulin/HDAC dual-targeting inhibitors with strong antitumor and antiangiogenic potency. European Journal of Medicinal Chemistry 225, pages 113790.
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Xiang Qiu, Lv Zhu, Huan Wang, Yan Tan, Zhuang Yang, Linyu Yang & Li Wan. (2021) From natural products to HDAC inhibitors: An overview of drug discovery and design strategy. Bioorganic & Medicinal Chemistry 52, pages 116510.
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Xiaopeng Peng, Jingxuan Chen, Ling Li, Zhiqiang Sun, Jin Liu, Yichang Ren, Junli Huang & Jianjun Chen. (2021) Efficient Synthesis and Bioevaluation of Novel Dual Tubulin/Histone Deacetylase 3 Inhibitors as Potential Anticancer Agents. Journal of Medicinal Chemistry 64:12, pages 8447-8473.
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Yang Ouyang, Juanjuan Li, Xinyue Chen, Xiaoyu Fu, Si Sun & Qi Wu. (2021) Chalcone Derivatives: Role in Anticancer Therapy. Biomolecules 11:6, pages 894.
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