Article
Biochemistry & Molecular Biology
Serdar Burmaoglu, Derya Aktas Anil, Arzu Gobek, Deryanur Kilic, Derya Yetkin, Nizami Duran, Oztekin Algul
Summary: This study describes a series of new chalcones that contain fluorine atoms on the B ring and exhibit antiproliferative activity against human tumor cells. Some of these compounds showed potent antiproliferative effects on certain tumor cells without cytotoxicity towards normal cells. The antiproliferative and cytotoxic effects were mediated through apoptosis. Molecular docking study suggested that these compounds interfere with cell division.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2022)
Article
Biochemistry & Molecular Biology
Zuzana Kudlickova, Radka Michalkova, Aneta Salayova, Marian Ksiazek, Maria Vilkova, Slavka Bekesova, Jan Mojzis
Summary: This research reports the synthesis, anticancer, and antioxidant activities of a series of indole-derived hybrid chalcones. Chalcone 18c exhibited selective activity against cancer cells and no toxicity to non-cancer cells. The 3,4-dihydroxychalcone derivatives showed properties as a lead compound for both antioxidant and antiproliferative activity.
Article
Chemistry, Organic
Jinjing Li, Pingping Fan, Yuxiao Liu, Yan Zhao, Chengyang Shi, Shujing Zhou, Hongbin Qiu
Summary: A series of novel 1,2,4-triazole-chalcone compounds were successfully designed and synthesized using molecular hybridization strategy. The anti-proliferative activities of these compounds against four cancer cell lines were evaluated, and compound 10o showed selectivity towards colon cancer cells while compound 10q exhibited good anti-proliferative activity against lung cancer cells.
HETEROCYCLIC COMMUNICATIONS
(2023)
Article
Oncology
Mohamed Hisham, Heba A. Hassan, Hesham A. M. Gomaa, Bahaa G. M. Youssif, Alaa M. Hayalah, Mohamed Abdel-Aziz
Summary: This study synthesized a series of novel compounds with anticancer activity and the potential to target specific cancer genes. The results showed that one of the hybrid compounds had significant effects on cell cycle and cell apoptosis, and exhibited good binding ability to the active site of EGFR.
ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Physical
Mohamed Hisham, Heba A. Hassan, Hesham A. M. Gomaa, Bahaa G. M. Youssif, Alaa M. Hayallah, Mohamed Abdel-Aziz
Summary: A new series of quinazoline-4-one/chalcone hybrids, 7-26, were synthesized and tested as EGFR inhibitors with antiproliferative activity. Three compounds showed the greatest antiproliferative activity and were the most potent EGFR inhibitors. These three compounds improved the levels of active caspase-3, 8, and 9, induced cytochrome c and Bax levels, and down regulated Bcl_2 levels. The most active inhibitors docked well inside EGFR active sites.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Biochemistry & Molecular Biology
Zuleima Blanco, Esteban Fernandez-Moreira, Michael R. Mijares, Carmen Celis, Gricelis Martinez, Juan B. De Sanctis, Sona Gurska, Petr Dzubak, Marian Hajduch, Ali Mijoba, Yael Garcia, Xenon Serrano, Nahum Herrera, Jhonny Correa-Abril, Yonathan Parra, Jorge Angel, Hegira Ramirez, Jaime E. Charris
Summary: This research reports 16 synthetic chalcone derivatives with potential therapeutic activities against parasites and cancer cells.
Article
Biochemistry & Molecular Biology
Aliaa M. Mohassab, Heba A. Hassan, Dalia Abdelhamid, Ahmed M. Gouda, Bahaa G. M. Youssif, Hiroshi Tateishi, Mikako Fujita, Masami Otsuka, Mohamed Abdel-Aziz
Summary: A series of new quinoline/chalcone hybrids containing 1,2,4-triazole moiety were designed and synthesized in this study, showing moderate to good activity against various cancer cell lines. Some of these compounds exhibited promising antiproliferative activities and displayed high binding affinities in inhibiting EGFR and BRAF(V600E) kinases.
BIOORGANIC CHEMISTRY
(2021)
Article
Plant Sciences
Noemie Saraux, Deniza Imeri, Luis Quiros-Guerrero, Soumana Karimou, Philippe Christen, Muriel Cuendet
Summary: Ipomoea asarifolia, a herbaceous plant from the Convolvulaceae family, has shown antiproliferative activity against multiple myeloma cells. A total of 15 compounds were isolated from the plant, with compound 3 demonstrating the most potent activity with an IC50 value of 3.0 μM against RPMI 8226 cells.
JOURNAL OF NATURAL PRODUCTS
(2022)
Article
Biochemistry & Molecular Biology
Isis A. Y. Ventura-Salazar, Francisco J. Palacios-Can, Leticia Gonzalez-Maya, Jessica Nayelli Sanchez-Carranza, Mayra Antunez-Mojica, Rodrigo Said Razo-Hernandez, Laura Alvarez
Summary: In this work, new chimeric compounds were designed and synthesized from the natural cytotoxic chalcone 2',4' -dihydroxychalcone (2',4' -DHC, A) in combination with cinnamic acids. Two quantitative structure-activity relationship (QSAR) models were developed to study the anti-cancer activities of the chimeric compounds against human breast cancer MCF-7. The models showed good predictive ability and were validated through synthesis and in vitro evaluation.
Article
Chemistry, Medicinal
Marco Mellado, Mauricio Reyna-Jeldes, Caroline Weinstein-Oppenheimer, Alejandra A. Covarrubias, Luis F. Aguilar, Claudio Coddou, Jaime Mella, Mauricio A. Cuellar
Summary: Neuroblastoma, a common cancer in infants, has limited response to traditional chemotherapy. This study focused on the development of new compounds with greater activity and selectivity against neuroblastoma. Through the synthesis of chalcones and the use of quantitative structure-activity relationship models, 16 new molecules were designed and synthesized, showing promising antiproliferative activity and selectivity against neuroblastoma cells.
ARCHIV DER PHARMAZIE
(2022)
Article
Chemistry, Medicinal
Zhichao Du, Guolong Li, Haixia Ge, Xiaoyang Zhou, Jian Zhang
Summary: The study systematically evaluated the impact of neoglycosylation on the anticancer activities and selectivity of steroids, revealing that neoglycosides displayed potential antiproliferative activities against HepG2 cells and induced morphological changes, cell cycle arrest, and apoptosis, possibly associated with enhanced HMGB1 expression. This suggests that neoglycosylation of steroids could be a promising strategy for discovering potential antiproliferative agents.
Article
Biochemistry & Molecular Biology
Edua Kovacs, Hazhmat Ali, Renata Minorics, Peter Traj, Vivien Resch, Gabor Paragi, Bella Bruszel, Istvan Zupko, Erzsebet Mernyak
Summary: Novel 13 alpha-estrone derivatives were synthesized through direct arylation of the phenolic hydroxy function. The antiproliferative activities of the synthesized compounds against human cancer cell lines were investigated, and the quinoline derivative showed substantial activity with low IC50 values. Disturbance of tubulin polymerization was confirmed, and computational calculations revealed significant interactions of the quinoline derivative with the taxoid binding site of tubulin.
Article
Pharmacology & Pharmacy
Zdenek Travnicek, Tomas Malina, Jan Vanco, Marek Sebela, Zdenek Dvorak
Summary: The paper describes the synthesis and characterization of six heteroleptic copper(II) complexes with different ligands. The results showed that complex 2 exhibited high cytotoxicity against cancer cells, while showing low toxicity against healthy cells. Further experiments revealed that complex 2 induced apoptosis and autophagy in A2780 cancer cells through the activation of caspases 3/7, ROS overproduction, and autophagy induction.
Article
Chemistry, Medicinal
Fatma Fouad Hagar, Samar H. Abbas, Dalia Abdelhamid, Hesham A. M. Gomaa, Bahaa G. M. Youssif, Mohamed Abdel-Aziz
Summary: A series of new 1,3,4-oxadiazole-chalcone/benzimidazole hybrids were synthesized and investigated for their antiproliferative activities. Compounds 9g-i and their oxygen isosteres, 10f-h, exhibited promising antiproliferative activities with IC50 values ranging from 0.80 to 2.27 μM.
ARCHIV DER PHARMAZIE
(2023)
Review
Biochemistry & Molecular Biology
Ajay Mallia, Joseph Sloop
Summary: Synthesis of hybrid chalcones with heteroaromatic components, especially utilizing green chemistry principles, is a significant method to prepare diverse heterocyclic molecules with medicinal and industrial properties.
Article
Biochemistry & Molecular Biology
Dong-Jun Fu, Xin-Xin Cui, Ting Zhu, Yan-Bing Zhang, Yang-Yang Hu, Li-Rong Zhang, Sheng-Hui Wang, Sai-Yang Zhang
Summary: The novel indole derivative V7 showed potent inhibitory activity against MGC803 cancer cells by inhibiting colony formation, inducing apoptosis, and arresting cell cycle at G2/M phase. Moreover, V7 also inhibited the NEDDy-lation pathway and MAPK pathway against MGC803 cells.
BIOORGANIC CHEMISTRY
(2021)
Review
Oncology
Hong-Li Li, Qian-Yu Li, Min-Jie Jin, Chao-Fan Lu, Zhao-Yang Mu, Wei-Yi Xu, Jian Song, Yan Zhang, Sai-Yang Zhang
Summary: The Hippo pathway can promote tumor invasion and metastasis by regulating the expression of target genes. YAP/TAZ, as the core molecules of the Hippo pathway, interact with TEADs to regulate the expression of target genes related to tumor metastasis and invasion. Target genes induced by YAP/TAZ can lead to invasive pseudopodia formation, reduced intercellular adhesion, ECM degradation, EMT, or indirectly promote invasion and metastasis through other signaling pathways.
JOURNAL OF CANCER RESEARCH AND CLINICAL ONCOLOGY
(2021)
Article
Chemistry, Medicinal
Ya-Xin Sun, Jian Song, Li-Jun Kong, Bei-Bei Sha, Xin-Yi Tian, Xiu-Juan Liu, Tao Hu, Ping Chen, Sai-Yang Zhang
Summary: This study designed a series of novel bis-substituted aromatic amide dithiocarbamate derivatives as tubulin inhibitors with potential anticancer activities. Among them, compound 20q exhibited the most potent antiproliferative activity and was identified as a tubulin inhibitor targeting the colchicine binding site.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Chong Liu, Jian Song, Xin-Xin Cui, Wen-Bo Liu, Yin-Ru Li, Guang-Xi Yu, Xin-Yi Tian, Ya-Feng Wang, Yang Liu, Sai-Yang Zhang
Summary: In this study, novel 1,2,4-triazine-chalcone hybrids were designed and synthesized, with compound 9l showing significant antiproliferative activity against various cancer cell lines via the ROS-ERK-DR5 axis. Compound 9l effectively inhibited gastric cancer cell growth in vitro and in vivo, making it a promising anti-gastric cancer agent.
ARABIAN JOURNAL OF CHEMISTRY
(2022)
Article
Pharmacology & Pharmacy
Yin-Ru Li, Fang-Fang Liu, Wen-Bo Liu, Yi-Fan Zhang, Xin-Yi Tian, Xiang-Jing Fu, Yan Xu, Jian Song, Sai-Yang Zhang
Summary: In this study, a novel aromatic amide derivative SY-65 was identified as a dual inhibitor of tubulin and histone deacetylase 1, showing potent anticancer activity in vitro and in vivo. The compound exhibited excellent antiproliferative activity against multiple cancer cell lines and demonstrated inhibition of tubulin polymerization and HDAC1 activity. It also induced cell cycle arrest and apoptosis in cancer cells. This study highlights the potential of compound SY-65 as a novel tubulin/HDAC1 inhibitor for future cancer therapeutics.
BIOCHEMICAL PHARMACOLOGY
(2022)
Article
Chemistry, Medicinal
Jian Song, Yong-Feng Guan, Wen-Bo Liu, Chun-Hong Song, Xin-Yi Tian, Ting Zhu, Xiang-Jing Fu, Ying-Qiu Qi, Sai-Yang Zhang
Summary: This study designed, synthesized, and evaluated novel coumarin-indole derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. Compound MY-413 showed potent inhibitory activities against gastric cancer cells, inhibited tubulin polymerization, and MAPK signaling pathway, induced cell apoptosis and proliferation inhibition both in vitro and in vivo. In addition, MY-413 significantly inhibited tumor growth in xenograft tumor models without obvious toxicity. Overall, MY-413 is a promising lead compound for further investigation as a potential anti-gastric cancer agent.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Guang-Xi Yu, Ying Hu, Wei-Xin Zhang, Xin-Yi Tian, Sai-Yang Zhang, Yan Zhang, Shuo Yuan, Jian Song
Summary: In this study, a series of [1,2,4]triazolo[1,5-a]pyrimidine indole derivatives were designed and synthesized as anticancer agents. Compound H12 showed the most potent antiproliferative activities against MGC-803, HCT-116, and MCF-7 cells, and it inhibited the ERK signaling pathway, induced cell apoptosis, and regulated cell cycle-related proteins.
Article
Chemistry, Medicinal
Jian Song, Sheng-Hui Wang, Chun-Hong Song, Wei-Xin Zhang, Jun-Xia Zhu, Xin-Yi Tian, Xiang-Jing Fu, Yan Xu, Cheng-Yun Jin, Sai-Yang Zhang
Summary: The novel compound showed potent antiproliferative activities by targeting the colchicine binding site of tubulin and activating the Hippo pathway, making it a promising agent for cancer therapy.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Review
Biochemistry & Molecular Biology
Hong-Li Li, Lu-Lu Dong, Min-Jie Jin, Qian-Yu Li, Xiao Wang, Mei-Qi Jia, Jian Song, Sai-Yang Zhang, Shuo Yuan
Summary: Neuroblastoma exhibits heterogeneity and can spontaneously degenerate into benign tumors. However, the prognosis for high-risk types remains unsatisfactory despite intensive treatments. Abnormal amplification and high-level expression of the MYCN gene are positively correlated with malignant progression, poor prognosis, and mortality of neuroblastoma. This article explores the role of N-Myc, the gene expression product of MYCN, on target genes related to the cell cycle and reveals its regulatory network in promoting tumor proliferation and malignant progression. It aims to provide ideas and direction for the research and development of drugs targeting N-Myc and its downstream target genes.
Article
Biochemistry & Molecular Biology
Xiu-Juan Liu, Hong-Cheng Zhao, Su-Juan Hou, Hao-Jie Zhang, Lei Cheng, Shuo Yuan, Li-Rong Zhang, Jian Song, Sai-Yang Zhang, Shi-Wu Chen
Summary: Vascular epidermal growth factor receptor-2 (VEGFR-2) is an important protein involved in regulating endothelial cell function and angiogenesis. Aberrant expression of VEGFR-2 is associated with cancer, and VEGFR-2 inhibitors are approved for clinical use in cancer therapy. However, their efficacy is limited, leading to the need for new strategies. Recent research has focused on dual-target therapy, inhibiting VEGFR-2 and other targets simultaneously, to improve therapeutic outcomes. This review discusses the structure, functions, and development of multi-target VEGFR-2 inhibitors as novel anticancer agents.
BIOORGANIC CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Qi-Sheng Ma, Yi-Fan Zhang, Cheng-Yang Li, Wei-Xin Zhang, Lu Yuan, Jin-Bo Niu, Jian Song, Sai-Yang Zhang, Hong-Min Liu
Summary: Histone lysine specific demethylase 1 (LSD1), an important epigenetic regulator, is a promising target for anticancer drug discovery. This study designed and synthesized a series of tranylcypromine-based derivatives, among which compound 12u exhibited the most potent inhibitory potency on LSD1 and showed effective antiproliferative effects on MGC-803, KYSE450, and HCT-116 cells. Further investigations demonstrated that compound 12u directly targeted LSD1, leading to increased levels of mono-/bi-methylation of H3K4 and H3K9. Additionally, compound 12u induced apoptosis, differentiation, and inhibition of migration and cell stemness in MGC-803 cells, suggesting its potential as an active LSD1 inhibitor for gastric cancer.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Review
Biochemistry & Molecular Biology
Yi-Fan Zhang, Jiao Huang, Wei-Xin Zhang, Yun-He Liu, Xiao Wang, Jian Song, Cheng-Yun Jin, Sai-Yang Zhang
Summary: The microtubule system is a crucial target for cancer treatment and various microtubule targeting agents have been approved for tumor therapy. Tubulin degradation agents show potential in overcoming drug resistance and reducing neurotoxicity, and natural drugs can specifically degrade tubulin in tumor cells with good biosafety. Small molecules have been designed to promote tubulin degradation for cancer treatment, and this study reviews the degradation mechanism and important functional groups of chemically synthesized compounds to aid in the design of tubulin degradation.
BIOORGANIC CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Jian Song, Shu-Yu Wang, Xiao Wang, Mei-Qi Jia, Xin-Yi Tian, Xiang-Jing Fu, Cheng-Yun Jin, Sai-Yang Zhang
Summary: In this study, a new coumarin-dihydroquinoxalone derivative, MY-673, was designed, synthesized, and evaluated for its anticancer potency. The results showed that MY-673 was a potent CBSI, inhibiting tubulin polymerization and significantly inhibiting the growth of cancer cells. It was also found to inhibit the ERK and TGF-beta/SMAD signaling pathways, leading to inhibition of cell proliferation, migration, and induction of apoptosis.
BIOORGANIC CHEMISTRY
(2023)
Review
Chemistry, Medicinal
Wei-Xin Zhang, Jiao Huang, Xin-Yi Tian, Yun-He Liu, Mei-Qi Jia, Wang Wang, Cheng-Yun Jin, Jian Song, Sai-Yang Zhang
Summary: Histone deacetylases (HDACs) are a new class of anticancer targets that regulate gene expression by catalyzing histone deacetylation. Dual-target drugs that simultaneously intervene with multiple tumor-related targets are being researched to improve treatment effects. Inhibiting HDAC along with other targets has been reported to enhance therapeutic effects and overcome multidrug resistance.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Organic
Shenghui Wang, Yongfeng Guan, Xiujuan Liu, Xinying Yuan, Guangxi Yu, Yinru Li, Yanbing Zhang, Jian Song, Wen Li, Saiyang Zhang
Summary: A series of novel quinoline-indole derivatives were designed and synthesized, among which compound 9b exhibited potent inhibitory activity against various cancer cell lines. Mechanism studies showed that compound 9b exerted its anticancer effects through inducing apoptosis, down-regulating apoptosis-related proteins, and arresting cells at G2/M phase.
CHINESE JOURNAL OF ORGANIC CHEMISTRY
(2021)
