Article
Pharmacology & Pharmacy
Long-fei Mao, Zhen-Zhen Wang, Qiong Wu, Xiaojie Chen, Jian-Xue Yang, Xin Wang, Yue-Ming Li
Summary: Nineteen erlotinib derivatives bearing different 1,2,3-triazole moieties were designed, synthesized, and evaluated for their potential against different cancer cell lines. Compound 3d showed the most promising inhibitory activity and suppressed cancer cell proliferation through the EGFR-TK pathway.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Chemistry, Multidisciplinary
Weidong Jia, Jingjing Wang, Chengxi Wei, Ming Bian, Shuyin Bao, Lijun Yu
Summary: A new series of quinoxalinone derivatives were designed and evaluated for their hypoglycemic activity. Compounds 5i and 6b showed stronger hypoglycemic effects compared to the lead compounds and were comparable to the positive control Pioglitazone. They exerted hypoglycemic effects by alleviating cellular oxidative stress and modulating the interactions among GLUT4, SGLT2, and GLUT1 proteins. Compound 6b showed better cellular oxidative stress alleviation and binding for most of the screening targets compared to 5i. Overall, compound 6b is a potential lead compound with hypoglycemic activity.
FRONTIERS IN CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Anna Jaromin, Anna Czopek, Silvia Parapini, Nicoletta Basilico, Ernest Misiak, Jerzy Gubernator, Agnieszka Zagorska
Summary: This study synthesized novel derivatives and conducted preliminary physicochemical characterization, showing strong inhibitory effects against Plasmodium falciparum, particularly the chloroquine-resistant strain. These molecules exhibited no hemolytic action on human erythrocytes and low toxicity on mammalian cell line.
Article
Biochemistry & Molecular Biology
Dawid Lazewski, Malgorzata Kucinska, Edward Potapskiy, Joanna Kuzminska, Lukasz Popenda, Artur Tezyk, Tomasz Goslinski, Marcin Wierzchowski, Marek Murias
Summary: This study has successfully developed a series of curcumin derivatives through modifications. The results showed that one derivative with PEG chains and a BF2 moiety exhibited higher cytotoxicity against bladder cancer cells and stronger anticancer effects under hypoxic conditions. However, PEGylation did not improve cellular uptake, and the lack of serum proteins limited intracellular uptake. The regulation of cell cycle and stress-related proteins may be involved in the anticancer mechanism. In conclusion, PEGylated curcumin derivatives are more effective anti-bladder cancer drugs than the parent compound, and derivative 5 deserves further investigation to elucidate its anticancer mechanism under hypoxic conditions.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Corina Popovici, Cristina-Maria Pavel, Valeriu Sunel, Corina Cheptea, Dan Gheorghe Dimitriu, Dana Ortansa Dorohoi, Diana David, Valentina Closca, Marcel Popa
Summary: The research focused on the impact of acyl-thiosemicarbazide residue reaction extension on the structure of 5-nitrobenzimidazole, aiming to enhance the applicative potential of new thiosemicarbazide derivatives in biochemistry and confirming the tuberculostatic activity of three compounds against Mycobacterium tuberculosis through in vitro biological tests.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Agronomy
Wei Zhang, Shengxin Guo, Ya Wang, Yikun Wu, Lijiao Yu, Jian Wu
Summary: Novel compounds S1-S28 were synthesized and evaluated for their curative effects against CMV. Compound S8 showed a strong binding affinity to CMV-coat protein and impacted the self-assemble of CMV particles, making it a potential lead compound for discovering a new anti-plant virus candidate.
PEST MANAGEMENT SCIENCE
(2023)
Article
Chemistry, Medicinal
Loida O. Casalme, Keisuke Katayama, Yoshiki Hayakawa, Kensuke Nakamura, Arisa Yamauchi, Yasuyuki Nogata, Erina Yoshimura, Fuyuhiko Matsuda, Taiki Umezawa
Summary: This study successfully synthesized some derivatives of dolastatin 16 through second-generation synthesis and evaluated their antifouling activity. The results showed that certain small fragments exhibited potent inhibitory activity against the settlement of cypris larvae.
Article
Biochemistry & Molecular Biology
Jingjing Zhang, Wenqiang Tan, Pengzhuo Zhao, Yingqi Mi, Zhanyong Guo
Summary: This study synthesized a series of novel carboxymethyl inulin derivatives and evaluated their antioxidant and antibacterial activities. The derivatives containing thiosemicarbazide salts showed significant improvement in antioxidant and antibacterial activities. Furthermore, these derivatives demonstrated good biocompatibility and low toxicity. These findings highlight the potential importance of these carboxymethyl inulin derivatives in food and medical applications.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2022)
Article
Biochemistry & Molecular Biology
Lukasz Banach, Lukasz Janczewski, Jakub Kajdanek, Katarzyna Milowska, Joanna Kolodziejczyk-Czepas, Grzegorz Galita, Wioletta Rozpedek-Kaminska, Ewa Kucharska, Ireneusz Majsterek, Beata Kolesinska
Summary: Eight dipeptides containing antifibrinolytic agents were successfully synthesized using a three-step process. Hemolysis tests and clotting tests showed that these compounds had no significant effects on blood components and clotting time. The clot formation and fibrinolysis assay revealed that two of the compounds exhibited high activity in the plasma coagulation cascade and fibrinolytic efficiency. The cytotoxicity and genotoxicity evaluation demonstrated that the synthesized dipeptides caused minimal damage to cells and DNA.
Article
Biochemistry & Molecular Biology
Jinfeng Chen, Yimou Yang, Yujie Zhou, Yang Wei, Rui Zhu, Shaojun Zheng
Summary: Efficient agricultural antifungal lead compounds were searched by designing, synthesizing, and evaluating 39 Chimonanthus praecox derivatives. Compounds b15 and b17 were identified as the most promising candidates for further study due to their excellent antifungal activities against Phytophthora infestans and Sclerotinia sclerotiorum, with minimum inhibitory concentrations of 1.95 µg/mL for both pathogens.
Article
Chemistry, Multidisciplinary
Mohamed A. A. Radwan, Osamah Al Rugaie, Waleed Al Abdulmonem, Mohammad Y. Alfaifi, Serag Eldin Elbehairi
Summary: The study described the synthesis of a new series of indolylpyrrole derivatives and tested their in vitro cytotoxic activity against prostate cancer cells, ovarian cancer cells, and colorectal cancer cells. Some compounds exhibited potent anticancer activity, laying the groundwork for further exploration of these compounds as antiproliferative agents.
ARABIAN JOURNAL OF CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Hisashi Takada, Naoki Takizawa, Shouta Shibasaki, Hiroki Asaba, Masayuki Igarashi, Masakatsu Shibasaki, Yoshiaki Takahashi
Summary: Through screening, a C-nucleoside antibiotic formycin A with strong anti-influenza virus activity was discovered. The modification of the C-7 position of the pyrazolopyrimidine ring and the sugar moiety greatly affected the activity.
BIOORGANIC & MEDICINAL CHEMISTRY
(2022)
Article
Pharmacology & Pharmacy
Xi-Xi Hou, Long-Fei Mao, Yajie Guo, Chaoxuan Lou, Lan Wang, Rui-Fang Li, Huili Wang, San-Qiang Li, Jian-Xue Yang
Summary: Based on structural modification, novel dolutegravir derivatives containing 1,2,3-triazole moieties with different substituted groups were synthesized. The derivatives exhibited good inhibitory effects on A549 cells, with compounds 4b and 4g being the most effective, showing IC50 values of 8.72 +/- 0.11 mu M and 12.97 +/- 0.32 mu M, respectively. Furthermore, compound 4g induced apoptosis and clonal suppression in A549 tumor cells, activated LC3 signaling pathway to induce autophagy, and activated gamma-H2AX signaling pathway to induce DNA damage in tumor cells.
FRONTIERS IN PHARMACOLOGY
(2023)
Article
Pharmacology & Pharmacy
Zuzanna Rzepka, Ewa Bebenek, Elwira Chrobak, Dorota Wrzesniok
Summary: The synthesized new 28-indole-betulin derivatives showed promising anticancer activity, particularly against MCF-7 breast cancer cells, possibly through inducing apoptosis.
Article
Biochemistry & Molecular Biology
Sergey N. Adamovich, Igor A. Ushakov, Elizaveta N. Oborina, Svetlana V. Lukyanova, Vladislav Y. Komarov
Summary: The biologically active compound 3-aminopropylsilatrane underwent an aza-Michael reaction to form mono- and diadducts containing functional groups. Characterization of these compounds revealed their bioavailability and druglike properties, as well as their antineoplastic and macrophage-colony-stimulating activity. The synthesized compounds exhibited inhibitory and stimulating effects on the growth of pathogenic bacteria in high and low concentrations, respectively.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Medicinal
Osama I. El-Sabbagh, Mohamed A. Shabaan, Hanan H. Kadry, Ehab Saad Al-Din
ARCHIV DER PHARMAZIE
(2010)
Article
Chemistry, Medicinal
Afaf K. Elansary, Ashraf A. Moneer, Hanan H. Kadry, Ehab M. Gedawy
ARCHIVES OF PHARMACAL RESEARCH
(2012)
Article
Biochemistry & Molecular Biology
Ghaneya Sayed Hassan, Hanan Hassan Kadry, Sahar Mahmoud Abou-Seri, Mamdouh Moawad Ali, Abeer Essam El-Din Mahmoud
BIOORGANIC & MEDICINAL CHEMISTRY
(2011)
Article
Biochemistry & Molecular Biology
Azza T. Taher, Hanan H. Kadry, Marco Allara, Vincenzo Di Marzo, Ashraf H. Abadi, Khaled A. Abouzid
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2013)
Article
Chemistry, Medicinal
Afaf K. Elansary, Hanan H. Kadry, Eman M. Ahmed, Amr Sayed Motawi Sonousi
MEDICINAL CHEMISTRY RESEARCH
(2012)
Article
Chemistry, Medicinal
Afaf K. Elansary, Hanan H. Kadry, Eman M. Ahmed, Amr Sayed Motawi Sonousi
MEDICINAL CHEMISTRY RESEARCH
(2012)
Article
Chemistry, Medicinal
Hanan H. Kadry
MEDICINAL CHEMISTRY RESEARCH
(2014)
Article
Chemistry, Multidisciplinary
Afaf K. Elansary, Ashraf A. Moneer, Hanan H. Kadry, Ehab M. Gedawy
JOURNAL OF CHEMICAL RESEARCH
(2014)
Article
Chemistry, Medicinal
Hanan M. Refaat, Omneya M. Khalil, Hanan H. Kadry
ARCHIVES OF PHARMACAL RESEARCH
(2007)
Article
Chemistry, Medicinal
Shuang Mei, Su Jiang, Yuting Wang, Han Jing, Peng Yang, Miao-Miao Niu, Jindong Li, Kai Yuan, Yan Zhang
Summary: This study identifies a dual-targeting peptide, AP-1, that effectively inhibits variants of concern (VOCs) of SARS-CoV-2 without impairing host cell viability. The findings suggest that AP-1 could be a promising broad-spectrum agent for treating emerging VOCs of SARS-CoV-2.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Hyeonjun Lee, Ju Yeon Lee, Hyunsoo Jang, Hye Young Cho, Minhee Kang, Sang Hyun Bae, Suin Kim, Eunji Kim, Jaebong Jang, Jin Young Kim, Young Ho Jeon
Summary: By using liquid chromatography-tandem mass spectrometry and nuclear magnetic resonance experiments, we identified new chemical moieties that bind to the target sites of the protein of interest, allowing for reversible binding and protein degradation. This method has the potential to expand the application of PROTAC technology.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Yingying Li, Xiyou Du, Xinru Kong, Yuelin Fang, Zhijing He, Dongzhu Liu, Hang Wu, Jianbo Ji, Xiaoye Yang, Lei Ye, Guangxi Zhai
Summary: This study proposes a novel nanoplatform based on the autophagy cascade to overcome the obstacles in chemo-immunotherapy. The platform combines chemotherapy and starvation therapy to initiate pro-death autophagy and enhance antigen presentation, while also remodeling the immunosuppressive tumor microenvironment. Furthermore, the study discovers a new therapeutic direction for the respiration inhibitor 3-bromopyruvic acid (3BP) in cancer treatment. Overall, this study offers an opportunity to improve antitumor efficacy and boost immune responses.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Bingsi Wang, Mingxu Ma, Yusen Dai, Pengfei Yu, Liang Ye, Wenyan Wang, Chunjie Sha, Huijie Yang, Yingjie Yang, Yunjing Zhu, Lin Dong, Shujuan Wei, Linlin Wang, Jingwei Tian, Hongbo Wang
Summary: Breast cancer is a common malignant tumor in women, and drug resistance remains a clinical challenge. In this study, a novel compound, G-5b, was developed with potent antagonistic and degradation activities comparable to the current drug fulvestrant. G-5b also showed improved stability and solubility. Mechanistically, G-5b engages the proteasome pathway to degrade ER, inhibiting the ER signaling pathway and inducing apoptosis and cell cycle arrest. In animal models, G-5b exhibited superior pharmacokinetics and pharmacodynamics properties. Overall, G-5b is a promising long-acting SERD worthy of further investigation and optimization.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Karoline B. Waitman, Larissa C. de Almeida, Marina C. Primi, Jorge A. E. G. Carlos, Claudia Ruiz, Thales Kronenberger, Stefan Laufer, Marcia Ines Goettert, Antti Poso, Sandra V. Vassiliades, Vinicius A. M. de Souza, Monica F. Z. J. Toledo, Neuza M. A. Hassimotto, Michael D. Cameron, Thomas D. Bannister, Leticia Costa-Lotufo, Joa o A. Machado-Neto, Mauricio T. Tavares, Roberto Parise-Filho
Summary: A series of hybrid inhibitors combining pharmacophores of known kinase inhibitors and benzohydroxamate HDAC inhibitors were synthesized and evaluated for their anticancer activity and pharmacokinetic properties. Compounds 4d-f exhibited promising cytotoxicity against hematological cells and moderate activity against solid tumor models. Compound 4d showed potent inhibition of multiple kinase targets and had stable interactions with HDAC and members of the JAK family. These compounds showed selective cytotoxicity with minimal effects on non-tumorigenic cells and favorable pharmacokinetic profiles.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Michal Sulik, Diana Fontinha, Dietmar Steverding, Szymon Sobczak, Michal Antoszczak, Miguel Prudencio, Adam Huczynski
Summary: This study describes the synthesis of the first-in-class ivermectin derivatives obtained through derivatization of the C13 position, along with the unexpected rearrangement of the macrolide ring. These derivatives show potential for antiparasitic activity and are important for the development of new antiparasitic agents.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Jun Liu, Qiu-Xian Chen, Wen-Fu Wu, Dong Wang, Si -Yu Zhao, Jia-Hao Li, Yi-Qun Chang, Shao-Gao Zeng, Jia-Yi Hu, Yu-Jie Li, Jia-Xin Du, Shu-Meng Jiao, Hai-Chuan Xiao, Qiang Zhang, Jun Xu, Jian-Fu Zhao, Hai -Bo Zhou, Yong-Heng Wang, Jian Zou, Ping-Hua Sun
Summary: A new anti-infective drug strategy has been discovered to attenuate virulence and modulate inflammation caused by drug-resistant Pseudomonas aeruginosa infections. Compound 5f inhibits biofilm formation, macrophage migration, and inflammatory response induced by P. aeruginosa, showing potential as a novel candidate against drug-resistant infections.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Liuzeng Chen, Ke Wang, Lingyun Wang, Wei Wang, Lifan Wang, Jia Li, Xiaohan Liu, Mengya Wang, Banfeng Ruan
Summary: In this study, a series of novel anti-inflammatory compounds were designed and synthesized based on the natural product pterostilbene skeleton. Among them, compound 8 showed the highest activity and exhibited its effects through inhibition of pro-inflammatory cytokines by blocking the NF-KB/MAPK signaling pathway. Compound 8 also demonstrated a good relieving effect on acute colitis in mice and showed good safety in acute toxicity experiments.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Si-Min Liang, Gui-Bin Liang, Hui-Ling Wang, Hong Jiang, Xian-Li Ma, Jian-Hua Wei, Ri-Zhen Huang, Ye Zhang
Summary: A series of novel multi-target antitumor agents were designed, synthesized, and evaluated. Some compounds exhibited significant antitumor activity and one compound showed excellent efficacy, limited toxicity, and low resistance. Further mechanism studies revealed that the compound exerted antitumor effects through multiple pathways.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
