Article
Biochemistry & Molecular Biology
Hanan I. Althagbi, Fitri Budiyanto, Ahmed Abdel-Lateff, Khalid O. Al-Footy, Nahed O. Bawakid, Mohamed A. Ghandourah, Mohammad Y. Alfaifi, Serag Eldin I. Elbehairi, Walied M. Alarif
Summary: Seven isoprenoid derivatives isolated from the soft coral Xenia umbellata exhibited cytotoxic effects against breast adenocarcinoma, hepatocellular carcinoma, and cervix adenocarcinoma cells, with compound 3 showing the most potent cytotoxic effect among them. Late apoptosis was prominent after treatment with compound 7 on all cancer cells.
Article
Immunology
Maryam Keshtvarz, Ehsan Rezaei, Jafar Amani, Mohammad Reza Pourmand, Jafar Salimian, Sheila Sarial, Masoumeh Douraghi
Summary: Immunotoxins, a type of targeted therapy, can kill cells using highly potent bacterial, fungal or plant toxins. In this study, a Stx-based immunotoxin was designed and used to selectively induce cytotoxicity and apoptosis in Fn-14-positive cells related to colon and lung cancer.
INTERNATIONAL IMMUNOPHARMACOLOGY
(2022)
Article
Chemistry, Multidisciplinary
Shizhen Zhao, Le Wang, Jie Wang, Chenwei Wang, Shaowei Zheng, Yajie Fu, Yunfu Li, Wei-Dong Chen, Ruifang Hou, Dongbin Yang, Yan-Dong Wang
Summary: TGR5 is an important target for the treatment of non-alcoholic steatohepatitis, type 2 diabetes mellitus, and obesity. Novel compounds have been discovered with excellent agonist activity.
Article
Chemistry, Medicinal
Xingchen Liu, Cheng Wang, Shang Li, Lailiang Qu, Fucheng Yin, Dehua Lu, Heng Luo, Xinye Chen, Zhongwen Luo, Ningjie Cui, Xiaobing Wang, Lingyi Kong
Summary: In this study, a potential drug candidate 29e for treating CRC was designed to inhibit tumor growth by targeting PKM2 kinase, demonstrating significant antiproliferative effects in cell experiments and animal models.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Physical
Penki V. S. Sashankh, Dorothy Priyanka Dorairaj, Jia-Ying Chen, Yu-Lan Chang, Kuldeep Chand, Ramasamy Karvembu, Ching-Ming Chien, Sodio C. N. Hsu
Summary: A series of piperazine bearing thiourea compounds were synthesized for the treatment of colorectal carcinoma. Compound L2 exhibited good cytotoxicity, especially against cisplatin-resistant cells, showing potential for cancer therapy.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Biochemistry & Molecular Biology
De-sheng Cai, Shao-Yan Lou, Su Huo, Feng Gao, Wen -Min Pi, Ke-Dian Chen, Cheng Wang, Xiao-Yun Yang, Jing-Yi Jiao, Bing Xu, Peng -Long Wang, Hai -Min Lei
Summary: Conjugation of bile acids with podophyllotoxin improves selectivity and activity against liver cancer cell lines.
BIOORGANIC CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Zhiyuan Cheng, Yijie Wang, Yao Zhang, Chan Zhang, Mengru Wang, Wei Wang, Jiacheng He, Yang Wang, Hankun Zhang, Qiansen Zhang, Chunyong Ding, Deyan Wu, Linlin Yang, Mingyao Liu, Weiqiang Lu
Summary: In recent years, small-molecule drugs have become essential in tumor immunotherapy. The study identified compound 1 as an EP4 antagonist hit, which showed promising antitumor immune response by blocking PGE2/EP4 signaling. Further exploration led to the discovery of compound 14, which displayed high EP4 antagonistic activity, selectivity, and favorable drug-like profiles. When administered orally, compound 14 significantly inhibited tumor growth by enhancing cytotoxic CD8+ T cell-mediated antitumor immunity.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Xin Zhang, Tingting Yang, Xin Jin, Kaige Lin, Xiling Dai, Ting Gao, Guozheng Huang, Minghui Fan, Liang Ma, Zi Liu, Jianguo Cao
Summary: In this study, podophyllotoxin derivatives incorporating piperazinyl-cinnamic amide moieties at the 4-position were synthesized. Compound 6e showed the best anti-proliferative properties and inhibited mitochondria-associated apoptosis in MCF-7 cells.
BIOORGANIC CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Nahed Obaid Bawakid, Walied Mohamed Alarif, Ahmed Abdel-Lateff
Summary: Two new rare 30-norisodinosterol derivatives were identified from Xenia umbellata, with compound 1 showing potent cytotoxicity against various cancer cells. Morphological detection using DNA-binding dyes revealed early and late apoptotic cell death induced by these compounds, particularly in HepG2 cells. Further investigation into the anti-proliferative activity of compounds 1 and 3 is warranted.
Article
Plant Sciences
Vimi Kshetrimayum, Rameshwari Heisnam, Ojit Singh Keithellakpam, Pullapanthula Radhakrishnanand, Sai Jyothi Akula, Pulok K. Mukherjee, Nanaocha Sharma
Summary: Paris polyphylla Sm. (Melanthiaceae) is an important and vulnerable herb with a wide range of traditional applications. The extract of P. polyphylla (PPE) showed good antioxidant activity and cytotoxicity against HCT-116 colon cancer cells without significant toxicity to normal cells. PPE also exhibited synergistic effects with 5FU and cisplatin in HCT-116 cells. The anticancer activities of PPE were attributed to its steroidal saponins.
Article
Biochemistry & Molecular Biology
Kangjia Du, Wantong Ma, Chengjie Yang, Zhongkun Zhou, Shujian Hu, Yanan Tian, Hao Zhang, Yunhao Ma, Xinrong Jiang, Hongmei Zhu, Huanxiang Liu, Peng Chen, Yingqian Liu
Summary: A series of novel derivatives of isaindigotone showed significant anti-proliferative activity on human gastrointestinal cancer cells, with Compound 6 being the most effective inhibitor on AGS cells. The potential mechanism suggested that Compound 6 induced apoptosis and suppressed the PI3K/AKT/mTOR signal pathway, possibly through its interaction with AKT1.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Qasim Shah, Zahid Hussain, Bilal Ahmad Khan, Kenneth A. Jacobson, Jamshed Iqbal
Summary: The study investigates the potency of P2X7 receptor antagonists and their relationship with cancer, revealing five compounds with strong selective inhibitory effects. These compounds exhibit varying cell viability and induction of apoptosis in transfected and non-transfected cell lines.
BIOORGANIC CHEMISTRY
(2023)
Review
Biochemistry & Molecular Biology
Yingqian Zhang, Chenyuan Wu, Nana Zhang, Rui Fan, Yang Ye, Jun Xu
Summary: Pyrazole derivatives, a class of heterocyclic compounds, possess unique chemical structures and exhibit a broad spectrum of pharmacological activities. Recent studies have focused on synthesizing and evaluating pyrazole derivatives for their anticancer potential. Structure-activity relationship studies have shown that appropriate substitution on the pyrazole ring can enhance anticancer efficacy and selectivity. Furthermore, these derivatives have demonstrated multiple mechanisms of anticancer action, making them promising candidates for developing anticancer drugs.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Pharmacology & Pharmacy
Wilson Castrillon-Lopez, Angie Herrera-Ramirez, Gustavo Moreno-Quintero, Juan Carlos Coa, Tonny W. Naranjo, Wilson Cardona-Galeano
Summary: A series of resveratrol/hydrazone hybrids were synthesized and evaluated for their activity against colorectal cancer cells and nonmalignant cells. The results showed that two compounds exhibited higher cytotoxic activity against malignant cells and displayed better activity and selectivity than parental compounds and the reference drug. Additionally, the compounds may exert their anti-proliferative activity through cell cycle arrest and mitochondrial depolarization.
Review
Oncology
Stefania Garzoli, Pedro Alarcon-Zapata, Gulnaz Seitimova, Barbara Alarcon-Zapata, Miquel Martorell, Farukh Sharopov, Patrick Valere Tsouh Fokou, Darline Dize, Lauve Rachel Tchokouaha Yamthe, Francisco Les, Guillermo Casedas, Victor Lopez, Marcello Iriti, Javad Sharifi Rad, Eda Sonmez Gurer, Daniela Calina, Raffaele Pezzani, Sara Vitalini
Summary: This paper reviews the preclinical studies on the role and mechanisms of essential oils in colorectal cancer (CRC). The results showed that essential oils exhibited a wide range of bioactive effects like cytotoxicity, antiproliferative, and antimetastatic effects on cancer cells through various mechanisms of action. Therefore, essential oils can be considered as efficient complementary therapies in chemotherapy in CRC.
CANCER CELL INTERNATIONAL
(2022)
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)