Article
Chemistry, Multidisciplinary
Jin-yi Liu, Wei-qi Fu, Xiang-jin Zheng, Wan Li, Li-wen Ren, Jin-hua Wang, Cui Yang, Guan-hua Du
Summary: Avasimibe demonstrated potent anticancer effects on human glioblastoma cells by inhibiting proliferation, inducing apoptosis, and regulating multiple signaling pathways. The drug showed promising potential as a chemotherapy treatment for glioblastoma.
ACTA PHARMACOLOGICA SINICA
(2021)
Article
Biochemistry & Molecular Biology
Jeyce Kelle Ferreira de Andrade, Alexandre Jose da Silva Goes, Vanessa Xavier Barbosa, Mariza Severina de Lima Silva, Mariana Aragao Matos Donato, Christina Alves Peixoto, Gardenia Carmen Gadelha Militao, Teresinha Goncalves da Silva
Summary: Thiosemicarbazones derived from beta-lapachone showed potent cytotoxic effects on leukemia cells, with BV3 being the most selective compound, exhibiting high toxicity to tumor cells and low toxicity to normal cells. These compounds have the potential to be promising candidates for anticancer drugs.
CHEMICO-BIOLOGICAL INTERACTIONS
(2022)
Article
Chemistry, Multidisciplinary
Xing Huang, Chang-Hao Zhang, Hao Deng, Dan Wu, Hong-Yan Guo, Jung Joon Lee, Fen-Er Chen, Qing-Kun Shen, Li-Li Jin, Zhe-Shan Quan
Summary: A series of quillaic acid derivatives with different substituents were synthesized and evaluated for their antitumor activity against human cancer cell lines. One compound showed strong antiproliferative activity and induced apoptosis and cell cycle arrest by modulating signaling pathways.
FRONTIERS IN CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Marwa Abdel-Motaal, Fardous F. El-Senduny, Saad Shaaban
Summary: Novel pyrazole hybrids (3-17) were synthesized successfully and their structures were confirmed using various methods. Compound 13 showed promising anticancer activity against 4T1 cells, leading to cell death via inhibition of wound healing, colony formation, cell cycle delay in the G0/G1 phase, activation of p27 levels, and apoptosis possibly through DNA intercalation.
Article
Chemistry, Multidisciplinary
Zhi-Gang Yin, Xiong-Wei Liu, Hui-Juan Wang, Min Zhang, Xiong-Li Liu, Ying Zhou
Summary: A highly efficient synthesis of structurally diverse ortho-acylphenol-diindolylmethane hybrids 3 using carboxylic acid-activated chromones as building blocks has been reported, showing promising anti-cancer activities against various tumor cells, with compound 3t demonstrating potent anti-proliferative effects against A549 cells. Mechanistic studies revealed that compound 3t induces apoptosis in A549 cells through the mitochondrial pathway, indicating its potential as a new anti-tumor drug candidate.
NEW JOURNAL OF CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Mohamed Y. Zaky, Rehab Mahmoud, Ahmed A. Farghali, Hany Abd El-Raheem, Ahmed Hassaballa, Mohamed Mohany, Dalal Hussien M. Alkhalifah, Wael N. Hozzein, Abdelrahman Mohamed
Summary: This study successfully synthesized and characterized a novel Cu/Fe layer double hydroxide (LDH) nanocomposite for the treatment of prostate cancer. The results demonstrated that Cu/Fe LDH had significant anticancer activities against prostate cancer cells, reducing cell viability, inhibiting cell migration, inducing cell cycle arrest, and triggering apoptosis. It also showed good safety impact on normal cells.
Article
Biochemistry & Molecular Biology
Thidarath Rattanaburee, Patpanat Sermmai, Kornthip Tangthana-umrung, Tienthong Thongpanchang, Potchanapond Graidist
Summary: This study investigated the cytotoxicity and anticancer activity of (+/-)-kusunokinin derivatives on various cancer cells. The results showed that (+/-)-TTPG-B exhibited the strongest cytotoxicity on breast cancer and cholangiocarcinoma cells. Both (+/-)-TTPG-A and (+/-)-TTPG-B induced cell cycle arrest and apoptosis, and their effects were superior to (+/-)-kusunokinin.
Article
Biochemistry & Molecular Biology
Yara El-Dash, Emad Elzayat, Amr M. Abdou, Rasha A. Hassan
Summary: Novel hybrid compounds of hexahydrobenzo[4,5]thieno[2,3-d]pyrimidine with aminothiazole scaffolds were synthesized and evaluated for their cytotoxic activity against human tumor cell lines. Compounds 7c, 7d, and 7e showed significant antiproliferative activities, with 7c demonstrating excellent cytotoxic activity against various cancer cell lines. Compound 7c also exhibited potential as a VEGFR-2 inhibitor and induced G2/M phase cell cycle arrest and apoptosis in treated cells.
BIOORGANIC CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Feng-Lung Tsai, Han-Li Huang, Mei-Jung Lai, Jing-Ping Liou, Shiow-Lin Pan, Chia-Ron Yang
Summary: The study found that MPT0G236, a pan-HDAC inhibitor, specifically targets malignant tumor cells and exhibits significant anticancer activity in human colorectal cancer cells, making it a potential candidate for colorectal cancer treatment.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Medicinal
Wei Han, Jieyi Li, Qianqian Li, Yusang Yang, Jiabin Li, Xiaowen Xue
Summary: Two novel series of derivatives were synthesized and evaluated for their cytotoxic activity against colon cancer and breast cancer cells. Most compounds exhibited better inhibitory activity than the reference compound, and HCT-116 cells were more sensitive to the compounds.
Review
Biochemistry & Molecular Biology
Dahye Yun, So Young Yoon, Soo Jung Park, Yoon Jung Park
Summary: Herbal plants enriched with isoquinoline alkaloids have been used in traditional folk medicine for their anti-inflammatory, antimicrobial, and analgesic effects. These alkaloids induce cell death through cell cycle arrest, apoptosis, and autophagy. The molecular mechanisms of these effects may involve binding to nucleic acids or proteins, enzyme inhibition, and epigenetic modulation.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Medicine, Research & Experimental
Tahereh Tajik, Kaveh Baghaei, Vahid Erfani Moghadam, Naser Farrokhi, Seyed Alireza Salami
Summary: Plant-derived extracellular vesicles (EVs) have gained attention in recent years due to their proven therapeutic properties. In this study, EVs were isolated from two different chemotypes of cannabis and classified as high-CBD and low-CBD EVs. These EVs exhibited different cytotoxicity and anticancer effects. The findings suggest that CDEVs could be an ideal natural vehicle for delivering bioactive phytocannabinoids and a promising strategy in cancer management.
BIOMEDICINE & PHARMACOTHERAPY
(2022)
Article
Biochemistry & Molecular Biology
Mona S. El-Zoghbi, Samiha A. El-Sebaey, Hanan A. AL-Ghulikah, Eman A. Sobh
Summary: New thiazolopyrimidine derivatives were synthesized and evaluated for their cytotoxicity against human tumor cell lines. Several compounds showed potent anticancer activity and inhibition of the Topo II enzyme, with compound 4c being the most effective Topo II inhibitor. It also exhibited significant disruption of the cell cycle and apoptosis in A549 cells. These findings suggest that our designed compounds have potential as promising anticancer agents targeting Topo II inhibition.
JOURNAL OF ENZYME INHIBITION AND 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)
Article
Immunology
Akebaier Sulaiman, Jin Lv, Junwei Fan, Reyila Abuliezi, Qian Zhang, Xuefeng Wan
Summary: The study showed that miR-22 may reduce the activity of cutaneous malignant melanoma A375 cells by targeting and inhibiting the activation of the NLRP3 inflammasome.
JOURNAL OF IMMUNOLOGY RESEARCH
(2022)
Article
Chemistry, Medicinal
Madasu Chandrashekhar, Vadithe Lakshma Nayak, Sistla Ramakrishna, Uppuluri Venkata Mallavadhani
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2016)
Article
Chemistry, Multidisciplinary
Chandrashekhar Madasu, Sagarika Gudem, Ramakrishna Sistla, Venkata Mallavadhani Uppuluri
MONATSHEFTE FUR CHEMIE
(2017)
Article
Biochemistry & Molecular Biology
Uppuluri Venkata Mallavadhani, Madasu Chandrashekhar, Karri Shailaja, Sistla Ramakrishna
BIOORGANIC CHEMISTRY
(2019)
Article
Chemistry, Medicinal
Chandrashekhar Madasu, Shailaja Karri, Rajendra Sangaraju, Ramakrishna Sistla, Mallavadhani Venkata Uppuluri
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2020)
Article
Chemistry, Multidisciplinary
Ya-ming Xu, Chandrashekhar Madasu, Manping X. Liu, E. M. Kithsiri Wijeratne, David Dierig, Bob White, Istvan Molnar, A. A. Leslie Gunatilaka
Summary: A total of 12 new cycloartane- and lanostane-type triterpenoids, along with 10 known triterpenoids, were isolated from the resin of Parthenium argentatum AZ-2 obtained as a byproduct of Bridgestone guayule rubber production. Compounds 13, 14, and 18 exhibited weak cytotoxic activity for several cancer cell lines.
Article
Chemistry, Medicinal
Chandrashekhar Madasu, Ya-Ming Xu, E. M. Kithsiri Wijeratne, Manping X. Liu, Istvan Molnar, A. A. Leslie Gunatilaka
Summary: Argentatins A-C, the major cycloartane-type triterpenoids in guayule resin, were converted into pyrimidine, thiazole, and indole analogues. The cytotoxic activities of these analogues were compared with the parent compounds against cancer cell lines and normal cells, showing enhanced activity in the pyrimidine analogues. These findings suggest the potential of triterpenoid constituents in guayule resin for anticancer drug discovery.
MEDICINAL CHEMISTRY RESEARCH
(2022)
Article
Chemistry, Medicinal
Ram K. Modukuri, Diana Monsivais, Feng Li, Murugesan Palaniappan, Kurt M. Bohren, Zhi Tan, Angela F. Ku, Yong Wang, Chandrashekhar Madasu, Jian-Yuan Li, Suni Tang, Gabriella Miklossy, Stephen S. Palmer, Damian W. Young, Martin M. Matzuk
Summary: Through screening 4.17 billion DNA-encoded chemical library molecules, we identified two selective kinase inhibitors, CDD-1115 and CDD-1431, for BMPR2. Further research led to the development of two more potent inhibitors, CDD-1281 and CDD-1653. This study demonstrates the reliability of DNA-encoded chemistry technology for discovering novel and highly selective kinase inhibitors.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Plant Sciences
Marielle C. Inacio, Weimao Zhong, Ya-Ming Xu, E. M. Kithsiri Wijeratne, Chandrashekhar Madasu, Istvan Molnar, A. A. Leslie Gunatilaka
Summary: Microbial biotransformation of argentatin A, isoargentatin A, and argentatin C, the triterpenoid constituents of guayule resin, was conducted using Chaetomium sp. PA001, an endophytic fungus of the same plant. Six new products were obtained, which formed through nucleophilic oxygenation, lactone ring opening, ring rearrangement, and reduction reactions. The structures of these new products were determined through detailed spectroscopic analysis. None of the products showed antimicrobial activity, but the hydroxy-carboxylic acid derivative of argentatin A exhibited weak cytotoxic activity with improved selectivity against human breast cancer cell line MCF-7 compared to the parent compound. This study reports the first microbial biotransformation of iso-argentatin A and argentatin C.
PHYTOCHEMISTRY LETTERS
(2023)
