Article
Chemistry, Medicinal
Mohd Asyraf Shamsuddin, Amatul Hamizah Ali, Nur Hanis Zakaria, Mohd Fazli Mohammat, Ahmad Sazali Hamzah, Zurina Shaameri, Kok Wai Lam, Wun Fui Mark-Lee, Hani Kartini Agustar, Mohd Ridzuan Mohd Abd Razak, Jalifah Latip, Nurul Izzaty Hassan
Summary: The study synthesized a new series of hybrids, among which 4b demonstrated strong antiplasmodial activity against both 3D7 and K1 strains with low cytotoxic effect. It displayed high selectivity index and low resistance index, suggesting selective inhibition on the 3D7 and K1 strains. Additionally, molecular docking analysis indicated that P. falciparum lactate dehydrogenase could be a potential molecular target for compound 4b.
Article
Biochemistry & Molecular Biology
Fernanda Valerio Lopes, Pedro Henrique Fazza Stroppa, Juliane Aparecida Marinho, Roberta Reis Soares, Lara de Azevedo Alves, Priscila Vanessa Zabala Capriles Goliatt, Clarice Abramo, Adilson David da Silva
Summary: This study evaluated the antimalarial activity of triazole derivatives, with compound 5 showing promising potential for further development in antimalarial chemotherapy. In vitro and in vivo studies showed that compound 5 had significant parasitemia suppression and minimal cytotoxicity, making it a leading candidate for future research in antimalarial drug development.
CHEMICO-BIOLOGICAL INTERACTIONS
(2021)
Article
Biochemistry & Molecular Biology
Sandor Kun, Rachel T. Mathomes, Tibor Docsa, Laszlo Somsak, Joseph M. Hayes
Summary: C-beta-D-glucopyranosyl azole type inhibitors have shown strong inhibitory effects on glycogen phosphorylase. The interactions between these inhibitors and the specific binding site of the enzyme, including hydrogen bonding and ion-ion interactions, are crucial for their potency. These findings have significant implications for the development of novel treatments for type 2 diabetes.
Article
Chemistry, Medicinal
Hegira Ramirez, Esteban Fernandez, Juan Rodrigues, Soriuska Mayora, Gricelis Martinez, Carmen Celis, Juan B. De Sanctis, Michael Mijares, Jaime Charris
Summary: Twelve 7-chloroquinoline derivatives were synthesized using molecular hybridization, showing potential as antimalarials and anticancer agents. Compounds 8 and 9 were the most active, particularly against MCF-7 cells. These compounds may be promising for developing new therapies for malaria and cancer treatment.
ARCHIV DER PHARMAZIE
(2021)
Review
Chemistry, Medicinal
Lekkala Ravindar, Siti Aishah Hasbullah, K. P. Rakesh, Nurul Izzaty Hassan
Summary: Malaria is a deadly parasitic infection ranked as the fifth most lethal worldwide. Antimalarial medications are crucial for preventing and eradicating malaria. The 4-aminoquinoline moiety has diverse biological applications and has been favored in antimalarial drug discovery. This review focuses on its efficacy when hybridized with various heterocyclic scaffolds, aiding the development of more effective antimalarial agents.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Scott Eagon, Jared T. Hammill, Kasey Fitzsimmons, Natalie Sienko, Brandon Nguyen, Jarvis Law, Aashrita Manjunath, Steven P. Wilkinson, Kara Thompson, Julia Elizabeth Glidden, Amy L. Rice, Mofolusho O. Falade, Joshua J. Kimball, Celine DiBernardo, R. Kiplin Guy
Summary: In the search for new anti-malarial drugs, this study reports the discovery of a derivative with potential efficacy against Plasmodium falciparum but without detectable toxicity.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2021)
Article
Biochemistry & Molecular Biology
Rui Cai, Yu Li, Li Zhu, Caiyan Wei, Xiaofeng Bao, Yu Zhao
Summary: In this study, twelve 2, 4, 5-trideoxyhexopyranosides derivatives of diphyllin were synthesized and showed potent inhibitory activity on cancer cell growth. Compounds 5c3 and 5c4 exhibited the best inhibitory activity on breast cancer cells.
CHEMICAL BIOLOGY & DRUG DESIGN
(2022)
Article
Biochemistry & Molecular Biology
Deblina Roy, Mohammad Anas, Ashan Manhas, Satyen Saha, Niti Kumar, Gautam Panda
Summary: In this study, a series of quinoline-imidazole hybrid compounds were synthesized and evaluated for their blood-stage antimalarial activity against Plasmodium falciparum. The results showed that one of the compounds exhibited significant antimalarial efficacy with low cytotoxicity and high selectivity. Furthermore, the study revealed the influence of substituents on the quinoline ring and the role of stereochemistry in the inhibitory activity.
BIOORGANIC CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Andreia Fortuna, Rita Goncalves-Pereira, Paulo J. Costa, Radek Jorda, Veronika Vojackova, Gabriel Gonzalez, Niels Heise, Rene Csuk, M. Conceicao Oliveira, Nuno M. Xavier
Summary: This study describes the synthesis and biological evaluation of novel guanidino sugars as isonucleoside analogs. Some of the compounds showed selective inhibition of acetylcholinesterase and moderate antiproliferative effects in chronic myeloid leukemia and breast cancer cells. The most potent compound also exhibited low toxicity in human fibroblasts.
Article
Chemistry, Physical
Ghada H. Elsayed, Asmaa M. Fahim, Ahmed I. Khodair
Summary: In this study, we synthesized different 2-thioxoimidazolidin-4-one derivatives and investigated their cytotoxicity activity and gene expression. The results showed potential anticancer activity and a mechanism for reducing drug resistance.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Chemistry, Applied
Jyoti, Rashmi Gaur, Yogesh Kumar, Harveer Singh Cheema, Deepak Singh Kapkoti, Mahendra P. Darokar, Feroz Khan, Rajendra Singh Bhakuni
Summary: Twenty one chalcone derivatives were synthesized through Claisen-Schmidt condensation, tested for their antimalarial activity, and a quantitative structure-activity relationship (QSAR) was developed. The most active compound exhibited an IC50 of 2.1 μM/L against malaria parasites in vitro. Molecular mechanisms were explored through in silico docking & ADMET studies for the active compounds.
NATURAL PRODUCT RESEARCH
(2021)
Article
Biochemistry & Molecular Biology
Zhihui Zhou, Jie He, Feiyi Yang, Qingshan Pan, Zunhua Yang, Pengwu Zheng, Shan Xu, Wufu Zhu
Summary: A new class of quinazoline derivatives as EGFR inhibitors was designed and synthesized, with compound 9e showing promising inhibitory activity and specificity, suggesting potential therapeutic value against lung cancer cells.
BIOORGANIC CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Yapeng Lu, Li Zhu, Rui Cai, Yu Li, Yu Zhao
Summary: The present study successfully synthesized a series of novel 2, 4, 5-trideoxyhexopyranosides derivatives of 4'-demethylepipodophyllotoxin as anticancer agents. The biological results demonstrated significant cytotoxicity of these derivatives in inhibiting the growth of various cancer cells. D-monosaccharide 5b was observed to cause concentration-dependent G2/M phase cell cycle arrest in HepG2 cells.
MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Lu Xu, Jinmeng Yu, Lu Jin, Le Pan
Summary: A series of 4-amino coumarin-based succinate dehydrogenase inhibitors (SDHIs) were designed and synthesized. These compounds showed broad-spectrum antifungal activity against various plant pathogenic fungi in vitro. Among them, compounds 3n and 4e displayed excellent activity against Alternaria alternata and Alternaria solani.
Article
Chemistry, Medicinal
Wei Cheng, Yingkun Yan, Tingting Xiao, Guilan Zhang, Tingting Zhang, Tong Lu, Wenjing Jiang, Jingwen Wang, Xiaorong Tang
Summary: Thirty-three new 2,3-dihydroquinolin-4(1H)-one analogues were synthesized, with one compound showing strong inhibitory activity against fungi, surpassing commercial fungicide. These analogues also exhibited excellent activity against succinate dehydrogenase.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)