Recent advances in the application of podophyllotoxin derivatives to fight against drugresistant cancer cells

Author(s):  
Qiuyan Guo ◽  
Enshe Jiang

: Podophyllotoxins including epipodophyllotoxin derivatives can act on a diverse array of drug targets in cancer cells, and thus possess potential activity against various forms of cancer cell lines including drug-resistant forms. Moreover, several podophyllotoxin derivatives which are represented by etoposide and teniposide have already been approved for the cancer therapy, demonstrating podophyllotoxin moiety is a useful pharmacophore for the discovery of novel anticancer agents. This review reports the recent advances in exploitation of podophyllotoxin derivatives to fight against multidrug-resistant cancer cells. The mechanism of action and structure-activity relationship (SAR) studies are also highlighted.

Author(s):  
Jiaqi Xiao ◽  
Meixiang Gao ◽  
Qiang Diao ◽  
Feng Gao

: Drug resistance including multidrug resistance resulting from different defensive mechanisms in cancer cells is the leading cause of the failure about the cancer therapy, making it an urgent need to develop more effective anticancer agents. Chalcones, widely distributed in nature, could act on diverse enzymes and receptors in cancer cells. Accordingly, chalcone derivatives possess potential activity against various cancers including drug-resistant even multidrug-resistant cancer. This review outlines the recent development of chalcone derivatives with potential activity against drug-resistant cancers covering articles published between 2010 and 2020, so as to facilitate further rational design of more effective candidate.


Author(s):  
Gangqiang Wang ◽  
Shaofa Sun ◽  
Bin Wu ◽  
Jikai Liu

: Cancer is the main cause of death, and the emergence of resistance by cancer cells towards existing anticancer agents is one of the major problems for effective chemotherapy, creating a great demand for the development of novel anticancer drugs. Coumarins, abundantly found in nature, constitute an important class of pharmacological agents pos-sessing physiological activities. The mechanism investigations elucidated that coumarins could lead to self-programmed cancer cell death (apoptosis) via different mechanisms, thereby coumarin-based derivatives possess potential activity against various forms of cancers including drug-resistant even multidrug-resistant cancers. This review article describes the recent progress in the discovery, structural modification, structure-activity relationship, and mechanism of action studies of cou-marin-based derivatives with potential activity against drug-resistant cancers, covering articles published between 2010 and 2020.


2011 ◽  
Vol 13 (5) ◽  
pp. 417-424 ◽  
Author(s):  
Yong-En Guo ◽  
Hong Chen ◽  
Song Zuo ◽  
Dai-Lin Liu ◽  
Yan-Ling Lu ◽  
...  

ChemInform ◽  
2006 ◽  
Vol 37 (27) ◽  
Author(s):  
Jin Chen ◽  
Larisa V. Kuznetsova ◽  
Ioana M. Ungreanu ◽  
Iwao Ojima

Amino Acids ◽  
2021 ◽  
Author(s):  
Katarzyna Guzow ◽  
Ewa Mulkiewicz ◽  
Michał Obuchowski ◽  
Wiesław Wiczk

AbstractSearching for new drugs is still a challenge for science, mainly because of civilization development and globalization which promote the rapid spread of diseases, which is particularly dangerous in the case of infectious ones. Moreover, readily available already known antibiotics are often overused or misused, possibly contributing to the increase in the number of multidrug-resistant microorganisms. A consequence of this is the need for new structures of potential drugs. One of them is a benzoxazole moiety, a basic skeleton of a group of fluorescent heterocyclic compounds already widely used in chemistry, industry, and medicine, which is also present in naturally occurring biologically active compounds. Moreover, synthetic benzoxazoles are also biologically active. Considering all of that, a large group of non-proteinogenic amino acids based on 3-(2-benzoxazol-5-yl)alanine skeleton was studied in search for new antimicrobial and anticancer agents. Screening tests revealed that antibacterial potential of 41 compounds studied is not very high; however, they are selective acting only against Gram-positive bacteria (B. subtilis). Moreover, almost half of the studied compounds have antifungal properties, also against pathogens (C. albicans). Most of studied compounds are toxic to both normal and cancer cells. However, in a few cases, toxicity to normal cells is much lower than for cancer cells indicating these compounds as future anticancer agents. The research carried out on such a large group of compounds allowed to establish a structure–activity relationship which enables to select candidates for further modifications, necessary to improve their biological activity and obtain a new lead structure with potential for therapeutic use.


MedChemComm ◽  
2015 ◽  
Vol 6 (11) ◽  
pp. 2012-2022 ◽  
Author(s):  
Jaya P. Shrestha ◽  
Yagya Prasad Subedi ◽  
Liaohai Chen ◽  
Cheng-Wei Tom Chang

Previously, we reported the synthesis and structure–activity relationship (SAR) study of a series of novel 4,9-dioxo-4,9-dihydro-1H-naphtho[2,3-d][1,2,3]triazol-3-ium salts, which had very potent anti-proliferative activities (low μM to nM GI50) against a broad range of cancer cells.


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