TY - JOUR
T1 - Nitro-Group-Containing Drugs
AU - Nepali, Kunal
AU - Lee, Hsueh Yun
AU - Liou, Jing Ping
N1 - Publisher Copyright:
© 2018 American Chemical Society.
PY - 2019/3/28
Y1 - 2019/3/28
N2 - The nitro group is considered to be a versatile and unique functional group in medicinal chemistry. Despite a long history of use in therapeutics, the nitro group has toxicity issues and is often categorized as a structural alert or a toxicophore, and evidence related to drugs containing nitro groups is rather contradictory. In general, drugs containing nitro groups have been extensively associated with mutagenicity and genotoxicity. In this context, efforts towards the structure-mutagenicity or structure-genotoxicity relationships have been undertaken. The current perspective covers various aspects of agents that contain nitro groups, their bioreductive activation mechanisms, and their toxicities, and approaches to combat their toxicity issues. In addition, recent advances in the field of anticancer, antitubercular and antiparasitic agents containing nitro groups, along with a patent survey on hypoxia-activated prodrugs containing nitro groups, are also covered.
AB - The nitro group is considered to be a versatile and unique functional group in medicinal chemistry. Despite a long history of use in therapeutics, the nitro group has toxicity issues and is often categorized as a structural alert or a toxicophore, and evidence related to drugs containing nitro groups is rather contradictory. In general, drugs containing nitro groups have been extensively associated with mutagenicity and genotoxicity. In this context, efforts towards the structure-mutagenicity or structure-genotoxicity relationships have been undertaken. The current perspective covers various aspects of agents that contain nitro groups, their bioreductive activation mechanisms, and their toxicities, and approaches to combat their toxicity issues. In addition, recent advances in the field of anticancer, antitubercular and antiparasitic agents containing nitro groups, along with a patent survey on hypoxia-activated prodrugs containing nitro groups, are also covered.
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U2 - 10.1021/acs.jmedchem.8b00147
DO - 10.1021/acs.jmedchem.8b00147
M3 - Review article
AN - SCOPUS:85056485313
SN - 0022-2623
VL - 62
SP - 2851
EP - 2893
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
IS - 6
ER -