TY - JOUR
T1 - Synthesis and anticancer properties of 'azole'based chemotherapeutics as emerging chemical moieties: A comprehensive review
AU - Prasher, Parteek
AU - Sharma, Mousmee
AU - Zacconi, Flavia
AU - Gupta, Gaurav
AU - Aljabali, Alaa A.
AU - Mishra, Vijay
AU - Tambuwala, Murtaza M.
AU - Kapoor, Deepak N.
AU - Negi, Poonam
AU - Andreoli Pinto, Terezinha De Jesus
AU - Singh, Inderbir
AU - Chellappan, Dinesh Kumar
AU - Dua, Kamal
PY - 2020/8/20
Y1 - 2020/8/20
N2 - Azole frameworks serve as privileged scaffolds in the contemporary drug design paradigm owing to their unique physicochemical profile that promotes the development of highly selective, physiological benevolent chemotherapeutics. Several azole nuclei function as bioisostere in medicinal chemistry and prompt the development of tailored therapeutics for targeting the desired biological entities. Besides, the azole scaffold forms an integral part in the advanced drug designing methodologies, such as target template insitu drug synthesis, that assists in rapid identification of the hit molecules form a diverse pool of leads; and direct biomolecule-drug conjugation, along with bioorthogonal strategies that ensure localization, and superior target specificity of the directed therapeutic. Lastly, the structural diversity of azole framework and high yielding click synthetic methods provide a comprehensive Structure-Activity Relationship analysis for design optimization of the potential drug molecules by fine-tuning the placement of different substituents critical for the activity. This review provides a comprehensive analysis of the synthesis and anticancer potential of azole based chemotherapeutics.
AB - Azole frameworks serve as privileged scaffolds in the contemporary drug design paradigm owing to their unique physicochemical profile that promotes the development of highly selective, physiological benevolent chemotherapeutics. Several azole nuclei function as bioisostere in medicinal chemistry and prompt the development of tailored therapeutics for targeting the desired biological entities. Besides, the azole scaffold forms an integral part in the advanced drug designing methodologies, such as target template insitu drug synthesis, that assists in rapid identification of the hit molecules form a diverse pool of leads; and direct biomolecule-drug conjugation, along with bioorthogonal strategies that ensure localization, and superior target specificity of the directed therapeutic. Lastly, the structural diversity of azole framework and high yielding click synthetic methods provide a comprehensive Structure-Activity Relationship analysis for design optimization of the potential drug molecules by fine-tuning the placement of different substituents critical for the activity. This review provides a comprehensive analysis of the synthesis and anticancer potential of azole based chemotherapeutics.
KW - Organic Chemistry
U2 - 10.2174/1385272824999200820152501
DO - 10.2174/1385272824999200820152501
M3 - Article
SN - 1385-2728
VL - 25
SP - 654
EP - 668
JO - Current Organic Chemistry
JF - Current Organic Chemistry
IS - 6
ER -
