Amide bond bioisosteres: Strategies, synthesis, and successes
The amide functional group plays a key role in the composition of biomolecules, including
many clinically approved drugs. Bioisosterism is widely employed in the rational …
many clinically approved drugs. Bioisosterism is widely employed in the rational …
The 1, 2, 3-triazole ring as a bioisostere in medicinal chemistry
E Bonandi, MS Christodoulou, G Fumagalli… - Drug Discovery …, 2017 - Elsevier
Highlights•Triazoles mimic different functional groups, resulting optimal bioisosteres for the
synthesis of new active molecules.•Triazoles present a marked stability under hydrolytic …
synthesis of new active molecules.•Triazoles present a marked stability under hydrolytic …
CuAAC-ensembled 1, 2, 3-triazole-linked isosteres as pharmacophores in drug discovery
A Rani, G Singh, A Singh, U Maqbool, G Kaur… - RSC advances, 2020 - pubs.rsc.org
The review lays emphasis on the significance of 1, 2, 3-triazoles synthesized via CuAAC
reaction having potential to act as anti-microbial, anti-cancer, anti-viral, anti-inflammatory …
reaction having potential to act as anti-microbial, anti-cancer, anti-viral, anti-inflammatory …
Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region–abelson (Bcr-Abl) kinase …
X Ren, X Pan, Z Zhang, D Wang, X Lu… - Journal of medicinal …, 2013 - ACS Publications
Bcr-AblT315I mutation-induced imatinib resistance remains a major challenge for clinical
management of chronic myelogenous leukemia (CML). Herein, we report GZD824 (10a) as …
management of chronic myelogenous leukemia (CML). Herein, we report GZD824 (10a) as …
Sulfonamide-based ring-fused analogues for CAN508 as novel carbonic anhydrase inhibitors endowed with antitumor activity: Design, synthesis, and in vitro …
In the present study, we report the design and synthesis of novel CAN508 sulfonamide-
based analogues (4, 8a-e, 9a-h and 10a-e) as novel carbonic anhydrase (CA) inhibitors with …
based analogues (4, 8a-e, 9a-h and 10a-e) as novel carbonic anhydrase (CA) inhibitors with …
Design and synthesis of certain 7-Aryl-2-Methyl-3-Substituted Pyrazolo {1, 5-a} Pyrimidines as multikinase inhibitors
Four new series 7a-e, 8a-e, 9a-e, and 10a-e of 7-aryl-3-substituted pyrazolo [1, 5-a]
pyrimidines were synthesized and tested for their RTK and STK inhibitory activity …
pyrimidines were synthesized and tested for their RTK and STK inhibitory activity …
Novel α-Aminophosphonates of imatinib Intermediate: Synthesis, anticancer Activity, human Abl tyrosine kinase Inhibition, ADME and toxicity prediction
S Aita, VN Badavath, M Gundluru, M Sudileti… - Bioorganic …, 2021 - Elsevier
An efficient method for the synthesis of a new class of α-aminophosphonates of imatinib
derivative has been developed in one-pot Kabachnik-Fields reaction of N-(5-amino-2-methyl …
derivative has been developed in one-pot Kabachnik-Fields reaction of N-(5-amino-2-methyl …
Transition metal free intermolecular direct oxidative C–N bond formation to polysubstituted pyrimidines using molecular oxygen as the sole oxidant
W Guo, C Li, J Liao, F Ji, D Liu, W Wu… - The Journal of Organic …, 2016 - ACS Publications
Various polysubstituted pyrimidines are smoothly formed via a base-promoted
intermolecular oxidation C–N bond formation of allylic C (sp3)–H and vinylic C (sp2)–H of …
intermolecular oxidation C–N bond formation of allylic C (sp3)–H and vinylic C (sp2)–H of …
A recent review on drug modification using 1, 2, 3-triazole
Motivated by evidence garnered from literature probing the use of triazoles in drug discovery
and development, we reported the utilization of bioisosteric replacement and molecular …
and development, we reported the utilization of bioisosteric replacement and molecular …
Syntheses and biological evaluation of 1, 2, 3-triazole and 1, 3, 4-oxadiazole derivatives of imatinib
YT Li, JH Wang, CW Pan, FF Meng, XQ Chu… - Bioorganic & Medicinal …, 2016 - Elsevier
Abstract Three novel series of 1, 2, 3-triazole and 1, 3, 4-oxadiazole derivatives of imatinib
were prepared and evaluated in vitro for their cytostatic effects against a human chronic …
were prepared and evaluated in vitro for their cytostatic effects against a human chronic …