Synthesis of indazole motifs and their medicinal importance: An overview

DD Gaikwad, AD Chapolikar, CG Devkate… - European journal of …, 2015 - Elsevier
Indazoles is an important class of heterocyclic compounds having a wide range of biological
and pharmaceutical applications. There is enormous potential in the synthesis of novel …

Through the “gatekeeper door”: exploiting the active kinase conformation

F Zuccotto, E Ardini, E Casale… - Journal of medicinal …, 2010 - ACS Publications
The human genome comprises more than 500 protein kinases including serine/threonine,
tyrosine and dual specificity kinases. 1, 2 Because of the important physiological and …

Recent advances in the development of indazole‐based anticancer agents

J Dong, Q Zhang, Z Wang, G Huang, S Li - ChemMedChem, 2018 - Wiley Online Library
Cancer is one of the leading causes of human mortality globally; therefore, intensive efforts
have been made to seek new active drugs with improved anticancer efficacy. Indazole …

Assessment of chemical coverage of kinome space and its implications for kinase drug discovery

P Bamborough, D Drewry, G Harper… - Journal of medicinal …, 2008 - ACS Publications
More than 500 compounds chosen to represent kinase inhibitor space have been screened
against a panel of over 200 protein kinases. Significant results include the identification of …

Benzimidazole-biologically attractive scaffold for protein kinase inhibitors

P Singla, V Luxami, K Paul - RSC Advances, 2014 - pubs.rsc.org
Great advances in elucidating molecular structures allow the precise determination of the
interactions between a protein and a therapeutic agent. Enzyme inhibitors are used as a …

EGFR inhibitors and methods of treating disorders

NS Gray, P Janne, MJ Eck, W Zhou - US Patent 9,908,884, 2018 - Google Patents
The present invention relates to novel pyrimidine, pyrrolo pyrimidine, pyrrolo-pyridine,
pyridine, purine and triazine compounds which are able to modulate epidermal growth factor …

Discovery of an orally bioavailable and selective PKMYT1 inhibitor, RP-6306

J Szychowski, R Papp, E Dietrich, B Liu… - Journal of medicinal …, 2022 - ACS Publications
PKMYT1 is a regulator of CDK1 phosphorylation and is a compelling therapeutic target for
the treatment of certain types of DNA damage response cancers due to its established …

Indazole as a Phenol Bioisostere: Structure–Affinity Relationships of GluN2B-Selective NMDA Receptor Antagonists

J Lüken, G Goerges, N Ritter, P Disse… - Journal of Medicinal …, 2023 - ACS Publications
Negative allosteric modulation of GluN2B subunit-containing NMDA receptors prevents
overstimulation, resulting in neuroprotective effects. Since the phenol of prominent negative …

Synthesis of N-Arylindazoles and Benzimidazoles from a Common Intermediate

BC Wray, JP Stambuli - Organic Letters, 2010 - ACS Publications
A variety of N-aryl-1 H-indazoles and benzimidazoles were synthesized from common
arylamino oximes in good to excellent yields. The product selectivity depends upon the base …

Bioisostere effects on the EPSA of Common permeability-limiting groups

AK Ecker, DA Levorse, DA Victor… - ACS Medicinal …, 2022 - ACS Publications
Polar molecular surface area provides a valuable metric when optimizing properties as
varied as membrane permeability and efflux susceptibility. The EPSA method to measure …