Exploring Pyrrolo-Fused Heterocycles as Promising Anticancer Agents: An Integrated Synthetic, Biological, and Computational Approach

RM Amărandi, MC Al-Matarneh, L Popovici… - Pharmaceuticals, 2023 - mdpi.com
Five new series of pyrrolo-fused heterocycles were designed through a scaffold
hybridization strategy as analogs of the well-known microtubule inhibitor phenstatin …

Advances in the discovery of heterocyclic-based drugs against Alzheimer's disease

JD Sánchez, AR Alcántara, JF González… - Expert Opinion on …, 2023 - Taylor & Francis
Introduction Alzheimer's disease is a multifactorial neurodegenerative disorder
characterized by beta-amyloid accumulation and tau protein hyperphosphorylation. The …

Benzimidazole: journey from single targeting to multitargeting molecule

PK Singh, OM Silakari - Key heterocycle cores for designing multitargeting …, 2018 - Elsevier
There have been continuous efforts to discover multitargeting agents to counter several
complex, multifactorial pathological conditions. Of various heterocycles explored for …

Benzopyrone, a privileged scaffold in drug discovery: An overview of FDA‐approved drugs and clinical candidates

V Sharma, A Sharma, BN Wadje… - Medicinal Research …, 2024 - Wiley Online Library
Natural products have always served as an important source of drugs for treating various
diseases. Among various privileged natural product scaffolds, the benzopyrone class of …

An evolving role of piperazine moieties in drug design and discovery

RV Patel, S Won Park - Mini Reviews in Medicinal Chemistry, 2013 - ingentaconnect.com
This article purposes to provide insights to piperazine based molecular designs that will
facilitate drug discovery program in future. In our pursuit to summarize the reservoir of …

Natural-based indirubins display potent cytotoxicity toward wild-type and T315I-resistant leukemia cell lines

N Gaboriaud-Kolar, V Myrianthopoulos… - Journal of natural …, 2016 - ACS Publications
Drug resistance in chronic myelogenous leukemia (CML) requires the development of new
CML chemotherapeutic drugs. Indirubin, a well-known mutikinase inhibitor, is the major …

Are pyridazines privileged structures?

CG Wermuth - MedChemComm, 2011 - pubs.rsc.org
One can estimate that about 50% of all the drug molecules used in medicine contain a
phenyl ring which can be substituted or not. The bioisosteric replacement of these phenyl …

The opening/closure of the P-loop and hinge of BCR-ABL1 decodes the low/high bioactivities of dasatinib and axitinib

J Wang, Q Chen, M Wang, C Zhong - Physical Chemistry Chemical …, 2017 - pubs.rsc.org
To obtain new insights into the resistance caused by T315I and the differential selectivities of
dasatinib and axitinib against BCR-ABL1 (WT) and BCR-ABL1 (T315), molecular dynamics …

Emerging therapeutic potentials of dual‐acting MAO and AChE inhibitors in Alzheimer's and Parkinson's diseases

B Mathew, DGT Parambi, GE Mathew… - Archiv der …, 2019 - Wiley Online Library
No drug has been approved to prevent neuronal cell loss in patients suffering from
Parkinson's disease (PD) or Alzheimer's disease (AD); despite increased comprehension of …

Synthesis and biological evaluation of quinazoline derivatives–a SAR study of novel inhibitors of ABCG2

MK Krapf, J Gallus, A Spindler, M Wiese - European Journal of Medicinal …, 2019 - Elsevier
Multidrug resistance (MDR) is a major obstacle for effective chemotherapeutic treatment of
cancer frequently leading to failure of the therapy. MDR is often associated with the …