Comprehensive review in current developments of imidazole‐based medicinal chemistry

L Zhang, XM Peng, GLV Damu… - Medicinal research …, 2014 - Wiley Online Library
Imidazole ring is an important five‐membered aromatic heterocycle widely present in natural
products and synthetic molecules. The unique structural feature of imidazole ring with …

Recent progress in the discovery of next generation inhibitors of aromatase from the structure–function perspective

D Ghosh, J Lo, C Egbuta - Journal of medicinal chemistry, 2016 - ACS Publications
Human aromatase catalyzes the synthesis of estrogen from androgen with high substrate
specificity. For the past 40 years, aromatase has been a target of intense inhibitor discovery …

Combating breast cancer with non-steroidal aromatase inhibitors (NSAIs): Understanding the chemico-biological interactions through comparative SAR/QSAR study

N Adhikari, SA Amin, A Saha, T Jha - European Journal of Medicinal …, 2017 - Elsevier
It is a challenging task to design target-specific and less toxic non-steroidal aromatase
inhibitors (NSAIs) though the modeling studies for designing anti-aromatase molecules have …

Synthesis and molecular docking of 1, 2, 3-triazole-based sulfonamides as aromatase inhibitors

R Pingaew, V Prachayasittikul, P Mandi… - Bioorganic & medicinal …, 2015 - Elsevier
Abstract A series of 1, 4-disubstituted-1, 2, 3-triazoles (13–35) containing sulfonamide
moiety were synthesized and evaluated for their aromatase inhibitory effects. Most triazoles …

Dietary flavones as dual inhibitors of DNA methyltransferases and histone methyltransferases

R Kanwal, M Datt, X Liu, S Gupta - PloS one, 2016 - journals.plos.org
Methylation of DNA and histone proteins are mutually involved in the epigenetic regulation
of gene expression mediated by DNA methyltransferases (DNMTs) and histone …

SAR, QSAR and docking of anticancer flavonoids and variants: a review

L Scotti… - Current topics in …, 2012 - ingentaconnect.com
Flavonoids are phenolic compounds, secondary metabolites of plants that cause several
benefits to our health, including helping the treatment against cancer. These …

Large-scale QSAR study of aromatase inhibitors using SMILES-based descriptors

A Worachartcheewan, P Mandi… - Chemometrics and …, 2014 - Elsevier
Aromatase inhibitors (AIs) represent a promising therapeutic class of anticancer agents
against estrogen receptor-positive breast cancer. Bioactivity data on pIC 50 of 973 AIs were …

Studies on non-steroidal inhibitors of aromatase enzyme; 4-(aryl/heteroaryl)-2-(pyrimidin-2-yl) thiazole derivatives

Z Sahin, M Ertas, B Berk, SN Biltekin, L Yurttas… - Bioorganic & medicinal …, 2018 - Elsevier
Steroidal and non-steroidal aromatase inhibitors target the suppression of estrogen
biosynthesis in the treatment of breast cancer. Researchers have increasingly focused on …

[HTML][HTML] Towards understanding aromatase inhibitory activity via QSAR modeling

W Shoombuatong, N Schaduangrat… - EXCLI …, 2018 - ncbi.nlm.nih.gov
Aromatase is a rate-limiting enzyme for estrogen biosynthesis that is overproduced in breast
cancer tissue. To block the growth of breast tumors, aromatase inhibitors (AIs) are employed …

Dual binding site and selective acetylcholinesterase inhibitors derived from integrated pharmacophore models and sequential virtual screening

S Gupta, CG Mohan - BioMed Research International, 2014 - Wiley Online Library
In this study, we have employed in silico methodology combining double pharmacophore
based screening, molecular docking, and ADME/T filtering to identify dual binding site …