Anti-cancer chalcones: Structural and molecular target perspectives

DK Mahapatra, SK Bharti, V Asati - European journal of medicinal chemistry, 2015 - Elsevier
Abstract Chalcone or (E)-1, 3-diphenyl-2-propene-1-one scaffold remained a fascination
among researchers in the 21st century due to its simple chemistry, ease of synthesis and a …

Coexistence of passive and carrier-mediated processes in drug transport

K Sugano, M Kansy, P Artursson, A Avdeef… - Nature reviews Drug …, 2010 - nature.com
The permeability of biological membranes is one of the most important determinants of the
pharmacokinetic processes of a drug. Although it is often accepted that many drug …

Fundamental aspects of DMPK optimization of targeted protein degraders

C Cantrill, P Chaturvedi, C Rynn, JP Schaffland… - Drug Discovery …, 2020 - Elsevier
Highlights•Degraders are an emerging modality which fall into the 'beyond rule of
5'space.•Poor permeability and solubility are critical features limiting oral absorption.• …

[HTML][HTML] In vitro Development of Chemotherapy and Targeted Therapy Drug-Resistant Cancer Cell Lines: A Practical Guide with Case Studies

M McDermott, AJ Eustace, S Busschots, L Breen… - Frontiers in …, 2014 - frontiersin.org
The development of a drug-resistant cell line can take from 3 to 18 months. However, little is
published on the methodology of this development process. This article will discuss key …

Predicting clearance mechanism in drug discovery: extended clearance classification system (ECCS)

MV Varma, SJ Steyn, C Allerton, AF El-Kattan - Pharmaceutical research, 2015 - Springer
Early prediction of clearance mechanisms allows for the rapid progression of drug discovery
and development programs, and facilitates risk assessment of the pharmacokinetic …

Bioavailability study of berberine and the enhancing effects of TPGS on intestinal absorption in rats

W Chen, YQ Miao, DJ Fan, SS Yang, X Lin, LK Meng… - Aaps Pharmscitech, 2011 - Springer
Berberine chloride (BBR) is a natural isoquinoline alkaloid extracted from medicinal herbs. It
has been reported that the intestinal absorption of BBR is very low. In this study, the absolute …

Berberine: a potential phytochemical with multispectrum therapeutic activities

PR Vuddanda, S Chakraborty… - Expert opinion on …, 2010 - Taylor & Francis
Importance of the field: The use of traditional medicines of natural origin is being
encouraged for the treatment of chronic disorders, as synthetic drugs in such cases may …

Usefulness of Caco-2/HT29-MTX and Caco-2/HT29-MTX/Raji B coculture models to predict intestinal and colonic permeability compared to Caco-2 monoculture

I Lozoya-Agullo, F Araujo… - Molecular …, 2017 - ACS Publications
The Caco-2 cellular monolayer is a widely accepted in vitro model to predict human
permeability but suffering from several and critical limitations. Therefore, some alternative …

Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination

MVS Varma, RS Obach, C Rotter… - Journal of medicinal …, 2010 - ACS Publications
Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall
elimination (Fg), and fraction escaping hepatic elimination (Fh). In this study, using a …

Enhanced oral paclitaxel absorption with vitamin E-TPGS: effect on solubility and permeability in vitro, in situ and in vivo

MVS Varma, R Panchagnula - European journal of pharmaceutical …, 2005 - Elsevier
Solubility and permeability being important determinants of oral drug absorption, this study
was aimed to investigate the effect of d-α-tocopheryl polyethylene glycol 1000 succinate …