Royal Society of Chemistry (RSC)

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The developability of heteroaromatic and heteroaliphatic rings – do some have a better pedigree as potential drug molecules than others?
Royal Society of Chemistry (RSC) - Tập 3 Số 9 - Trang 1062 - 2012
Timothy J. Ritchie, Simon J. F. Macdonald, Simon Peace, Stephen D. Pickett, Christopher N. Luscombe
Are pyridazines privileged structures?
Royal Society of Chemistry (RSC) - Tập 2 Số 10 - Trang 935-941
Camille G. Wermuth

Compared to carbocyclic drug molecules, pyridazine-containing drugs present additional interaction possibilities, as illustrated here for the antirhinoviral agent R 61837.

Druggability assessment of mammalian Per–Arnt–Sim [PAS] domains using computational approaches
Royal Society of Chemistry (RSC) - Tập 10 Số 7 - Trang 1126-1137
João Vicente Braga de Souza, Sylvia Reznikov, Ruidi Zhu, Agnieszka K. Bronowska

Protein dynamics finely tune the “druggability” of mammalian PAS-B domains, as assessed by atomistic molecular dynamics simulations and hotspot mapping.

Synthesis and cytotoxicity evaluation of regioisomeric substituted N-phenyl-3′-(chrom-4-one-3-yl)-isoxazolidines: induction of apoptosis through a mitochondrial-dependent pathway
Royal Society of Chemistry (RSC) - Tập 4 Số 6 - Trang 972 - 2013
Gagandeep Singh, Amritpal Kaur, Vishal Sharma, Nitasha Suri, Parduman Raj Sharma, Ajit Kumar Saxena, Mohan Paul S. Ishar
Design, synthesis and biological activity evaluation of regioisomeric spiro-(indoline-isoxazolidines) in the inhibition of TNF-α-induced ICAM-1 expression on human endothelial cells
Royal Society of Chemistry (RSC) - Tập 3 Số 12 - Trang 1536 - 2012
Shashwat Malhotra, Sakshi Balwani, Ashish Dhawan, Raunak Raunak, Yogesh Kumar, Brajendra K. Singh, Carl Erik Olsen, Ashok K. Prasad, Virinder S. Parmar, Balaram Ghosh
Tumor cell resistance against targeted therapeutics: the density of cultured glioma tumor cells enhances Stat3 activity and offers protection against the tyrosine kinase inhibitor canertinib
Royal Society of Chemistry (RSC) - Tập 8 Số 1 - Trang 96-102
Viktoria von Manstein, Bernd Groner

Tumor cell resistance to drug treatment severely limits the therapeutic success of treatment.

Novel valdecoxib derivatives by ruthenium(<scp>ii</scp>)-promoted 1,3-dipolar cycloaddition of nitrile oxides with alkynes – synthesis and COX-2 inhibition activity
Royal Society of Chemistry (RSC) - Tập 9 Số 3 - Trang 534-544
Silvia Roscales, Nicole Bechmann, Daniel Holger Weiß, Martin Köckerling, Jens Pietzsch, Torsten Knieß

By Ru(ii)-promoted 1,3-dipolar cycloaddition of nitrile oxides with alkynes 3,4-diaryl-substituted isoxazoles are formed in one step, showing high inhibition potency for COX-2.

Structure–activity relationships for the synthesis of selective cyclooxygenase 2 inhibitors: an overview (2009–2016)
Royal Society of Chemistry (RSC) - Tập 8 Số 3 - Trang 492-500
Gabriele Carullo, F. Galligano, Francesca Aiello

An original point of view inside the SAR studies to develop new selective COX-2 inhibitors.

Exploring cinnamic acid scaffold: development of promising neuroprotective lipophilic antioxidants
Royal Society of Chemistry (RSC) - Tập 6 Số 6 - Trang 1043-1053
Daniel Chavarria, Tiago Silva, Daniel Martins, Joana Bravo, Teresa Summavielle, Jorge Garrido, Fernanda Borges

New lipophilic hydroxycinnamic acid based derivatives were designed and synthesized and their antioxidant and neuroprotective activities evaluated.

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