Photodynamic therapy holds great promise as a non-invasive anticancer tool against drug-resistant cancers. However, highly effective, non-toxic, and reliable photosensitizers with operability under hypoxic conditions remain to be developed. Herein, we took the advantageous properties of COUPY fluorophores and cyclometalated Ir(III) complexes to develop
Anna Rovira+10 more
openaire +6 more sources
Structure - Activity Relationship of Mutant KatG from INH resistant Mycobacterium tuberculosis
Mutation in katG gene of Mycobacterium tuberculosis encoding catalase-peroxidase that damage its enzyme activities is well associated with isoniazid (INH) resistance. The katG gene from INH resistant strain of M.
Purkan Purkan+4 more
doaj +1 more source
Structure-activity relationships of 3-substituted-5,5- diphenylhydantoins as potential antiproliferative and antimicrobial agents [PDF]
A series of twelve 3-substituted-5,5-diphenylhydantoins was synthesized, including some whose anticonvulsant activities have already been reported in the literature.
Trišović Nemanja+7 more
doaj +1 more source
To investigate and compare the pharmacokinetic profile and anti-cancer activity of fluorinated and iodinated photosensitizers (PSs), the 3-(1′-(o-fluorobenzyloxy)ethyl pyropheophorbide and the corresponding meta-(m-) and para (p-) fluorinated analogs ...
Taur Prakash Pandurang+8 more
doaj +1 more source
Absorption of Unconjugated Bile Acids from the Perfused Jejunum of the Anesthetized Rat: Structure–Activity Relationships and Rate‐Limiting Steps [PDF]
Peer Reviewed ; https://deepblue.lib.umich.edu/bitstream/2027.42/145508/1/lipd12052_am.pdf ; https://deepblue.lib.umich.edu/bitstream/2027.42/145508/2/lipd12052 ...
Dupas, Jean‐louis+2 more
openaire +3 more sources
Structure–Activity Relationship Study Reveals ML240 and ML241 as Potent and Selective Inhibitors of p97 ATPase [PDF]
AbstractTo discover more potent p97 inhibitors, we carried out a structure–activity relationship study of the quinazoline scaffold previously identified from our HTS campaigns. Two improved inhibitors, ML240 and ML241, inhibit p97 ATPase with IC50 values of 100 nM.
Raymond J. Deshaies+5 more
openaire +6 more sources
Design and Synthesis of Orally Bioavailable Piperazine Substituted 4(1H)-Quinolones with Potent Antimalarial Activity: Structure–Activity and Structure–Property Relationship Studies [PDF]
Malaria deaths have been decreasing over the last 10-15 years, with global mortality rates having fallen by 47% since 2000. While the World Health Organization (WHO) recommends the use of artemisinin-based combination therapies (ACTs) to combat malaria, the emergence of artemisinin resistant strains underscores the need to develop new antimalarial ...
Raghupathi Neelarapu+12 more
openaire +4 more sources
Investigating the Structure–Activity Relationship of the Insecticidal Natural Product Rocaglamide
The natural product Rocaglamide (1), isolated from the tree Aglaia elliptifolia, is a compelling but also challenging lead structure for crop protection.
Roger G. Hall+6 more
doaj +1 more source
Synthesis and Fungicidal Activity of β-Carboline Alkaloids and Their Derivatives
A series of β-Carboline derivatives were designed, synthesized, and evaluated for their fungicidal activities in this study. Several derivatives electively exhibited fungicidal activities against some fungi.
Zhibin Li+5 more
doaj +1 more source
A series of new N-phenylacetamide derivatives containing 4-arylthiazole moieties was designed and synthesized by introducing the thiazole moiety into the amide scaffold.
Hui Lu, Xia Zhou, Lei Wang, Linhong Jin
doaj +1 more source