Search Results - "Kadayat, Tara"
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Potent inhibitory activity of hydroxylated 2-benzylidene-3,4-dihydronaphthalen-1(2H)-ones on LPS-stimulated reactive oxygen species production in RAW 264.7 macrophages
Published in Bioorganic & medicinal chemistry letters (01-10-2022)“…[Display omitted] •Sixty-six 2-benzylidene-3,4-dihydronaphthalen-1(2H)-ones were synthesized.•6 and 7‑Hydroxyl substituents exhibited potent ROS inhibitory…”
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2
Di-indenopyridines as topoisomerase II-selective anticancer agents: Design, synthesis, and structure–activity relationships
Published in Bioorganic & medicinal chemistry (15-08-2023)“…[Display omitted] •Twenty-three novel di-indeno[1,2-b]pyridines were synthesized.•Di- and tri-hydroxylation on di-indenopyridines were favorable for the topo…”
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3
4-Flourophenyl-substituted 5H-indeno[1,2-b]pyridinols with enhanced topoisomerase IIα inhibitory activity: Synthesis, biological evaluation, and structure–activity relationships
Published in Bioorganic chemistry (01-11-2021)“…[Display omitted] •Thirty six 4-flourophenyl-substituted 5H-indeno[1,2-b]pyridinols were synthesized.•Majority of compounds displayed potent topo IIα…”
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4
Design, synthesis, and antitumor evaluation of 2,4,6-triaryl pyridines containing chlorophenyl and phenolic moiety
Published in European journal of medicinal chemistry (01-06-2012)“…We have designed and synthesized a series of 2,4,6-triaryl pyridine derivatives containing chlorophenyl and phenolic moeity at 2- and 4- position of the…”
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5
Design, synthesis, biological evaluation, structure-activity relationship study, and mode of action of 2-phenol-4,6-dichlorophenyl-pyridines
Published in Bioorganic chemistry (01-09-2018)“…[Display omitted] •2-Phenol-4,6-dichlorophenyl-substituted pyridines (1–27) were designed and synthesized.•Compounds (1–18) exhibited potent and selective topo…”
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Synthesis of a unique dimethyl thiazoline containing intermediate of novel peroxisome proliferator-activated receptors(PPAR)δ agonists
Published in Tetrahedron letters (12-12-2018)“…[Display omitted] •Method for unique dimethyl thiazoline containing intermediate of PPARδ agonists.•TBAHS as catalyst for efficient coupling of 11 with…”
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Targeting Peroxisome Proliferator-Activated Receptor Delta (PPARδ): A Medicinal Chemistry Perspective
Published in Journal of medicinal chemistry (24-09-2020)“…One of the three subtypes of the peroxisome proliferator-activated receptor (PPAR) functioning as a transcription factor is the PPARβ or PPARδ. PPARδ is…”
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Antioxidative and anti-inflammatory activity of psiguadial B and its halogenated analogues as potential neuroprotective agents
Published in Bioorganic chemistry (01-08-2021)“…[Display omitted] •Psiguadial B and its halogenated derivatives were synthesized.•Synthetic route involved a simple and one-step reaction with inexpensive…”
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9
HIGHLY POTENT AND SELECTIVE PPAR DELTA AGONIST REVERSES MEMORY DEFICITS IN ALZHEIMER'S DISEASE MOUSE MODELS
Published in IBRO neuroscience reports (01-10-2023)Get full text
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10
Topoisomerase I and II inhibitory activity, cytotoxicity, and structure–activity relationship study of dihydroxylated 2,6-diphenyl-4-aryl pyridines
Published in Bioorganic & medicinal chemistry (01-07-2015)“…Total thirty-six dihydroxylated 2,6-diphenyl-4-aryl pyridines were designed, synthesized and tested for topo I and II inhibitory activity and cytotoxicity for…”
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11
An orally available inverse agonist of estrogen-related receptor gamma showed expanded efficacy for the radioiodine therapy of poorly differentiated thyroid cancer
Published in European journal of medicinal chemistry (01-11-2020)“…Estrogen-related receptor gamma (ERRγ) is the NR3B subgroup of associated transcription factors. In this report, a new generation of a potent and selective…”
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12
Dihydroxylated 2,4,6-triphenyl pyridines: Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure–activity relationship study
Published in European journal of medicinal chemistry (01-03-2012)“…Twelve dihydroxylated 2,4,6-triphenyl pyridines were designed and synthesized which contain hydroxyl groups at ortho, meta or para position of 2- and 6-phenyl,…”
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13
Synthesis and biological evaluation of 2-phenol-4-chlorophenyl-6-aryl pyridines as topoisomerase II inhibitors and cytotoxic agents
Published in Bioorganic chemistry (01-06-2016)“…[Display omitted] •Thirty-six 2-phenol-4-chlorophenyl-6-aryl pyridines were synthesized.•Evaluated for topo I and II inhibitory activity, and…”
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14
Enantioselective Synthesis of a Novel Thiazoline Core as a Potent Peroxisome Proliferator-Activated Receptor δ Agonist
Published in ACS omega (28-02-2018)“…The convergent and enantioselective synthesis of a highly potent human peroxisome proliferator-activated receptor delta agonist is presented. More…”
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15
Targeting the Nuclear Receptor-Binding SET Domain Family of Histone Lysine Methyltransferases for Cancer Therapy: Recent Progress and Perspectives
Published in Journal of medicinal chemistry (28-10-2021)“…Nuclear receptor-binding SET domain (NSD) proteins are a class of histone lysine methyltransferases (HKMTases) that are amplified, mutated, translocated, or…”
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16
Antitrypanosomal Chloronitrobenzamides
Published in Journal of medicinal chemistry (14-03-2024)“…Human African trypanosomiasis (HAT), a neglected tropical disease caused by Trypanosoma brucei gambiense (Tbg) or Trypanosoma brucei rhodesiense (Tbr), remains…”
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Synthesis and biological evaluation of 4,7,9-trisubstituted benzoxazepines as antileishmanial agents
Published in Bioorganic & medicinal chemistry letters (01-12-2024)“…[Display omitted] •New anti-leishmanial chemotypes.•Leishmania lead validation.•Leishmania structure–activity relationships.•Leishmania pharmacophore. Herein…”
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18
Discovery of the therapeutic potential of PPARδ agonist bearing 1,3,4- thiadiazole in inflammatory disorders
Published in European journal of medicinal chemistry (05-12-2024)“…As a defense mechanism against deleterious stimuli, inflammation plays a vital role in the development of many disorders, including atherosclerosis,…”
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19
Topoisomerase IIα inhibitory and antiproliferative activity of dihydroxylated 2,6-diphenyl-4-fluorophenylpyridines: Design, synthesis, and structure-activity relationships
Published in Bioorganic & medicinal chemistry letters (15-03-2022)“…[Display omitted] •Synthesis of fluorine functionalities substituted 2,4,6-triphenylpyridines.•Strong antiproliferative activity by compounds 11, 12, 37, 50,…”
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A Series of Novel Terpyridine-Skeleton Molecule Derivants Inhibit Tumor Growth and Metastasis by Targeting Topoisomerases
Published in Journal of medicinal chemistry (12-02-2015)“…A series of novel terpyridine-skeleton molecules containing conformational rigidity, 14 containing benzo[4,5]furo[3,2-b]pyridine core and 15 comprising…”
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