Search Results - "Ablordeppey, Seth"
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The Mechanistic Targets of Antifungal Agents: An Overview
Published in Mini reviews in medicinal chemistry (01-01-2016)“…Pathogenic fungi are a major causative group for opportunistic infections (OIs). AIDS patients and other immunocompromised individuals are at risk for OIs,…”
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An Evaluation of the Anticancer Properties of SYA014, a Homopiperazine-Oxime Analog of Haloperidol in Triple Negative Breast Cancer Cells
Published in Cancers (08-12-2022)“…Triple negative breast cancer (TNBC) is a type of breast cancer associated with early metastasis, poor prognosis, high relapse rates, and mortality…”
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New analogs of SYA013 as sigma-2 ligands with anticancer activity
Published in Bioorganic & medicinal chemistry (15-06-2019)“…[Display omitted] Our previous study has revealed 4-(4-(4-chlorophenyl)-1,4-diazepan-1-yl)-1-(4-fluorophenyl)butan-1-one·2HCl (SYA013) 1 as a sigma ligand with…”
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SYA 013 analogs as moderately selective sigma-2 (σ2) ligands: Structure-affinity relationship studies
Published in Bioorganic & medicinal chemistry (15-06-2019)“…[Display omitted] Several lines of evidence suggest that selective sigma-2 (σ2) ligands might be useful for the treatment of solid tumors. However, very few…”
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Evaluation of the potential of antipsychotic agents to induce catalepsy in rats: Assessment of a new, commercially available, semi-automated instrument
Published in Pharmacology, biochemistry and behavior (01-05-2014)“…Haloperidol induced catalepsy was determined using the classic bar test and a new MED Associates Catalepsy Test Chamber instrument. The dose that produced an…”
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A study of the structure-affinity relationship in SYA16263; is a D2 receptor interaction essential for inhibition of apormorphine-induced climbing behavior in mice?
Published in Bioorganic & medicinal chemistry (15-01-2021)“…[Display omitted] Dopamine (DA) and serotonin (5-HT) receptors are prime targets for the development of antipsychotics. The specific role of each receptor…”
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A study of the structure-affinity relationship in SYA16263; is a D 2 receptor interaction essential for inhibition of apormorphine-induced climbing behavior in mice?
Published in Bioorganic & medicinal chemistry (15-01-2021)“…Dopamine (DA) and serotonin (5-HT) receptors are prime targets for the development of antipsychotics. The specific role of each receptor subtype to the…”
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Enantioseparation of 5‐chloro‐2‐{2‐[3,4‐dihydroisoquinoline‐2(1H)‐yl]ethyl}‐2‐methyl‐2,3‐dihydro‐1H‐inden‐1‐one (SYA 40247), a high‐affinity 5‐HT7 receptor ligand, by HPLC–PDA using amylose tris‐(3, 5‐ dimethylphenylcarbamate) as a chiral stationary phase
Published in Biomedical chromatography (01-09-2019)“…In previous structure–activity relationship studies to identify new and selective 5‐HT7 receptor (5‐HT7R) ligands, we identified the chiral compound,…”
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New dual 5-HT1A and 5-HT7 receptor ligands derived from SYA16263
Published in European journal of medicinal chemistry (15-03-2021)“…We have previously reported that dual 5-HT1A and 5-HT7 receptor ligands might find utility as treatment options for various CNS related conditions including…”
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Synthesis and evaluation of the structural elements in alkylated tetrahydroisoquinolines for binding to CNS receptors
Published in Bioorganic & medicinal chemistry (15-11-2016)“…Diseases of the CNS are often complex and involve multiple receptor systems and thus, the treatment options for these diseases must focus on targeting the…”
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Indolo[3,2-b]quinolines: synthesis, biological evaluation and structure activity-relationships
Published in Mini reviews in medicinal chemistry (01-06-2008)“…The tetracyclic indolo[3,2-b]quinoline ring system constitutes an important structural moiety in natural products exhibiting numerous biological activities. In…”
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12
Design and synthesis of dual 5-HT1A and 5-HT7 receptor ligands
Published in Bioorganic & medicinal chemistry (15-08-2016)“…[Display omitted] 5-HT1A and 5-HT7 receptors have been at the center of discussions recently due in part to their major role in the etiology of major central…”
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Design and discovery of a high affinity, selective and β-arrestin biased 5-HT7 receptor agonist
Published in Medicinal chemistry research (01-02-2022)“…Compound 1c , 5-chloro-2-(2-(3,4-dihydroisoquinolin-2(1H)-yl)ethyl)-2,3-dihydro-1H-inden-1-one was previously reported from our laboratory showing high…”
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A Mechanistic Investigation on the Anticancer Properties of SYA013, a Homopiperazine Analogue of Haloperidol with Activity against Triple Negative Breast Cancer Cells
Published in ACS omega (29-12-2020)“…Triple-negative breast cancer (TNBC) is one of the most malignant cancers associated with early metastasis, poor clinical prognosis, and high recurrence rate…”
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CoMFA studies and in vitro evaluation of some 3-substituted benzylthio quinolinium salts as anticryptococcal agents
Published in Bioorganic & medicinal chemistry (15-11-2013)“…3-Substituted quinolinium salts. The 3-dimensional quantitative structure–activity relationship (3D-QSAR) molecular modeling technique or comparative molecular…”
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Identification of a new selective dopamine D4 receptor ligand
Published in Bioorganic & medicinal chemistry (15-06-2014)“…The dopamine D4 receptor has been shown to play key roles in certain CNS pathologies including addiction to cigarette smoking. Thus, selective D4 ligands may…”
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Enantiomeric Separation, Absolute Configuration by X‑ray Crystallographic Analysis, and Functional Evaluation of Enantiomers of the Dual Ligand, SYA0340 at 5‑HT1A and 5‑HT7A Receptors
Published in ACS omega (20-06-2023)“…We have previously identified 5-chloro-2-methyl-2-(3-(4-(pyridin-2-yl)piperazin-1-yl)propyl)-2,3-dihydro-1H-inden-1-one (SYA0340) as a dual 5-HT1A and 5-HT7…”
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Enantiomeric Separation, Absolute Configuration by X-ray Crystallographic Analysis, and Functional Evaluation of Enantiomers of the Dual Ligand, SYA0340 at 5-HT 1A and 5-HT 7A Receptors
Published in ACS omega (20-06-2023)“…We have previously identified 5-chloro-2-methyl-2-(3-(4-(pyridin-2-yl)piperazin-1-yl)propyl)-2,3-dihydro-1 -inden-1-one (SYA0340) as a dual 5-HT and 5-HT…”
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Further evaluation of the tropane analogs of haloperidol
Published in Bioorganic & medicinal chemistry letters (01-09-2014)“…Previous work from our labs has indicated that a tropane analog of haloperidol with potent D2 binding but designed to avoid the formation of MPP+-like…”
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Polyisoprenylated methylated protein methyl esterase: A putative biomarker and therapeutic target for pancreatic cancer
Published in European journal of medicinal chemistry (23-06-2014)“…Pancreatic cancer is the most deadly neoplasm with a 5-year survival rate of less than 6%. Over 90% of cases harbor K-Ras mutations, which are the most…”
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