Search Results - "Unadkat, Vishal"
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Synthesis and structure–activity relationship of potent, selective and orally active anthranilamide-based factor Xa inhibitors: Application of weakly basic sulfoximine group as novel S4 binding element
Published in European journal of medicinal chemistry (01-12-2012)“…A novel series of potent and efficacious factor Xa inhibitors which possesses sulfoximine moiety as novel S4 binding element in anthranilamide chemotype has…”
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Bioisosteric replacement of dihydropyrazole of 4S-(-)-3-(4-chlorophenyl)-N-methyl-N'-[(4-chlorophenyl)-sulfonyl]-4-phenyl-4,5-dihydro-1H-pyrazole-1-caboxamidine (SLV-319) a potent CB1 receptor antagonist by imidazole and oxazole
Published in Bioorganic & medicinal chemistry letters (01-02-2008)“…Design, synthesis and conformational analysis of few imidazole and oxazole as bioisosters of…”
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Rational design-aided discovery of novel 1,2,4-oxadiazole derivatives as potential EGFR inhibitors
Published in Bioorganic chemistry (01-09-2021)“…[Display omitted] A molecular dynamics-based sampling of epidermal growth factor receptor tyrosine kinase (EGFR-TK) was carried out to search for energetically…”
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Identification of 1,2,4-Oxadiazoles-Based Novel EGFR Inhibitors: Molecular Dynamics Simulation-Guided Identification and in vitro ADME Studies
Published in OncoTargets and therapy (01-01-2022)“…In this work, we have identified heterocyclic derivatives with 1,2,4 oxadiazole scaffold mimicking the functions of tyrosine kinase inhibitors. Fourteen…”
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Abstract 1616: Preclinical characterization of KSHN001126, a novel, differentiated and steroidal oral selective estrogen receptor degrader (SERD)
Published in Cancer research (Chicago, Ill.) (04-04-2023)“…Abstract Fulvestrant (FLV) (Faslodex®) is the only clinically approved steroidal SERD that requires painful intramuscular administration. Several oral SERDs…”
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Abstract 4043: KSHN001034: An intramuscular prodrug of fulvestrant to treat estrogen-receptor (ER) positive advanced metastatic breast cancer
Published in Cancer research (Chicago, Ill.) (15-06-2022)“…Abstract Purpose: Breast cancer (BC) remains a considerable health concern, with over 75% of total cases accounting for ER+ BC. Fulvestrant, a selective…”
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Abstract 3356: Comparative analysis of approved and undertrial SERDs in estrogen receptor-α (ERα): An in-silico approach
Published in Cancer research (Chicago, Ill.) (15-06-2022)“…Abstract Background: Despite recent advancements in early detection and treatment, breast cancer is the second most common cancer affecting women globally,…”
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Abstract 3077: Pharmacological profiling of KSHN001034 - A novel prodrug of Fulvestrant with improved efficacy
Published in Cancer research (Chicago, Ill.) (04-04-2023)“…Abstract Purpose: KSHN001034, a Fulvestrant (FLV) prodrug, was developed to enhance solubility and achieve higher FLV plasma exposures. Currently, Faslodex®…”
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Design, Synthesis of Novel, Potent, Selective, Orally Bioavailable Adenosine A2A Receptor Antagonists and Their Biological Evaluation
Published in Journal of medicinal chemistry (26-01-2017)“…Our initial structure–activity relationship studies on 7-methoxy-4-morpholino-benzothiazole derivatives featured by aryloxy-2-methylpropanamide moieties at the…”
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Design, Synthesis of Novel, Potent, Selective, Orally Bioavailable Adenosine A 2A Receptor Antagonists and Their Biological Evaluation
Published in Journal of medicinal chemistry (26-01-2017)“…Our initial structure-activity relationship studies on 7-methoxy-4-morpholino-benzothiazole derivatives featured by aryloxy-2-methylpropanamide moieties at the…”
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Bioisosteric replacement of dihydropyrazole of 4 S-(−)-3-(4-chlorophenyl)- N-methyl- N′-[(4-chlorophenyl)-sulfonyl]-4-phenyl-4,5-dihydro-1H-pyrazole-1-caboxamidine (SLV-319) a potent CB1 receptor antagonist by imidazole and oxazole
Published in Bioorganic & medicinal chemistry letters (2008)“…Design, synthesis and conformational analysis of few imidazole and oxazole as bioisosters of 4 S-(−)-3-(4-chlorophenyl)- N-methyl-…”
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Bioisosteric replacement of dihydropyrazole of 4S-(-)-3-(4-chlorophenyl)-N-methyl-N'-[(4-chlorophenyl)-sulfonyl]-4-phenyl-4,5-dihydro-lH-pyrazole-1-caboxamidine (SLV-319) a potent CB1 receptor antagonist by imidazole and oxazole
Published in Bioorganic & medicinal chemistry letters (2008)Get full text
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