Search Results - "Palanki, Moorthy S"
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Development of novel linkers to conjugate pharmacophores to a carrier antibody
Published in Bioorganic & medicinal chemistry letters (01-07-2012)“…We have developed modified maleimide novel linkers with improved chemical stability that could potentially be used in conjugating various pharmacophores such…”
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Discovery of 3,3‘-(2,4-Diaminopteridine-6,7-diyl)diphenol as an Isozyme-Selective Inhibitor of PI3K for the Treatment of Ischemia Reperfusion Injury Associated with Myocardial Infarction
Published in Journal of medicinal chemistry (06-09-2007)“…In studies aimed toward identifying effective and safe inhibitors of kinase signaling cascades that underlie ischemia/reperfusion (I/R) injury, we synthesized…”
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Development of Prodrug 4-Chloro-3-(5-methyl-3-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino}-1,2,4-benzotriazin-7-yl)phenyl Benzoate (TG100801): A Topically Administered Therapeutic Candidate in Clinical Trials for the Treatment of Age-Related Macular Degeneration
Published in Journal of medicinal chemistry (27-03-2008)“…Age-related macular degeneration (AMD) is one of the leading causes of loss of vision in the industrialized world. Attenuating the VEGF signal in the eye to…”
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Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine—a potent, orally active Src kinase inhibitor with anti-tumor activity in preclinical assays
Published in Bioorganic & medicinal chemistry letters (01-02-2007)“…We describe the identification of benzotriazine 3, a potent and orally active Src inhibitor with desirable pharmacokinetic properties and anti-tumor activity…”
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Development of a long acting human growth hormone analog suitable for once a week dosing
Published in Bioorganic & medicinal chemistry letters (15-01-2013)“…Human growth hormone was conjugated to a carrier aldolase antibody, using a novel linker by connecting a disulphide bond in growth hormone to a lysine-94 amine…”
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Discovery and preliminary structure–activity relationship studies of novel benzotriazine based compounds as Src inhibitors
Published in Bioorganic & medicinal chemistry letters (01-11-2006)“…We report the SAR studies of a series of structurally novel benzotriazine analogs as inhibitors of Src. The 3-(2-(1-pyrrolidinyl)-ethoxy)phenyl analog ( 43)…”
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Inhibitors of ABL and the ABL-T315I mutation
Published in Current topics in medicinal chemistry (01-07-2008)“…Chronic myelogenous leukemia (CML) is a hematological stem cell disorder caused by increased and unregulated growth of myeloid cells in the bone marrow, and…”
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Special issue of Medicinal Chemistry Research in honor of Professor Gary L. Grunewald
Published in Medicinal chemistry research (01-07-2021)Get full text
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Inhibitors of AP-1 and NF-kappa B mediated transcriptional activation: therapeutic potential in autoimmune diseases and structural diversity
Published in Current medicinal chemistry (01-01-2002)“…Cytokines and chemokines play a very important role in a number of inflammatory diseases. In activated T cells, transcription factors such as the activator…”
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Inhibition of Nuclear Factor-κB in T Cells Suppresses Lung Fibrosis
Published in American journal of respiratory and critical care medicine (15-12-2007)Get full text
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The design and preliminary structure–activity relationship studies of benzotriazines as potent inhibitors of Abl and Abl-T315I enzymes
Published in Bioorganic & medicinal chemistry letters (01-11-2007)“…We describe the design, synthesis and structure–activity relationship studies in optimizing a series of benzotriazine compounds as potent inhibitors of both…”
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Functional analogs of CC-1065 and the duocarmycins incorporating the 9a-(chloromethyl)-1,2,9,9a-tetrahydrocyclopropa[c]benz[e]indol-4-one (C2BI) alkylation subunit: synthesis and preliminary DNA alkylation studies
Published in Journal of the American Chemical Society (01-11-1992)Get full text
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Inhibition of Nuclear Factor-{kappa}B in T Cells Suppresses Lung Fibrosis
Published in American journal of respiratory and critical care medicine (15-12-2007)“…Cytokines secreted by T cells play a pivotal role in the pathogenesis of lung injury and fibrosis, and the transcription factors nuclear factor (NF)-kappaB and…”
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Inhibitors of NF-κB and AP-1 Gene Expression: SAR Studies on the Pyrimidine Portion of 2-Chloro-4-trifluoromethylpyrimidine-5-[N-(3‘,5‘-bis(trifluoromethyl)phenyl)carboxamide]
Published in Journal of medicinal chemistry (19-10-2000)“…We investigated the structure−activity relationship studies of N-[3,5-bis(trifluoromethyl)phenyl][2-chloro-4-(trifluoromethyl)pyrimidin-5-yl]carboxamide (1),…”
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2-Chloro-4-(trifluoromethyl)pyrimidine-5-N-(3‘,5‘-bis(trifluoromethyl)phenyl)- carboxamide: A Potent Inhibitor of NF-κB- and AP-1-Mediated Gene Expression Identified Using Solution-Phase Combinatorial Chemistry
Published in Journal of medicinal chemistry (12-02-1998)“…Described is the identification of a novel series of compounds that blocks the activation of two key transcription factors, AP-1 and NF-κB. These transcription…”
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Immunospecific Reduction of Antioligonucleotide Antibody-Forming Cells with a Tetrakis-oligonucleotide Conjugate (LJP 394), a Therapeutic Candidate for the Treatment of Lupus Nephritis
Published in Journal of medicinal chemistry (01-06-1995)“…A discrete tetravalent conjugate, 7a (LJP 394), consisting of four oligonucleotides attached to a common carrier or platform was prepared. Single-stranded…”
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The design and synthesis of novel orally active inhibitors of AP-1 and NF-kappaB mediated transcriptional activation. SAR of in vitro and in vivo studies
Published in Bioorganic & medicinal chemistry letters (17-11-2003)“…We have developed novel orally active quinazoline analogues as inhibitors of AP-1 and NF-kappaB mediated transcriptional activation. Among the derivatives…”
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Structure-activity relationship studies of ethyl 2-[(3-methyl-2,5-dioxo(3-pyrrolinyl))amino]-4-(trifluoromethyl)pyrimidine-5-carboxylate: an inhibitor of AP-1 and NF-kappaB mediated gene expression
Published in Bioorganic & medicinal chemistry letters (16-09-2002)“…Several analogues of ethyl 2-[(3-methyl-2,5-dioxo(3-pyrrolinyl))amino]-4-(trifluoromethyl)pyrimidine-5-carboxylate (1) were synthesized and tested as…”
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