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SAR towards indoline and 3-azaindoline classes of IDO1 inhibitors

Bioorganic & medicinal chemistry letters, 2021-09, Vol.47, p.128214-128214, Article 128214

2021

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Variations in the C-unit of bedaquiline provides analogues with improved biology and pharmacology

Bioorganic & medicinal chemistry, 2020-01, Vol.28 (1), p.115213, Article 115213

2020

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Structure activity relationships of benzyl C-region analogs of 2-(3-fluoro-4-methylsulfonamidophenyl)propanamides as potent TRPV1 antagonists

Bioorganic & medicinal chemistry, 2015-11, Vol.23 (21), p.6844-6854

2015

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Design, synthesis and biological evaluation of (2S,3R,4R,5S,6R)-5-fluoro-6-(hydroxymethyl)-2-aryltetrahydro-2H-pyran-3,4-diols as potent and orally active SGLT dual inhibitors

Bioorganic & medicinal chemistry letters, 2018-11, Vol.28 (21), p.3446-3453

2018

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N-sulfonyl peptide-hybrids as a new class of dengue virus protease inhibitors

European journal of medicinal chemistry, 2023-05, Vol.251, p.115227-115227, Article 115227

2023

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Synthesis, biological evaluation, and molecular docking analysis of phenstatin based indole linked chalcones as anticancer agents and tubulin polymerization inhibitors

Bioorganic chemistry, 2020-12, Vol.105, p.104447, Article 104447

2020

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Discovery of potent and selective CDK8 inhibitors from an HSP90 pharmacophore

Bioorganic & medicinal chemistry letters, 2016-03, Vol.26 (5), p.1443-1451

2016

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Synthesis and biological evaluation of clovamide analogues as potent anti-neuroinflammatory agents in vitro and in vivo

European journal of medicinal chemistry, 2018-05, Vol.151, p.261-271

2018

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Structure-activity relationships for unit C pyridyl analogues of the tuberculosis drug bedaquiline

Bioorganic & medicinal chemistry, 2019-04, Vol.27 (7), p.1283-1291

2019

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Design, synthesis, and evaluation of amphiphilic sofalcone derivatives as potent Gram-positive antibacterial agents

European journal of medicinal chemistry, 2020-09, Vol.202, p.112596, Article 112596

2020

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2-(4-Methylsulfonylaminophenyl) propanamide TRPV1 antagonists: Structure–activity relationships in the B and C-regions

Bioorganic & medicinal chemistry, 2012-02, Vol.20 (3), p.1310-1318

2012

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Discovery of Dioxino[2,3-f]quinazoline derivative VEGFR-2 inhibitors exerting significant antipro-liferative activity in HUVECs and mice

European journal of medicinal chemistry, 2019-08, Vol.175, p.349-356

2019

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Biarylmethoxy 2-nitroimidazooxazine antituberculosis agents: Effects of proximal ring substitution and linker reversal on metabolism and efficacy

Bioorganic & medicinal chemistry letters, 2015-09, Vol.25 (18), p.3804-3809

2015

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Fluoromethylcyclopropylamine derivatives as potential in vivo toxicophores – A cautionary disclosure

Bioorganic & medicinal chemistry letters, 2019-02, Vol.29 (4), p.560-562

2019

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Discovery of IDO1 inhibitors containing a decahydroquinoline, decahydro-1,6-naphthyridine, or octahydro-1H-pyrrolo[3,2-c]pyridine scaffold

Bioorganic & medicinal chemistry letters, 2021-10, Vol.49, p.128314-128314, Article 128314

2021

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Naa10p Inhibits Beige Adipocyte-Mediated Thermogenesis through N-α-acetylation of Pgc1α

Molecular cell, 2019-11, Vol.76 (3), p.500-515.e8

2019

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Emerging roles of protein O-GlcNAcylation in cardiovascular diseases: Insights and novel therapeutic targets

Pharmacological research, 2021-03, Vol.165, p.105467-105467, Article 105467

2021

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Identification of a κ-opioid agonist as a potent and selective lead for drug development against human African trypanosomiasis

Biochemical pharmacology, 2010-11, Vol.80 (10), p.1478-1486

2010

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Chalcones bearing a 3,4,5-trimethoxyphenyl motif are capable of selectively inhibiting oncogenic K-Ras signaling

Bioorganic & medicinal chemistry letters, 2020-06, Vol.30 (11), p.127144-127144, Article 127144

2020

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Structure and Mechanism of Acetylation by the N-Terminal Dual Enzyme NatA/Naa50 Complex

Structure (London), 2019-07, Vol.27 (7), p.1057-1070.e4

2019

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Indomethacin-based PROTACs as pan-coronavirus antiviral agents

European journal of medicinal chemistry, 2021-12, Vol.226, p.113814-113814, Article 113814

2021

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Dysregulation of histone methyltransferases in breast cancer – Opportunities for new targeted therapies?

Molecular oncology, 2016-12, Vol.10 (10), p.1497-1515

2016

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β- N-Acetylhexosaminidase: What's in a name…?

Biotechnology advances, 2010-11, Vol.28 (6), p.682-693

2010

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Site-specific interplay between O-GlcNAcylation and phosphorylation in cellular regulation

FEBS letters, 2010-06, Vol.584 (12), p.2526-2538

2010

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Mechanism of Cross-talk between H2B Ubiquitination and H3 Methylation by Dot1L

Cell, 2019-03, Vol.176 (6), p.1490-1501.e12

2019

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SAR towards indoline and 3-azaindoline classes of IDO1 inhibitors

Variations in the C-unit of bedaquiline provides analogues with improved biology and pharmacology

Structure activity relationships of benzyl C-region analogs of 2-(3-fluoro-4-methylsulfonamidophenyl)propanamides as potent TRPV1 antagonists

Design, synthesis and biological evaluation of (2S,3R,4R,5S,6R)-5-fluoro-6-(hydroxymethyl)-2-aryltetrahydro-2H-pyran-3,4-diols as potent and orally active SGLT dual inhibitors

N-sulfonyl peptide-hybrids as a new class of dengue virus protease inhibitors

Synthesis, biological evaluation, and molecular docking analysis of phenstatin based indole linked chalcones as anticancer agents and tubulin polymerization inhibitors

Discovery of potent and selective CDK8 inhibitors from an HSP90 pharmacophore

Synthesis and biological evaluation of clovamide analogues as potent anti-neuroinflammatory agents in vitro and in vivo

Structure-activity relationships for unit C pyridyl analogues of the tuberculosis drug bedaquiline

Design, synthesis, and evaluation of amphiphilic sofalcone derivatives as potent Gram-positive antibacterial agents

2-(4-Methylsulfonylaminophenyl) propanamide TRPV1 antagonists: Structure–activity relationships in the B and C-regions

Discovery of Dioxino[2,3-f]quinazoline derivative VEGFR-2 inhibitors exerting significant antipro-liferative activity in HUVECs and mice

Biarylmethoxy 2-nitroimidazooxazine antituberculosis agents: Effects of proximal ring substitution and linker reversal on metabolism and efficacy

Fluoromethylcyclopropylamine derivatives as potential in vivo toxicophores – A cautionary disclosure

Discovery of IDO1 inhibitors containing a decahydroquinoline, decahydro-1,6-naphthyridine, or octahydro-1H-pyrrolo[3,2-c]pyridine scaffold

Naa10p Inhibits Beige Adipocyte-Mediated Thermogenesis through N-α-acetylation of Pgc1α

Emerging roles of protein O-GlcNAcylation in cardiovascular diseases: Insights and novel therapeutic targets

Identification of a κ-opioid agonist as a potent and selective lead for drug development against human African trypanosomiasis

Chalcones bearing a 3,4,5-trimethoxyphenyl motif are capable of selectively inhibiting oncogenic K-Ras signaling

Structure and Mechanism of Acetylation by the N-Terminal Dual Enzyme NatA/Naa50 Complex

Indomethacin-based PROTACs as pan-coronavirus antiviral agents

Dysregulation of histone methyltransferases in breast cancer – Opportunities for new targeted therapies?

β- N-Acetylhexosaminidase: What's in a name…?

Site-specific interplay between O-GlcNAcylation and phosphorylation in cellular regulation

Mechanism of Cross-talk between H2B Ubiquitination and H3 Methylation by Dot1L

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