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Natural-Products-Inspired Use of the gem-Dimethyl Group in Medicinal Chemistry

Journal of medicinal chemistry, 2018-03, Vol.61 (6), p.2166-2210

Talele, Tanaji T

2018

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Structural basis for allosteric PARP-1 retention on DNA breaks

Science (American Association for the Advancement of Science), 2020-04, Vol.368 (6486)

2020

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The “Cyclopropyl Fragment” is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules

Journal of medicinal chemistry, 2016-10, Vol.59 (19), p.8712-8756

Talele, Tanaji T

2016

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Opportunities for Tapping into Three-Dimensional Chemical Space through a Quaternary Carbon

Journal of medicinal chemistry, 2020-11, Vol.63 (22), p.13291-13315

Talele, Tanaji T

2020

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The ubiquitin-dependent ATPase p97 removes cytotoxic trapped PARP1 from chromatin

Nature cell biology, 2022-01, Vol.24 (1), p.62-73

2022

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Acetylene Group, Friend or Foe in Medicinal Chemistry

Journal of medicinal chemistry, 2020-06, Vol.63 (11), p.5625-5663

Talele, Tanaji T

2020

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Multiple transport-active binding sites are available for a single substrate on human P-glycoprotein (ABCB1)

PloS one, 2013-12, Vol.8 (12), p.e82463

2013

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Characterization of Solid Dispersion of Itraconazole Prepared by Solubilization in Concentrated Aqueous Solutions of Weak Organic Acids and Drying

Pharmaceutical research, 2016-06, Vol.33 (6), p.1456-1471

2016

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Nek2 Kinase Signaling in Malaria, Bone, Immune and Kidney Disorders to Metastatic Cancers and Drug Resistance: Progress on Nek2 Inhibitor Development

Molecules (Basel, Switzerland), 2022-01, Vol.27 (2), p.347

2022

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Sildenafil Reverses ABCB1- and ABCG2-Mediated Chemotherapeutic Drug Resistance

Cancer research (Chicago, Ill.), 2011-04, Vol.71 (8), p.3029-3041

2011

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Bafetinib (INNO-406) reverses multidrug resistance by inhibiting the efflux function of ABCB1 and ABCG2 transporters

Scientific reports, 2016-05, Vol.6 (1), p.25694-25694, Article 25694

2016

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Nilotinib potentiates anticancer drug sensitivity in murine ABCB1-, ABCG2-, and ABCC10-multidrug resistance xenograft models

Cancer letters, 2013-01, Vol.328 (2), p.307-317

2013

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Recent development in the discovery of PARP inhibitors as anticancer agents: a patent update (2016-2020)

Expert opinion on therapeutic patents, 2021-07, Vol.31 (7), p.609-623

2021

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Design and Synthesis of Human ABCB1 (P-Glycoprotein) Inhibitors by Peptide Coupling of Diverse Chemical Scaffolds on Carboxyl and Amino Termini of (S)‑Valine-Derived Thiazole Amino Acid

Journal of medicinal chemistry, 2014-05, Vol.57 (10), p.4058-4072

2014

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Lamellarin O, a pyrrole alkaloid from an Australian marine sponge, Ianthella sp., reverses BCRP mediated drug resistance in cancer cells

Marine drugs, 2014-06, Vol.12 (7), p.3818-3837

2014

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In Vitro Antibacterial Activity of Rhodanine Derivatives against Pathogenic Clinical Isolates

PloS one, 2016-10, Vol.11 (10), p.e0164227

2016

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2-O, 3-O desulfated heparin (ODSH) increases bacterial clearance and attenuates lung injury in cystic fibrosis by restoring HMGB1-compromised macrophage function

Molecular medicine (Cambridge, Mass.), 2021-07, Vol.27 (1), p.79-79, Article 79

2021

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Discovery and Structure–Activity Relationship of Novel 2,3-Dihydrobenzofuran-7-carboxamide and 2,3-Dihydrobenzofuran-3(2H)‑one-7-carboxamide Derivatives as Poly(ADP-ribose)polymerase‑1 Inhibitors

Journal of medicinal chemistry, 2014-07, Vol.57 (13), p.5579-5601

2014

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GW583340 and GW2974, human EGFR and HER-2 inhibitors, reverse ABCG2- and ABCB1-mediated drug resistance

Biochemical pharmacology, 2012-06, Vol.83 (12), p.1613-1622

2012

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2-Heteroarylimino-5-arylidene-4-thiazolidinones as a new class of non-nucleoside inhibitors of HCV NS5B polymerase

European journal of medicinal chemistry, 2013-11, Vol.69, p.931-941

2013

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Correction to: 2‑O, 3‑O desulfated heparin (ODSH) increases bacterial clearance and attenuates lung injury in cystic fibrosis by restoring HMGB1‑compromised macrophage function

Molecular medicine (Cambridge, Mass.), 2021-09, Vol.27 (1), p.98-98, Article 98

2021

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The phosphodiesterase-5 inhibitor vardenafil is a potent inhibitor of ABCB1/P-glycoprotein transporter

PloS one, 2011-04, Vol.6 (4), p.e19329

2011

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Pharmacophore Modeling of Nilotinib as an Inhibitor of ATP-Binding Cassette Drug Transporters and BCR-ABL Kinase Using a Three-Dimensional Quantitative Structure–Activity Relationship Approach

Molecular pharmaceutics, 2014-07, Vol.11 (7), p.2313-2322

2014

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Synthesis and SAR optimization of quinazolin-4(3H)-ones as poly(ADP-ribose)polymerase-1 inhibitors

European journal of medicinal chemistry, 2012-04, Vol.50, p.264-273

2012

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Thiazole-valine peptidomimetic (TTT-28) antagonizes multidrug resistance in vitro and in vivo by selectively inhibiting the efflux activity of ABCB1

Scientific reports, 2017-02, Vol.7 (1), p.42106, Article 42106

2017

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Natural-Products-Inspired Use of the gem-Dimethyl Group in Medicinal Chemistry

Structural basis for allosteric PARP-1 retention on DNA breaks

The “Cyclopropyl Fragment” is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules

Opportunities for Tapping into Three-Dimensional Chemical Space through a Quaternary Carbon

The ubiquitin-dependent ATPase p97 removes cytotoxic trapped PARP1 from chromatin

Acetylene Group, Friend or Foe in Medicinal Chemistry

Multiple transport-active binding sites are available for a single substrate on human P-glycoprotein (ABCB1)

Characterization of Solid Dispersion of Itraconazole Prepared by Solubilization in Concentrated Aqueous Solutions of Weak Organic Acids and Drying

Nek2 Kinase Signaling in Malaria, Bone, Immune and Kidney Disorders to Metastatic Cancers and Drug Resistance: Progress on Nek2 Inhibitor Development

Sildenafil Reverses ABCB1- and ABCG2-Mediated Chemotherapeutic Drug Resistance

Bafetinib (INNO-406) reverses multidrug resistance by inhibiting the efflux function of ABCB1 and ABCG2 transporters

Nilotinib potentiates anticancer drug sensitivity in murine ABCB1-, ABCG2-, and ABCC10-multidrug resistance xenograft models

Recent development in the discovery of PARP inhibitors as anticancer agents: a patent update (2016-2020)

Design and Synthesis of Human ABCB1 (P-Glycoprotein) Inhibitors by Peptide Coupling of Diverse Chemical Scaffolds on Carboxyl and Amino Termini of (S)‑Valine-Derived Thiazole Amino Acid

Lamellarin O, a pyrrole alkaloid from an Australian marine sponge, Ianthella sp., reverses BCRP mediated drug resistance in cancer cells

In Vitro Antibacterial Activity of Rhodanine Derivatives against Pathogenic Clinical Isolates

2-O, 3-O desulfated heparin (ODSH) increases bacterial clearance and attenuates lung injury in cystic fibrosis by restoring HMGB1-compromised macrophage function

Discovery and Structure–Activity Relationship of Novel 2,3-Dihydrobenzofuran-7-carboxamide and 2,3-Dihydrobenzofuran-3(2H)‑one-7-carboxamide Derivatives as Poly(ADP-ribose)polymerase‑1 Inhibitors

GW583340 and GW2974, human EGFR and HER-2 inhibitors, reverse ABCG2- and ABCB1-mediated drug resistance

2-Heteroarylimino-5-arylidene-4-thiazolidinones as a new class of non-nucleoside inhibitors of HCV NS5B polymerase

Correction to: 2‑O, 3‑O desulfated heparin (ODSH) increases bacterial clearance and attenuates lung injury in cystic fibrosis by restoring HMGB1‑compromised macrophage function

The phosphodiesterase-5 inhibitor vardenafil is a potent inhibitor of ABCB1/P-glycoprotein transporter

Pharmacophore Modeling of Nilotinib as an Inhibitor of ATP-Binding Cassette Drug Transporters and BCR-ABL Kinase Using a Three-Dimensional Quantitative Structure–Activity Relationship Approach

Synthesis and SAR optimization of quinazolin-4(3H)-ones as poly(ADP-ribose)polymerase-1 inhibitors

Thiazole-valine peptidomimetic (TTT-28) antagonizes multidrug resistance in vitro and in vivo by selectively inhibiting the efflux activity of ABCB1

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