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Can We Make Small Molecules Lean? Optimization of a Highly Lipophilic TarO Inhibitor.
Mandal, Mihirbaran; Tan, Zheng; Madsen-Duggan, Christina; Buevich, Alexei V; Caldwell, John P; Dejesus, Reynalda; Flattery, Amy; Garlisi, Charles G; Gill, Charles; Ha, Sookhee Nicole; Ho, Ginny; Koseoglu, Sandra; Labroli, Marc; Basu, Kallol; Lee, Sang Ho; Liang, Lianzhu; Liu, Jenny; Mayhood, Todd; McGuinness, Debra; McLaren, David G; Wen, Xiujuan; Parmee, Emma; Rindgen, Diane; Roemer, Terry; Sheth, Payal; Tawa, Paul; Tata, James; Yang, Christine; Yang, Shu-Wei; Xiao, Li; Wang, Hao; Tan, Christopher; Tang, Haifeng; Walsh, Paul; Walsh, Erika; Wu, Jin; Su, Jing.
  • Mandal M; Global Chemistry, ‡Early Discovery Bacteriology, §Discovery Pharmaceutical Sciences, ∥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, ⊥In Vivo Pharmacology, and #In Vitro Pharmacology, MRL, Merck & Co., Inc. , Kenilworth, New Jersey 07033, United States.
  • Tan Z; Global Chemistry, ‡Early Discovery Bacteriology, §Discovery Pharmaceutical Sciences, ∥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, ⊥In Vivo Pharmacology, and #In Vitro Pharmacology, MRL, Merck & Co., Inc. , Kenilworth, New Jersey 07033, United States.
  • Madsen-Duggan C; Global Chemistry, ‡Early Discovery Bacteriology, §Discovery Pharmaceutical Sciences, ∥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, ⊥In Vivo Pharmacology, and #In Vitro Pharmacology, MRL, Merck & Co., Inc. , Kenilworth, New Jersey 07033, United States.
  • Buevich AV; Global Chemistry, ‡Early Discovery Bacteriology, §Discovery Pharmaceutical Sciences, ∥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, ⊥In Vivo Pharmacology, and #In Vitro Pharmacology, MRL, Merck & Co., Inc. , Kenilworth, New Jersey 07033, United States.
  • Caldwell JP; Global Chemistry, ‡Early Discovery Bacteriology, §Discovery Pharmaceutical Sciences, ∥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, ⊥In Vivo Pharmacology, and #In Vitro Pharmacology, MRL, Merck & Co., Inc. , Kenilworth, New Jersey 07033, United States.
  • Dejesus R; Global Chemistry, ‡Early Discovery Bacteriology, §Discovery Pharmaceutical Sciences, ∥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, ⊥In Vivo Pharmacology, and #In Vitro Pharmacology, MRL, Merck & Co., Inc. , Kenilworth, New Jersey 07033, United States.
  • Flattery A; Global Chemistry, ‡Early Discovery Bacteriology, §Discovery Pharmaceutical Sciences, ∥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, ⊥In Vivo Pharmacology, and #In Vitro Pharmacology, MRL, Merck & Co., Inc. , Kenilworth, New Jersey 07033, United States.
  • Garlisi CG; Global Chemistry, ‡Early Discovery Bacteriology, §Discovery Pharmaceutical Sciences, ∥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, ⊥In Vivo Pharmacology, and #In Vitro Pharmacology, MRL, Merck & Co., Inc. , Kenilworth, New Jersey 07033, United States.
  • Gill C; Global Chemistry, ‡Early Discovery Bacteriology, §Discovery Pharmaceutical Sciences, ∥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, ⊥In Vivo Pharmacology, and #In Vitro Pharmacology, MRL, Merck & Co., Inc. , Kenilworth, New Jersey 07033, United States.
  • Ha SN; Global Chemistry, ‡Early Discovery Bacteriology, §Discovery Pharmaceutical Sciences, ∥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, ⊥In Vivo Pharmacology, and #In Vitro Pharmacology, MRL, Merck & Co., Inc. , Kenilworth, New Jersey 07033, United States.
  • Ho G; Global Chemistry, ‡Early Discovery Bacteriology, §Discovery Pharmaceutical Sciences, ∥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, ⊥In Vivo Pharmacology, and #In Vitro Pharmacology, MRL, Merck & Co., Inc. , Kenilworth, New Jersey 07033, United States.
  • Koseoglu S; Global Chemistry, ‡Early Discovery Bacteriology, §Discovery Pharmaceutical Sciences, ∥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, ⊥In Vivo Pharmacology, and #In Vitro Pharmacology, MRL, Merck & Co., Inc. , Kenilworth, New Jersey 07033, United States.
  • Labroli M; Global Chemistry, ‡Early Discovery Bacteriology, §Discovery Pharmaceutical Sciences, ∥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, ⊥In Vivo Pharmacology, and #In Vitro Pharmacology, MRL, Merck & Co., Inc. , Kenilworth, New Jersey 07033, United States.
  • Basu K; Global Chemistry, ‡Early Discovery Bacteriology, §Discovery Pharmaceutical Sciences, ∥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, ⊥In Vivo Pharmacology, and #In Vitro Pharmacology, MRL, Merck & Co., Inc. , Kenilworth, New Jersey 07033, United States.
  • Lee SH; Global Chemistry, ‡Early Discovery Bacteriology, §Discovery Pharmaceutical Sciences, ∥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, ⊥In Vivo Pharmacology, and #In Vitro Pharmacology, MRL, Merck & Co., Inc. , Kenilworth, New Jersey 07033, United States.
  • Liang L; Global Chemistry, ‡Early Discovery Bacteriology, §Discovery Pharmaceutical Sciences, ∥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, ⊥In Vivo Pharmacology, and #In Vitro Pharmacology, MRL, Merck & Co., Inc. , Kenilworth, New Jersey 07033, United States.
  • Liu J; Global Chemistry, ‡Early Discovery Bacteriology, §Discovery Pharmaceutical Sciences, ∥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, ⊥In Vivo Pharmacology, and #In Vitro Pharmacology, MRL, Merck & Co., Inc. , Kenilworth, New Jersey 07033, United States.
  • Mayhood T; Global Chemistry, ‡Early Discovery Bacteriology, §Discovery Pharmaceutical Sciences, ∥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, ⊥In Vivo Pharmacology, and #In Vitro Pharmacology, MRL, Merck & Co., Inc. , Kenilworth, New Jersey 07033, United States.
  • McGuinness D; Global Chemistry, ‡Early Discovery Bacteriology, §Discovery Pharmaceutical Sciences, ∥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, ⊥In Vivo Pharmacology, and #In Vitro Pharmacology, MRL, Merck & Co., Inc. , Kenilworth, New Jersey 07033, United States.
  • McLaren DG; Global Chemistry, ‡Early Discovery Bacteriology, §Discovery Pharmaceutical Sciences, ∥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, ⊥In Vivo Pharmacology, and #In Vitro Pharmacology, MRL, Merck & Co., Inc. , Kenilworth, New Jersey 07033, United States.
  • Wen X; Global Chemistry, ‡Early Discovery Bacteriology, §Discovery Pharmaceutical Sciences, ∥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, ⊥In Vivo Pharmacology, and #In Vitro Pharmacology, MRL, Merck & Co., Inc. , Kenilworth, New Jersey 07033, United States.
  • Parmee E; Global Chemistry, ‡Early Discovery Bacteriology, §Discovery Pharmaceutical Sciences, ∥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, ⊥In Vivo Pharmacology, and #In Vitro Pharmacology, MRL, Merck & Co., Inc. , Kenilworth, New Jersey 07033, United States.
  • Rindgen D; Global Chemistry, ‡Early Discovery Bacteriology, §Discovery Pharmaceutical Sciences, ∥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, ⊥In Vivo Pharmacology, and #In Vitro Pharmacology, MRL, Merck & Co., Inc. , Kenilworth, New Jersey 07033, United States.
  • Roemer T; Global Chemistry, ‡Early Discovery Bacteriology, §Discovery Pharmaceutical Sciences, ∥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, ⊥In Vivo Pharmacology, and #In Vitro Pharmacology, MRL, Merck & Co., Inc. , Kenilworth, New Jersey 07033, United States.
  • Sheth P; Global Chemistry, ‡Early Discovery Bacteriology, §Discovery Pharmaceutical Sciences, ∥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, ⊥In Vivo Pharmacology, and #In Vitro Pharmacology, MRL, Merck & Co., Inc. , Kenilworth, New Jersey 07033, United States.
  • Tawa P; Global Chemistry, ‡Early Discovery Bacteriology, §Discovery Pharmaceutical Sciences, ∥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, ⊥In Vivo Pharmacology, and #In Vitro Pharmacology, MRL, Merck & Co., Inc. , Kenilworth, New Jersey 07033, United States.
  • Tata J; Global Chemistry, ‡Early Discovery Bacteriology, §Discovery Pharmaceutical Sciences, ∥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, ⊥In Vivo Pharmacology, and #In Vitro Pharmacology, MRL, Merck & Co., Inc. , Kenilworth, New Jersey 07033, United States.
  • Yang C; Global Chemistry, ‡Early Discovery Bacteriology, §Discovery Pharmaceutical Sciences, ∥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, ⊥In Vivo Pharmacology, and #In Vitro Pharmacology, MRL, Merck & Co., Inc. , Kenilworth, New Jersey 07033, United States.
  • Yang SW; Global Chemistry, ‡Early Discovery Bacteriology, §Discovery Pharmaceutical Sciences, ∥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, ⊥In Vivo Pharmacology, and #In Vitro Pharmacology, MRL, Merck & Co., Inc. , Kenilworth, New Jersey 07033, United States.
  • Xiao L; Global Chemistry, ‡Early Discovery Bacteriology, §Discovery Pharmaceutical Sciences, ∥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, ⊥In Vivo Pharmacology, and #In Vitro Pharmacology, MRL, Merck & Co., Inc. , Kenilworth, New Jersey 07033, United States.
  • Wang H; Global Chemistry, ‡Early Discovery Bacteriology, §Discovery Pharmaceutical Sciences, ∥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, ⊥In Vivo Pharmacology, and #In Vitro Pharmacology, MRL, Merck & Co., Inc. , Kenilworth, New Jersey 07033, United States.
  • Tan C; Global Chemistry, ‡Early Discovery Bacteriology, §Discovery Pharmaceutical Sciences, ∥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, ⊥In Vivo Pharmacology, and #In Vitro Pharmacology, MRL, Merck & Co., Inc. , Kenilworth, New Jersey 07033, United States.
  • Tang H; Global Chemistry, ‡Early Discovery Bacteriology, §Discovery Pharmaceutical Sciences, ∥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, ⊥In Vivo Pharmacology, and #In Vitro Pharmacology, MRL, Merck & Co., Inc. , Kenilworth, New Jersey 07033, United States.
  • Walsh P; Global Chemistry, ‡Early Discovery Bacteriology, §Discovery Pharmaceutical Sciences, ∥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, ⊥In Vivo Pharmacology, and #In Vitro Pharmacology, MRL, Merck & Co., Inc. , Kenilworth, New Jersey 07033, United States.
  • Walsh E; Global Chemistry, ‡Early Discovery Bacteriology, §Discovery Pharmaceutical Sciences, ∥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, ⊥In Vivo Pharmacology, and #In Vitro Pharmacology, MRL, Merck & Co., Inc. , Kenilworth, New Jersey 07033, United States.
  • Wu J; Global Chemistry, ‡Early Discovery Bacteriology, §Discovery Pharmaceutical Sciences, ∥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, ⊥In Vivo Pharmacology, and #In Vitro Pharmacology, MRL, Merck & Co., Inc. , Kenilworth, New Jersey 07033, United States.
  • Su J; Global Chemistry, ‡Early Discovery Bacteriology, §Discovery Pharmaceutical Sciences, ∥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, ⊥In Vivo Pharmacology, and #In Vitro Pharmacology, MRL, Merck & Co., Inc. , Kenilworth, New Jersey 07033, United States.
J Med Chem ; 60(9): 3851-3865, 2017 05 11.
Article en En | MEDLINE | ID: mdl-28322556
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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Bibliotecas de Moléculas Pequeñas / Lípidos Límite: Animals Idioma: En Año: 2017 Tipo del documento: Article
Texto completo
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XML
PubMed Links
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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Bibliotecas de Moléculas Pequeñas / Lípidos Límite: Animals Idioma: En Año: 2017 Tipo del documento: Article