Discovery of cytotoxic dolastatin 10 analogues with N-terminal modifications

Journal of Medicinal Chemistry

Volumn 57, Issue 24, 2014, Pages 10527-10543

  Maderna, Andreas ^a   Doroski, Matthew ^a   Subramanyam, Chakrapani ^a   Porte, Alexander ^a   Leverett, Carolyn A ^a   Vetelino, Beth C ^a   Chen, Zecheng ^a   Risley, Hud ^a   Parris, Kevin ^a   Pandit, Jayvardhan ^a   Varghese, Alison H ^a   Shanker, Suman ^a   Song, Cynthia ^a   Sukuru, Sai Chetan K ^a   Farley, Kathleen A ^a   Wagenaar, Melissa M ^a   Shapiro, Michael J ^a   Musto, Sylvia ^a   Lam, My Hanh ^a   Loganzo, Frank ^a   O'Donnell, Christopher J ^a   more..

^a PFIZER INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 METHYL PROLYL N [3 METHOXY 1 [2 [1 METHOXY 2 METHYL 3 OXO 3 [[2 PHENYL 1 (1,3 THIAZOL 2 YL)ETHYL]AMINO]PROPYL]PYRROLIDIN 1 YL] 5 METHYL 1 OXOHEPTAN 4 YL]N METHYL VALINAMIDE; 2 METHYL PROLYL N[3 METHOXY 1 [2 [1 METHOXY 2 METHYL 3 OXO 3 [[2 PHENYL 1 (1,3 THIAZOL 2YL)ETHYL]AMINO]PROPYL]PYRROLIDIN 1 YL] 5 METHYL 1 OXOHEPTAN 4 YL]N METHYL VALINAMIDE; 2 METHYLALANYL N[3 METHOXY 1 [2 [1 METHOXY 2 METHYL 3 OXO 3 [[2 PHENYL 1 (1,3 THIAZOL 2 YL)ETHYL]AMINO]PROPYL]PYRROLIDIN 1 YL] 5 METHYL 1 OXOHEPTAN 4 YL]N METHYL VALINAMIDE; AMIDE; CARBON; CYTOTOXIC AGENT; DIMER; N,2 DIMETHYLALANYL N [4 [2 [3 [(1 CARBOXY 2 PHENYLETHYL)AMINO] 1 METHOXY 2 METHYL 3 OXOPROPYL]PYRROLIDIN 1 YL] 2 METHOXY 1 [1 METHYLPROPYL] 4 OXOBUTYL]N METHYL VALINAMIDE; N,2 DIMETHYLALANYL N[3 METHOXY 1 [2 [1 METHOXY 2 METHYL 3 OXO 3 [[2 PHENYL 1 (1,3 THIAZOL 2 YL)ETHYL]AMINO]PROPYL]PYRROLIDIN 1 YL] 5 METHYL 1 OXOHEPTAN 4 YL]N METHYL VALINAMIDE; N[1 [[3 METHOXY 1 [2 [1 METHOXY 2 METHYL 3 OXO 3 [[2 PHENYL 1 (1,3 THIAZOL 2 YL)ETHYL]AMINO]PROPYL]PYRROLIDIN 1 YL] 5 METHYL 1 OXOHEPTAN 4 YL](METHYL)AMINO] 3 METHYL 1 OXOBUTAN 2 YL] 2 METHYLPIPERIDINE 2 CARBOXAMIDE; N[3 METHOXY 1 [2 [1 METHOXY 2 METHYL 3 OXO 3[[2 PHENYL 1 (1,3 THIAZOL 2 YL)ETHYL]AMINO]PROPYL]PYRROLIDIN 1 YL] 5 METHYL 1 OXOHEPTAN 4 YL]N METHYL L VALINAMIDE; TETRAMER; TUBULIN; UNCLASSIFIED DRUG; ANTINEOPLASTIC AGENT; DEPSIPEPTIDE; DOLASTATIN 10;

AMINO TERMINAL SEQUENCE; ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CELL PROLIFERATION ASSAY; CELL VIABILITY ASSAY; CHEMICAL MODIFICATION; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG CLEARANCE; DRUG DESIGN; DRUG POTENCY; DRUG SYNTHESIS; ELIMINATION HALF-LIFE; HUMAN; HUMAN CELL; INTRINSIC CLEARANCE; MALE; MAXIMUM PLASMA CONCENTRATION; MICROSOME; NONHUMAN; PROTEIN STRUCTURE; RAT; SINGLE DRUG DOSE; SUBSTITUTION REACTION; TIME TO MAXIMUM PLASMA CONCENTRATION; TUMOR CELL; VOLUME OF DISTRIBUTION; ANIMAL; CELL CULTURE; CELL PROLIFERATION; CHEMICAL STRUCTURE; CHEMISTRY; CYTOLOGY; DRUG DEVELOPMENT; DRUG EFFECTS; DRUG SCREENING; LIVER CELL; LIVER MICROSOME; METABOLISM; NEOPLASMS; PROTEIN CONFORMATION; STRUCTURE ACTIVITY RELATION; TANDEM MASS SPECTROMETRY; WISTAR RAT; X RAY CRYSTALLOGRAPHY;

ANIMALS; ANTINEOPLASTIC AGENTS; AREA UNDER CURVE; CELL PROLIFERATION; CELLS, CULTURED; CRYSTALLOGRAPHY, X-RAY; DEPSIPEPTIDES; DRUG DISCOVERY; DRUG SCREENING ASSAYS, ANTITUMOR; HEPATOCYTES; HUMANS; MALE; MICROSOMES, LIVER; MODELS, MOLECULAR; MOLECULAR STRUCTURE; NEOPLASMS; PROTEIN CONFORMATION; RATS; RATS, WISTAR; STRUCTURE-ACTIVITY RELATIONSHIP; TANDEM MASS SPECTROMETRY; TUBULIN;

EID: 84920109887     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm501649k     Document Type: Article

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