Synthesis and biological activity of a novel series of 6-substituted thieno[2,3-d]pyrimidine antifolate inhibitors of purine biosynthesis with selectivity for high affinity folate receptors over the reduced folate carrier and proton-coupled folate transporter for cellular entry

Journal of Medicinal Chemistry

Volumn 52, Issue 9, 2009, Pages 2940-2951

  Deng, Yijun ^a   Zhou, Xilin ^b   Desmoulin, Sita Kugel ^a   Wu, Jianmei ^c   Cherian, Christina ^c   Hou, Zhanjun ^c   Matherly, Larry H ^a,c   Gangjee, Aleem ^b  

^a WAYNE STATE UNIVERSITY SCHOOL OF MEDICINE   (United States)

^b DUQUESNE UNIVERSITY   (United States)

^c KARMANOS CANCER INSTITUTE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

5 AMINO 4 IMIDAZOLECARBOXAMIDE; ADENOSINE; FOLATE RECEPTOR; FOLIC ACID; FOLIC ACID ANTAGONIST; FOLINIC ACID; LOMETREXOL; METHOTREXATE; N [4 [2 (2 AMINO 4 OXO 3,4 DIHYDROTHIENO[2,3 D]PYRIMIDIN 6 YL)ETHYL]BENZOYL]GLUTAMIC ACID; N [4 [3 (2 AMINO 4 OXO 3,4 DIHYDROTHIENO[2,3 D]PYRIMIDIN 6 YL)PROPYL]BENZOYL]GLUTAMIC ACID; N [4 [4 (2 AMINO 4 OXO 3,4 DIHYDROTHIENO[2,3 D]PYRIMIDIN 6 YL)BUTYL]BENZOYL]GLUTAMIC ACID; N [4 [5 (2 AMINO 4 OXO 3,4 DIHYDROTHIENO[2,3 D]PYRIMIDIN 6 YL)PENTYL]BENZOYL]GLUTAMIC ACID; N [4 [6 (2 AMINO 4 OXO 3,4 DIHYDROTHIENO[2,3 D]PYRIMIDIN 6 YL)HEXYL]BENZOYL]GLUTAMIC ACID; N [4 [7 (2 AMINO 4 OXO 3,4 DIHYDROTHIENO[2,3 D]PYRIMIDIN 6 YL)HEPTYL]BENZOYL]GLUTAMIC ACID; N [4 [8 (2 AMINO 4 OXO 3,4 DIHYDROTHIENO[2,3 D]PYRIMIDIN 6 YL)OCTYL]BENZOYL]GLUTAMIC ACID; PEMETREXED; PHOSPHORIBOSYLAMINOIMIDAZOLECARBOXAMIDE FORMYLTRANSFERASE; PHOSPHORIBOSYLGLYCINAMIDE FORMYLTRANSFERASE; PURINE; RALTITREXED; REDUCED FOLATE CARRIER; THIENO[2,3 D]PYRIMIDINE DERIVATIVE; THYMIDINE; UNCLASSIFIED DRUG;

ANIMAL CELL; ANTINEOPLASTIC ACTIVITY; ARTICLE; BINDING AFFINITY; CANCER INHIBITION; CELL PROLIFERATION; COMPETITIVE INHIBITION; CONTROLLED STUDY; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG SYNTHESIS; DRUG UPTAKE; ENZYME ACTIVITY; ENZYME INHIBITION; HUMAN; HUMAN CELL; NONHUMAN; PROTEIN EXPRESSION; PURINE SYNTHESIS; RADIOASSAY;

ANIMALS; ANION TRANSPORT PROTEINS; ANTINEOPLASTIC AGENTS; BIOLOGICAL TRANSPORT; CARRIER PROTEINS; CELL PROLIFERATION; CHO CELLS; CRICETINAE; CRICETULUS; FOLIC ACID ANTAGONISTS; GENE EXPRESSION REGULATION; HUMANS; HYDROGEN BONDING; MEMBRANE TRANSPORT PROTEINS; NUCLEOSIDES; PHOSPHORIBOSYLAMINOIMIDAZOLECARBOXAMIDE FORMYLTRANSFERASE; PROTONS; PURINES; PYRIMIDINES; RECEPTORS, CELL SURFACE; SUBSTRATE SPECIFICITY; TRANSFECTION;

EID: 65649129763     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm8011323     Document Type: Article

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