pmx-464 and Kidney-Neoplasms

pmx-464 has been researched along with Kidney-Neoplasms* in 2 studies

Other Studies

2 other study(ies) available for pmx-464 and Kidney-Neoplasms

Article	Year
Quinols as novel therapeutic agents. 7.1 Synthesis of antitumor 4-[1-(arylsulfonyl-1H-indol-2-yl)]-4-hydroxycyclohexa-2,5-dien-1-ones by Sonogashira reactions. Journal of medicinal chemistry, 2007, Apr-05, Volume: 50, Issue:7 Interaction of 2-iodoaniline or 5-fluoro-2-iodoaniline with a range of arylsulfonyl chlorides affords sulfonamides that undergo Sonogashira couplings under thermal or microwave conditions with the alkyne 4-ethynyl-4-hydroxycyclohexa-2,5-dien-1-one followed by cyclization to 4-[1-(arylsulfonyl-1H-indol-2-yl)]-4-hydroxycyclo-hexa-2,5-dien-1-ones. This method allows for incorporation of a range of substituents into the arylsulfonyl moiety, and compounds showed selective in vitro inhibition of cancer cell lines of colon and renal origin, a feature of compounds bearing the quinol pharmacophore. Topics: Antineoplastic Agents; Cell Line, Tumor; Colonic Neoplasms; Cyclohexenes; Drug Screening Assays, Antitumor; Humans; Indoles; Kidney Neoplasms; Structure-Activity Relationship; Sulfones	2007
4-Substituted 4-hydroxycyclohexa-2,5-dien-1-ones with selective activities against colon and renal cancer cell lines. Journal of medicinal chemistry, 2003, Feb-13, Volume: 46, Issue:4 The synthesis and antitumor evaluation of a series of new heteroaromatic- and aromatic-substituted hydroxycyclohexadienones ("quinols"), and their imine counterparts, are described. The quinols were synthesized via the addition of a lithiated aromatic moiety to a quinone ketal followed by deprotection. When the aromatic portion of the molecule is a fused heterobicyclic structure (e.g., benzothiazole derivative 7a), potent in vitro antitumor activity was observed in HCT 116 (GI50 = 40 nM) and HT 29 (GI50 = 380 nM) human colon as well in as MCF-7 and MDA 468 human breast cancer cell lines. When examined on the NCI Developmental Therapeutics Screening Program in vitro screen (60 human cancer cell lines), active compounds in this series consistently displayed a highly unusual pattern of selectivity; cytotoxicity (LC50) was concentrated in certain colon and renal cell lines only. Analogue 7a also showed in vivo antitumor activity against human RXF 944XL renal xenografts in nude NMRI mice and is the focus of further study. Topics: Algorithms; Animals; Antineoplastic Agents; Benzothiazoles; Colonic Neoplasms; Computer Simulation; Cyclohexanes; Cyclohexanones; Drug Screening Assays, Antitumor; Humans; Kidney Neoplasms; Mice; Mice, Nude; Neoplasm Transplantation; Structure-Activity Relationship; Thiazoles; Transplantation, Heterologous; Tumor Cells, Cultured	2003

Article

Year

Quinols as novel therapeutic agents. 7.1 Synthesis of antitumor 4-[1-(arylsulfonyl-1H-indol-2-yl)]-4-hydroxycyclohexa-2,5-dien-1-ones by Sonogashira reactions.

Journal of medicinal chemistry, 2007, Apr-05, Volume: 50, Issue:7

Interaction of 2-iodoaniline or 5-fluoro-2-iodoaniline with a range of arylsulfonyl chlorides affords sulfonamides that undergo Sonogashira couplings under thermal or microwave conditions with the alkyne 4-ethynyl-4-hydroxycyclohexa-2,5-dien-1-one followed by cyclization to 4-[1-(arylsulfonyl-1H-indol-2-yl)]-4-hydroxycyclo-hexa-2,5-dien-1-ones. This method allows for incorporation of a range of substituents into the arylsulfonyl moiety, and compounds showed selective in vitro inhibition of cancer cell lines of colon and renal origin, a feature of compounds bearing the quinol pharmacophore.

Topics: Antineoplastic Agents; Cell Line, Tumor; Colonic Neoplasms; Cyclohexenes; Drug Screening Assays, Antitumor; Humans; Indoles; Kidney Neoplasms; Structure-Activity Relationship; Sulfones

2007

4-Substituted 4-hydroxycyclohexa-2,5-dien-1-ones with selective activities against colon and renal cancer cell lines.

Journal of medicinal chemistry, 2003, Feb-13, Volume: 46, Issue:4

The synthesis and antitumor evaluation of a series of new heteroaromatic- and aromatic-substituted hydroxycyclohexadienones ("quinols"), and their imine counterparts, are described. The quinols were synthesized via the addition of a lithiated aromatic moiety to a quinone ketal followed by deprotection. When the aromatic portion of the molecule is a fused heterobicyclic structure (e.g., benzothiazole derivative 7a), potent in vitro antitumor activity was observed in HCT 116 (GI50 = 40 nM) and HT 29 (GI50 = 380 nM) human colon as well in as MCF-7 and MDA 468 human breast cancer cell lines. When examined on the NCI Developmental Therapeutics Screening Program in vitro screen (60 human cancer cell lines), active compounds in this series consistently displayed a highly unusual pattern of selectivity; cytotoxicity (LC50) was concentrated in certain colon and renal cell lines only. Analogue 7a also showed in vivo antitumor activity against human RXF 944XL renal xenografts in nude NMRI mice and is the focus of further study.

Topics: Algorithms; Animals; Antineoplastic Agents; Benzothiazoles; Colonic Neoplasms; Computer Simulation; Cyclohexanes; Cyclohexanones; Drug Screening Assays, Antitumor; Humans; Kidney Neoplasms; Mice; Mice, Nude; Neoplasm Transplantation; Structure-Activity Relationship; Thiazoles; Transplantation, Heterologous; Tumor Cells, Cultured

2003