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Your search keyword '"Furness K."' showing total 2 results
Start Over Author "Furness K." Topic carbazoles
2 results on '"Furness K."'

1. Synthetic approaches to indolo[6,7-a]pyrrolo[3,4-c]carbazoles: potent cyclin D1/CDK4 inhibitors.

Author

Faul MM, Engler TA, Sullivan KA, Grutsch JL, Clayton MT, Martinelli MJ, Pawlak JM, LeTourneau M, Coffey DS, Pedersen SW, Kolis SP, Furness K, Malhotra S, Al-awar RS, and Ray JE

Subjects
Acetamides chemistry, Acetates chemistry, Cyclin-Dependent Kinase 4, Humans, Maleimides chemistry, Oxidants chemistry, Photochemistry, Structure-Activity Relationship, Antineoplastic Agents chemical synthesis, Carbazoles chemical synthesis, Cyclin D1 antagonists & inhibitors, Cyclin-Dependent Kinases antagonists & inhibitors, Enzyme Inhibitors chemical synthesis, Indoles chemistry, Proto-Oncogene Proteins, Pyrroles chemistry
Abstract

Synthesis of indolo[6,7-a]pyrrolo[3,4-c]carbazoles 1, a new class of cyclin D1/CDK4 inhibitors, by oxidation of the corresponding aryl indolylmaleimides 2, will be described. Two approaches to the synthesis of 2 were identified that required new methods for the synthesis of 7-substituted indole acetamides 3 and N-methyl (indol-7-yl)oxoacetates 6. The chemistry developed enabled introduction of functionality (-OR, NR(2)) at C(12) and N(13) facilitating structure-activity relationship (SAR) evaluation of this indolocarbazole platform.

Published
2004
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2. Novel, potent and selective cyclin D1/CDK4 inhibitors: indolo[6,7-a]pyrrolo[3,4-c]carbazoles.

Author

Engler TA, Furness K, Malhotra S, Sanchez-Martinez C, Shih C, Xie W, Zhu G, Zhou X, Conner S, Faul MM, Sullivan KA, Kolis SP, Brooks HB, Patel B, Schultz RM, DeHahn TB, Kirmani K, Spencer CD, Watkins SA, Considine EL, Dempsey JA, Ogg CA, Stamm NB, Anderson BD, Campbell RM, Vasudevan V, and Lytle ML

Subjects
Calcium-Calmodulin-Dependent Protein Kinase Type 2, Calcium-Calmodulin-Dependent Protein Kinases antagonists & inhibitors, Cell Cycle drug effects, Cell Division drug effects, Cell Line, Tumor, Cyclic AMP-Dependent Protein Kinases antagonists & inhibitors, Cyclin-Dependent Kinase 4, Drug Screening Assays, Antitumor, Enzyme Inhibitors chemical synthesis, Enzyme Inhibitors pharmacology, Humans, Phosphorylation, Rubidium metabolism, Structure-Activity Relationship, Antineoplastic Agents chemical synthesis, Antineoplastic Agents pharmacology, Carbazoles chemical synthesis, Carbazoles pharmacology, Cyclin D1 antagonists & inhibitors, Cyclin-Dependent Kinases antagonists & inhibitors, Proto-Oncogene Proteins
Abstract

The synthesis and CDK inhibitory properties of a series of indolo[6,7-a]pyrrolo[3,4-c]carbazoles is reported. In addition to their potent CDK activity, the compounds display antiproliferative activity against two human cancer cell lines. These inhibitors also effect strong G1 arrest in these cell lines and inhibit Rb phosphorylation at Ser780 consistent with inhibition of cyclin D1/CDK4.

Published
2003
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