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Your search keyword '"DiMeo, Susan V."' showing total 4 results
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4 results on '"DiMeo, Susan V."'

1. Development of a Scalable Synthesis toward a KRAS G12C Inhibitor Building Block Bearing an All-Carbon Quaternary Stereocenter, Part 2: Asymmetric Synthesis via Shi Epoxidation.

Author

Tan, Zhulin, Ju, Xuan, Wu, Hao, Dong, Weitong, Leung, Joyce C., Hou, Xiaowen, Lee, Heewon, Granger, Alice, Paolillo, Joshua M., DiMeo, Susan V., Chen, Chengsheng, Wu, Linglin, Lorenz, Jon C., Sarvestani, Max, Buono, Frederic, Frutos, Rogelio, Tampone, Thomas G., Huang, Xiaojun, Zhang, Gulin, and Wang, Yuwen

Published
2024
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2. Development of a Scalable Synthesis toward a KRAS G12C Inhibitor Building Block Bearing an All-Carbon Quaternary Stereocenter, Part 1: From Discovery Route to Kilogram-Scale Production.

Author

Leung, Joyce C., Xu, Yibo, Radomkit, Suttipol, Lee, Jaehee, Kim, Wan Shin, Reeves, Jonathan T., Dong, Weitong, Jang, Hwanjong, Hou, Xiaowen, Lorenz, Jon C., Shao, Xiaole, Byrne, Denis, Johnson, Joe, Brundage, Anthony, Valentin, Clement, Beyer, Phouvieng, DiMeo, Susan V., Qu, Bo, Li, Ruoshi, and Sarvestani, Max

Published
2024
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4. Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. 3. Structure activity relationships at C3(1,2).

Author

Yue EW, Higley CA, DiMeo SV, Carini DJ, Nugiel DA, Benware C, Benfield PA, Burton CR, Cox S, Grafstrom RH, Sharp DM, Sisk LM, Boylan JF, Muckelbauer JK, Smallwood AM, Chen H, Chang CH, Seitz SP, and Trainor GL

Subjects
Antineoplastic Agents chemical synthesis, Antineoplastic Agents chemistry, Antineoplastic Agents pharmacology, Apoptosis, Cell Division drug effects, Crystallography, X-Ray, Cyclin-Dependent Kinase 2, Cyclin-Dependent Kinase 4, Drug Screening Assays, Antitumor, Enzyme Inhibitors chemistry, Enzyme Inhibitors pharmacology, Humans, Kinetics, Models, Molecular, Protein Serine-Threonine Kinases antagonists & inhibitors, Pyrazoles chemistry, Pyrazoles pharmacology, Structure-Activity Relationship, Tumor Cells, Cultured, CDC2-CDC28 Kinases, Cyclin-Dependent Kinases antagonists & inhibitors, Enzyme Inhibitors chemical synthesis, Proto-Oncogene Proteins, Pyrazoles chemical synthesis
Abstract

The identification of indeno[1,2-c]pyrazol-4-ones as inhibitors of cyclin-dependent kinases (CDKs) has led to the discovery of a series of novel and potent compounds. Herein, we report the effects of substitutions at C3 of the indeno[1,2-c]pyrazol-4-one core with alkyls, heterocycles, and substituted phenyls. Substitutions at the para position of the phenyl ring at C3 were generally well-tolerated; however, larger groups were generally inactive. For alkyls directly attached to C3, longer chain substituents were not tolerated; however, shorter alkyl groups and cyclic alkyls were acceptable. In general, the heterocycles at C3 gave the most potent analogues. One such heterocycle, 24j, was examined in detail and was determined to have a biological profile consistent with CDK inhibition. An X-ray crystal structure of one of the alkyl compounds, 13q, complexed with CDK2 was determined and showed the inhibitor residing in the adenosine 5'-triphosphate pocket of the enzyme.

Published
2002
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