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Banerjee S, Mahmud F, Deng S, et al. X-ray Crystallography-Guided Design, Antitumor Efficacy, and QSAR Analysis of Metabolically Stable Cyclopenta-Pyrimidinyl Dihydroquinoxalinone as a Potent Tubulin Polymerization Inhibitor. J Med Chem. 2021;64(17):13072-13095doi: 10.1021/acs.jmedchem.1c01202.
Banerjee, S., Mahmud, F., Deng, S., Ma, L., Yun, M. K., Fakayode, S. O., Arnst, K. E., Yang, L., Chen, H., Wu, Z., Lukka, P. B., Parmar, K., Meibohm, B., White, S. W., Wang, Y., Li, W., & Miller, D. D. (2021). X-ray Crystallography-Guided Design, Antitumor Efficacy, and QSAR Analysis of Metabolically Stable Cyclopenta-Pyrimidinyl Dihydroquinoxalinone as a Potent Tubulin Polymerization Inhibitor. Journal of medicinal chemistry, 64(17), 13072-13095. https://doi.org/10.1021/acs.jmedchem.1c01202
Banerjee, Souvik, et al. "X-ray Crystallography-Guided Design, Antitumor Efficacy, and QSAR Analysis of Metabolically Stable Cyclopenta-Pyrimidinyl Dihydroquinoxalinone as a Potent Tubulin Polymerization Inhibitor." Journal of medicinal chemistry vol. 64,17 (2021): 13072-13095. doi: https://doi.org/10.1021/acs.jmedchem.1c01202
Banerjee S, Mahmud F, Deng S, Ma L, Yun MK, Fakayode SO, Arnst KE, Yang L, Chen H, Wu Z, Lukka PB, Parmar K, Meibohm B, White SW, Wang Y, Li W, Miller DD. X-ray Crystallography-Guided Design, Antitumor Efficacy, and QSAR Analysis of Metabolically Stable Cyclopenta-Pyrimidinyl Dihydroquinoxalinone as a Potent Tubulin Polymerization Inhibitor. J Med Chem. 2021 Sep 09;64(17):13072-13095. doi: 10.1021/acs.jmedchem.1c01202. Epub 2021 Aug 18. PMID: 34406768.
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J Med Chem. 2021 Sep 09;64(17):13072-13095. doi: 10.1021/acs.jmedchem.1c01202. Epub 2021 Aug 18.

X-ray Crystallography-Guided Design, Antitumor Efficacy, and QSAR Analysis of Metabolically Stable Cyclopenta-Pyrimidinyl Dihydroquinoxalinone as a Potent Tubulin Polymerization Inhibitor.

Journal of medicinal chemistry

Souvik Banerjee, Foyez Mahmud, Shanshan Deng, Lingling Ma, Mi-Kyung Yun, Sayo O Fakayode, Kinsie E Arnst, Lei Yang, Hao Chen, Zhongzhi Wu, Pradeep B Lukka, Keyur Parmar, Bernd Meibohm, Stephen W White, Yuxi Wang, Wei Li, Duane D Miller

Affiliations

  1. Department of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, Tennessee 38163, United States.
  2. Department of Physical Sciences, College of STEM, University of Arkansas Fort Smith, Fort Smith, Arkansas 72913, United States.
  3. Department of Respiratory and Critical Care Medicine, Targeted Tracer Research and Development Laboratory, West China Hospital, Sichuan University, Chengdu 610041, China.
  4. Department of Structural Biology, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, United States.
  5. Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, United States.

PMID: 34406768 DOI: 10.1021/acs.jmedchem.1c01202

Abstract

Small molecules that interact with the colchicine binding site in tubulin have demonstrated therapeutic efficacy in treating cancers. We report the design, syntheses, and antitumor efficacies of new analogues of pyridopyrimidine and hydroquinoxalinone compounds with improved drug-like characteristics. Eight analogues,

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