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Literature DB >> 28488201

Synthesis of deuterium-enriched and fluorine-substituted plinabulin derivatives and evaluation of their antitumor activities.

Zhongpeng Ding¹, Yingwei Hou², Shixiao Wang², Tianwen Sun^1,2, Mingxu Ma¹, Huashi Guan^1,2, Wenbao Li^3,4.

Abstract

Deuterium-enriched and fluorine-substituted compounds have been widely applied in drug discovery due to their advantages in the studies of clinical pharmacokinetics and metabolic profiles. Herein we synthesized a library of deuterated and fluorine-substituted plinabulin derivatives, and all 15 D- or F-compounds were characterized by MS, [Formula: see text] NMR and [Formula: see text]. Their antitumor activities were evaluated against human Jurkat T lymphocyte cells.

Entities: Chemical Species

Keywords: Antitumor activity; Deuterium-enriched; Fluorine-substituted; Parallel synthesis; Plinabulin

Mesh：

Substances：

Year: 2017 PMID： 28488201 DOI： 10.1007/s11030-017-9742-y

Source DB: PubMed Journal: Mol Divers ISSN： 1381-1991 Impact factor: 2.943

13 in total

1. Stable-isotope probing as a tool in microbial ecology.

Authors: S Radajewski; P Ineson; N R Parekh; J C Murrell
Journal: Nature Date: 2000-02-10 Impact factor: 49.962

2. Anti-microtubule 'plinabulin' chemical probe KPU-244-B3 labeled both alpha- and beta-tubulin.

Authors: Yuri Yamazaki; Makiko Sumikura; Koushi Hidaka; Hiroyuki Yasui; Yoshiaki Kiso; Fumika Yakushiji; Yoshio Hayashi
Journal: Bioorg Med Chem Date: 2010-03-23 Impact factor: 3.641

3. Medicinal chemistry and chemical biology of diketopiperazine-type antimicrotubule and vascular-disrupting agents.

Authors: Yoshio Hayashi; Yuri Yamazaki-Nakamura; Fumika Yakushiji
Journal: Chem Pharm Bull (Tokyo) Date: 2013 Impact factor: 1.645

4. Vascular effects of plinabulin (NPI-2358) and the influence on tumour response when given alone or combined with radiation.

Authors: Lotte B Bertelsen; Yuan Yuan Shen; Thomas Nielsen; Hans Stødkilde-Jørgensen; G Kenneth Lloyd; Dietmar W Siemann; Michael R Horsman
Journal: Int J Radiat Biol Date: 2011-11 Impact factor: 2.694

5. Synthesis and structure-activity relationship study of antimicrotubule agents phenylahistin derivatives with a didehydropiperazine-2,5-dione structure.

Authors: Yuri Yamazaki; Koji Tanaka; Benjamin Nicholson; Gordafaried Deyanat-Yazdi; Barbara Potts; Tomoko Yoshida; Akiko Oda; Takayoshi Kitagawa; Sumie Orikasa; Yoshiaki Kiso; Hiroyuki Yasui; Miki Akamatsu; Takumi Chinen; Takeo Usui; Yuki Shinozaki; Fumika Yakushiji; Brian R Miller; Saskia Neuteboom; Michael Palladino; Kaneo Kanoh; George Kenneth Lloyd; Yoshio Hayashi
Journal: J Med Chem Date: 2012-01-20 Impact factor: 7.446

6. Phase 1 first-in-human trial of the vascular disrupting agent plinabulin(NPI-2358) in patients with solid tumors or lymphomas.

Authors: Monica M Mita; Matthew A Spear; Lorrin K Yee; Alain C Mita; Elisabeth I Heath; Kyriakos P Papadopoulos; Kristine C Federico; Steven D Reich; Ofelia Romero; Lisa Malburg; MaryJo Pilat; G Kenneth Lloyd; Saskia T C Neuteboom; Gillian Cropp; Edward Ashton; Patricia M LoRusso
Journal: Clin Cancer Res Date: 2010-12-01 Impact factor: 12.531

1. Biological activity and interaction mechanism of the diketopiperazine derivatives as tubulin polymerization inhibitors.

Authors: Zhenhua Tian; Yanyan Chu; Hui Wang; Lili Zhong; Mengyan Deng; Wenbao Li
Journal: RSC Adv Date: 2018-01-03 Impact factor: 4.036

1 in total

Synthesis of deuterium-enriched and fluorine-substituted plinabulin derivatives and evaluation of their antitumor activities.

1. Stable-isotope probing as a tool in microbial ecology.

2. Anti-microtubule 'plinabulin' chemical probe KPU-244-B3 labeled both alpha- and beta-tubulin.

3. Medicinal chemistry and chemical biology of diketopiperazine-type antimicrotubule and vascular-disrupting agents.

4. Vascular effects of plinabulin (NPI-2358) and the influence on tumour response when given alone or combined with radiation.

5. Synthesis and structure-activity relationship study of antimicrotubule agents phenylahistin derivatives with a didehydropiperazine-2,5-dione structure.

6. Phase 1 first-in-human trial of the vascular disrupting agent plinabulin(NPI-2358) in patients with solid tumors or lymphomas.

7. Stable isotope constraints on Holocene carbon cycle changes from an Antarctic ice core.

8. Synthesis of indazole based diarylurea derivatives and their antiproliferative activity against tumor cell lines.

9. Using deuterium in drug discovery: leaving the label in the drug.

10. Expression, purification, assay, and crystal structure of perdeuterated human arginase I.

1. Biological activity and interaction mechanism of the diketopiperazine derivatives as tubulin polymerization inhibitors.