Synthesis and biological evaluation of novel cabazitaxel analogues
文献类型：期刊论文
| 作者 | Ren, Sumei1,2; Zhang, Minmin3 ; Wang, Yujie1; Guo, Jia1; Wang, Junfei1; Li, Yingxia1; Ding, Ning1
|
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| 出版日期 | 2021-07-01 |
| 卷号 | 41页码:12 |
| 关键词 | Tritium extraction Hydrogen isotopes Eutectic Pb-Li Fusion fuel cycle Cabazitaxel Docetaxel Taxel Anticancer Semi-synthesis 10-Deacetylbaccatin III Cytotoxicity |
| ISSN号 | 0968-0896 |
| DOI | 10.1016/j.bmc.2021.116224 |
| 通讯作者 | Ding, Ning(dingning@fudan.edu.cn) |
| 英文摘要 | Cabazitaxel is one of the most recently FDA-approved taxane anticancer agent. In view of the advantages in preclinical and clinical data of cabazitaxel over former toxoids, the synthesis and biological evaluation of novel cabazitaxel analogues were conducted. First, a novel semi-synthesis of cabazitaxel was described. This strategy is concise and efficient, which needs five steps from the 10-deacetylbaccatin III (10-DAB) moiety and a commercially available C13 side chain precursor with a 32% overall yield. Besides, this strategy avoids using many hazardous reagents that involved in the previously reported processes. Then, a panel of cabazitaxel analogues were prepared basing on this strategy. The cytotoxicity evaluations showed that the majority of these cabazitaxel analogues are potent against both A549 and KB cells and their corresponding drug-resistant cell lines KB/VCR, and A549/T, respectively. Further in vivo antitumor efficacies assessment of 7,10-di-O-methylthiomethyl (MTM) modified cabazitaxel (compounds 16 and 19) on SCID mice A549 xenograft model showed they both had similar antitumor activity to the cabazitaxel. Since compound 19 was observed causing more body wight loss on the mice than 16, these preliminary studies suggest 16 might be a potent drug candidate for further preclinical evaluation. |
| WOS关键词 | BETA-LACTAMS ; TAXANE ; PACLITAXEL ; TAXOIDS ; DESIGN |
| 资助项目 | National Major Scientific and Technological Special Project of China for Significant New Drugs Development[2018ZX09101004-003] ; National Major Scientific and Technological Special Project of China for Significant New Drugs Development[2018ZX09101-004-006-008] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000661664000009 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/297183]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Ding, Ning |
| 作者单位 | 1.Fudan Univ, Sch Pharm, Dept Med Chem, Shanghai 201203, Peoples R China 2.Shenzhen Univ, Hlth Sci Ctr, Sch Pharmaceut Sci, Shenzhen 518060, Guangdong, Peoples R China 3.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Div Antitumor Pharmacol, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Ren, Sumei,Zhang, Minmin,Wang, Yujie,et al. Synthesis and biological evaluation of novel cabazitaxel analogues[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2021,41:12. |
| APA | Ren, Sumei.,Zhang, Minmin.,Wang, Yujie.,Guo, Jia.,Wang, Junfei.,...&Ding, Ning.(2021).Synthesis and biological evaluation of novel cabazitaxel analogues.BIOORGANIC & MEDICINAL CHEMISTRY,41,12. |
| MLA | Ren, Sumei,et al."Synthesis and biological evaluation of novel cabazitaxel analogues".BIOORGANIC & MEDICINAL CHEMISTRY 41(2021):12. |
入库方式： OAI收割
来源：上海药物研究所
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