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封面介绍CDK4/6 inhibitors have become pivotal therapeutic agents in the treatment of breast cancer, lung cancer, and other malignancies. A systematic examination of the synthetic routes of eight representative compounds— palbociclib and dalpiciclib, ribociclib and volbociclib, abemaciclib and tericiclib, as well as trilaciclib and lerociclib—selected based on their time of market authorization and structural homology, is provided by Li, Gao, and Zhang on page 315. Special emphasis is placed on the role of novel reaction systems and advanced synthetic strategies in enhancing process efficiency. -
封面介绍The isolation of one new dihydroisocoumarin (1) and three known compounds (2~4) from the marine fungus Cladosporium sp. MDW-211 was reported by Wang, Zheng, Zhang, Gao, Kong, Li, Wang, and Cao on page 684. The absolute configuration of compound 1 was determined by X-ray diffraction analysis. Evaluation using a zebrafish model demonstrated that compound 3 exhibited significant pro-angiogenic activity at concen-trations of 20 and 40 μmol/L. -
封面介绍Despite the advances in other site-selective methylations, there are scarce reports on C4 methylation of indoles and combination of a carbonyl rearrangement with C—H methylation on indole ring. Herein, the C4 methylation of indoles and the steric controlled C4-methy- lation/carbonyl migration are reported by Xie, Cheng, and An on page 475. The large steric hindrance at carbonyl facilitates the carbonyl migration, which provides a straightforward protocol for the synthesis of C2/C4 disubstituted indoles. -
封面介绍A series of 17β-amino acid ester modified pregnane derivatives were reported by Gu, Yao, Zhong, Wen, Yang, Liu, and Gan on page 545. Among them, ester derivatives 7h and 7d displayed significant antiprolifer-ative activities against SKOV 3 and T47D cells, outper-forming abiraterone. The findings highlight that esterifi-cation can effectively enhance cell permeability and antitumor efficacy, providing a promising amino ac-id-based strategy for developing new steroid anticancer drugs.
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本期栏目
综述与进展
研究论文
研究简报
亮点述评