220913-43-9Relevant articles and documents
ISOTHIOCYANATE-ANDROGEN RECEPTOR INHIBITOR CONJUGATES FOR APOPTOSIS AND/OR FERROPTOSIS INDUCTION IN CANCER CELLS
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Paragraph 0040; 0154; 0156, (2021/04/17)
Isothiocyanate (ITC)-androgen receptor (AR) inhibitor conjugates for apoptosis induction in cancer cells are described. The conjugates can have electrophilicity blocked with an agent such as N-acetyl cysteine. When administered in combination with a glutathione (GSH)-depleting agent, the conjugates result in ferroptosis of cancer cells.
ALLOSTERIC INHIBITOR OF WEE1 KINASE
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Page/Page column 57, (2020/02/23)
Disclosed is a method for selecting a cancer therapeutic for a patient that involves assaying a tumor biopsy sample from the subject to detect PAXIP1 expression, and selecting a WEE1 inhibitor as the cancer therapeutic if PAXIP1 is detected in the tumor biopsy sample.
Novel cyclin-dependent kinase 9 (CDK9) inhibitor with suppression of cancer stemness activity against non-small-cell lung cancer
Wang, Xin,Yu, Chenhua,Wang, Cheng,Ma, Yakun,Wang, Tianqi,Li, Yao,Huang, Zhi,Zhou, Manqian,Sun, Peiqing,Zheng, Jianyu,Yang, Shengyong,Fan, Yan,Xiang, Rong
supporting information, (2019/08/02)
A series of novel, highly potent, selective CDK9 inhibitors with cancer stem cells (CSCs) inhibition activity were designed and synthesized for non-small-cell lung cancer (NSCLC) therapy. Structure-activity relationship analysis based on enzymatic and cellular activities led to the discovery of a promising inhibitor 21e. 21e potently inhibited CDK9 with IC50 value of 11 nM and suppressed the stemness properties of NSCLC effectively. It could decrease the stemness phenotypes of NSCLC cells, including tumor sphere formation, side-population and stemness markers abundance. 21e displayed good selectivity over the CDK family kinases and kinase profiling assay against 381 kinases. In addition, 21e inhibited cell proliferation, colony-formation, and cell cycle progression and induced apoptosis in NSCLC. In H1299 xenograft mouse model, a once-daily dose of compound 21e at 20 mg/kg significantly suppressed the tumor growth without obvious toxicity. Studies of mechanisms of action indicated that 21e efficiently inhibited CDK9 signaling pathway and stemness both in vitro and in vivo. Collectively, 21e as a novel CDK9 inhibitor with CSCs inhibition properties could be a promising agent for the treatment of NSCLC.
Camptothecin analogs and methods of preparation thereof
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, (2008/06/13)
A compound and a method of synthesizing a compound having the following general formula (1): wherein R1 and R2 are independently the same or different and are hydrogen, an alkyl group, an alkenyl group, a benzyl group, an alkynyl group, an alkoxy group, a
Camptothecin analogs and methods of preparation thereof
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, (2008/06/13)
The present invention provides generally a compound having the following general formula (1): wherein R1 and R2 are independently the same or different and are hydrogen, an alkyl group, an alkenyl group, a benzyl group, an alkynyl group, an alkoxyl group,