160446-15-1Relevant articles and documents
Preparation and application of Sigma-2 fluorescent ligand
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Paragraph 0070; 0075-0076; 0078, (2021/06/06)
The invention mainly relates to synthesis of a series of sigma-2 fluorescent ligands and application of the sigma-2 fluorescent ligands in the fields of pharmacy and medicine, specifically to a series of compounds containing benzopyran structures, wherein the compounds have high affinity activity and selectivity to a sigma-2 receptor, have good affinity activity to the sigma-2 receptor, and have diagnosis and treatment effects on tumor cells, brain cells of patients with Alzheimer's disease, and other cells highly expressing the sigma-2 receptor.
2, 4, 7 -substituted pyrimido indole compound antitumor drug resistance effect
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Paragraph 0027; 0056-0059, (2021/09/08)
The invention relates to 2, 4 and 7 - tri-substituted pyrimido-indole structural compounds which can inhibit the growth of various drug-resistant tumor cells, and in particular, can efficiently inhibit doxorubicin resistant breast cancer. Cisplatin-resistant lung cancer and cisplatin liver cancer cell proliferation. In addition, the compounds of the present invention can inhibit the formation of drug-resistant tumor cell clones at very low concentrations and inhibit P glycoprotein and ABCG2 transport in vitro functions. The invention also relates to a preparation method of the compound and an application of the compound in tumor treatment or adjuvant therapy.
Structure-Based Discovery of Pyrimidine Aminobenzene Derivatives as Potent Oral Reversal Agents against P-gp- And BCRP-Mediated Multidrug Resistance
Qiu, Qianqian,Zou, Feng,Li, Huilan,Shi, Wei,Zhou, Daoguang,Zhang, Ping,Li, Teng,Yin, Ziyu,Cai, Zilong,Jiang, Yuxuan,Huang, Wenlong,Qian, Hai
, p. 6179 - 6197 (2021/06/01)
Overexpression of ATP binding cassette (ABC) transporters, including P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP), is an important factor leading to multidrug resistance (MDR) in cancer treatments. Three subclasses of dual inhibitors of P-gp and BCRP were designed based on the active moieties of BCRP inhibitors, tyrosine kinase inhibitors, and P-gp inhibitors, of which compound 21 possessed low cytotoxicity, high reversal potency, and good lipid distribution coefficient. 21 also increased the accumulation of Adriamycin (ADM) and Mitoxantrone (MX), blocked Rh123 efflux, and made no change in the protein expression of P-gp and BCRP. Importantly, coadministration of 21 can significantly improve the oral bioavailability of paclitaxel (PTX). It was also demonstrated that 21 significantly inhibited the growth of K562/A02 xenograft tumors by increasing the sensitivity of ADM in vivo. In summary, 21 has the potential to overcome MDR caused by P-gp and BCRP and to improve the oral bioavailability of PTX.