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Androgen receptor micromolecular fluorescent probe as well as preparation method and application thereof

A technology of androgen receptor and fluorescent probe, applied in the field of androgen receptor small molecule fluorescent probe and its preparation, can solve the problems of high saturated drug concentration and drug resistance

Inactive Publication Date: 2021-10-08
NANJING FIRST HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are still defects in the currently marketed drugs: as: (1) 20% to 40% of patients are unresponsive to existing AR antagonists; (2) AR antagonists require very high saturation drug concentrations to realize their clinical benefits , which is also a major challenge in the current drug development process; (3) long-term drug resistance will inevitably produce drug resistance; (4) AR splice variants lacking the AR-LBD region exist in about 75% of clinical samples7 (ARV7); (5) AR overexpression and other AR signaling mechanisms

Method used

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  • Androgen receptor micromolecular fluorescent probe as well as preparation method and application thereof
  • Androgen receptor micromolecular fluorescent probe as well as preparation method and application thereof
  • Androgen receptor micromolecular fluorescent probe as well as preparation method and application thereof

Examples

Experimental program
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Embodiment 1F

[0025] The synthesis of embodiment 1FITC-enzalutamide (Probe-1)

[0026] Add T1 (20g, 0.048mol) into a mixed solution of 40mL isopropyl acetate and 8mL DMSO, stir at room temperature until dissolved, add T-2 (44g, 0.20mol) after complete dissolution, heat the oil bath to 80°C, 80°C React for 14 hours, TLC detects that when the fluorescence intensity of the raw material point is similar to that of the product point, stop heating, wait for the reaction solution to drop to room temperature, wash three times with 150 mL of water, three times with 150 mL of saturated saline, dry over anhydrous sodium sulfate, and distill off the solvent under reduced pressure. The obtained oily substance was completely dissolved in 100mL of methanol, and the pH of the reaction solution was adjusted to 2-3 with 5N HCl. The oil bath was heated to reflux. TLC detected that the reaction was complete, and the heating was stopped. After the reaction solution dropped to room temperature, the solvent was di...

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Abstract

The invention discloses an androgen receptor micromolecular fluorescent probe as well as a preparation method and application thereof. The structural formula of the micromolecular fluorescent probe is shown as a formula (I). The androgen receptor micromolecular fluorescent probe disclosed by the invention has a fluorescence characteristic and has better specific binding to an androgen receptor. The compound is used as a fluorescence polarization probe, screening of androgen receptor antagonists or agonists and evaluation of ligand affinity can be achieved through a competitive binding method, and a basis is provided for subsequent androgen receptor targeted drug design.

Description

technical field [0001] The invention relates to an androgen receptor small-molecule fluorescent probe, a preparation method and application thereof, and belongs to the technical field of androgen receptor small-molecule fluorescent probes. Background technique [0002] Prostate cancer (PCa) is a malignant tumor of the genitourinary system in elderly men with high morbidity and mortality. The incidence of prostate cancer in my country is increasing year by year, and its morbidity and fatality rate are now the first in male genitourinary system tumors, and most patients are already in the advanced stage when they are first diagnosed. Among them, androgen and androgen receptor (AR) play a key role in the occurrence and development of prostate cancer. The androgen receptor (AR) belongs to the steroid receptor in the nuclear receptor superfamily and is a ligand-dependent trans-transcriptional regulatory protein. The human AR gene has a full length of about 90kb, a molecular mas...

Claims

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Application Information

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IPC IPC(8): C07D493/10C09K11/06G01N21/64G01N33/74
CPCC07D493/10C09K11/06G01N21/6428G01N21/6445G01N33/74C09K2211/1044C09K2211/1088
Inventor 杜前明刘超胡容卞金磊顾延庆姚懿琴
Owner NANJING FIRST HOSPITAL
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