Pyrrolopyrazinone derivatives for treatment of triple-negative breast cancer and process of preparation thereof

• Main Authors: JUNG YOUNG SUK, LIM SOO BIN, KWAK JAE HWAN, KWON YE MI, KIM YE JIN
• Format: Patent
• Language: English; Korean
• Published: 12.03.2021
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The present disclosure relates to a pyrrolopyrazinone derivative with high target selectivity for triple-negative breast cancer, and a method for manufacturing the same. Moe specifically, the pyrrolopyrazinone derivative of the present disclosure has improved that the target selectivity of a conventional pyrazinoindolone derivative is not high. The pyrrolopyrazinone derivative having high target selectivity has an effect of inhibiting the expression of the proliferation signaling protein in MDA-MB-468 cells and inducing the expression of the death signaling protein, thereby having a stronger triple-negative breast cancer cell inhibitory effect than gefitinib. 본 개시내용의 삼중음성유방암에 표적선택성이 높은 파이롤로피라지논 유도체 및 이의 제조방법에 관한 것이다. 보다 구체적으로, 본 개시내용의 파이롤로피라지논 유도체는 종래 피라지노인돌론 유도체가 표적선택성이 높지 않다는 점을 개선하였다. 높은 표적선택성을 가지는 상기 파이롤로피라지논 유도체는 MDA-MB-468 세포의 증식 신호전달 단백질의 발현을 억제하고 사멸신호전달 단백질의 발현을 유도하는 효과가 있어, 제피티닙보다 강력한 삼중음성유방암 세포 억제효과가 있다.