[EN] QUINOLINONE DERIVATIVES AS METHIONINE ADENOSYLTRANSFERASE 2A INHIBITORS [FR] DÉRIVÉS DE QUINOLINONE EN TANT QU'INHIBITEURS DE LA MÉTHIONINE ADÉNOSYLTRANSFÉRASE 2A
摘要:
本文披露了某些 Formula (A) 的喹啉酮衍生物,这些衍生物是蛋氨酸腺苷转移酶 2A(MAT2A)抑制剂。还披露了包含这些化合物的药物组合物以及治疗通过抑制 MAT2A 可治疗的疾病的方法,如癌症,包括其特征为甲硫腺苷磷酸化酶(MTAP)活性降低或缺乏的癌症。
Regioselective Ring Expansion of Isatins with <i>In Situ</i> Generated α-Aryldiazomethanes: Direct Access to Viridicatin Alkaloids
作者:Yellaiah Tangella、Kesari Lakshmi Manasa、Namballa Hari Krishna、B. Sridhar、Ahmed Kamal、Bathini Nagendra Babu
DOI:10.1021/acs.orglett.8b01417
日期:2018.6.15
A novel efficient one-pot regioselective ring-expansion reaction of isatins with in situ generated α-aryl/heteroaryldiazomethanes for the construction of viridicatin alkaloids has been described under metal-free conditions. The utility of this protocol is further demonstrated in the synthesis of naturally occurring viridicatin, viridicatol, and substituted 3-O-methyl viridicatin and their scale up