Aso K, Hitaka T, Yukishige K, Ootsu K, Akimoto H
Pharmaceutical Research Laboratories III, Takeda Chemical Industries, Ltd., Osaka, Japan.
Chem Pharm Bull (Tokyo). 1995 Feb;43(2):256-61. doi: 10.1248/cpb.43.256.
Novel pyrrolo[2,3-d]pyrimidine antifolates (1a, b and 2a, b) with a nitrogen atom in the bridge chain between the 2,4-diaminopyrrolo[2,3-d]pyrimidine and phenylene rings were designed and efficiently synthesized. These compounds exhibited more potent inhibitory activities than methotrexate (MTX) against the proliferation of human epidermoid carcinoma KB cells and human non-small cell lung carcinoma A549 cells despite their modest dihydrofolate reductase (DHFR)-inhibitory potency.
设计并高效合成了在2,4-二氨基吡咯并[2,3 - d]嘧啶与亚苯基环之间的桥链中含有氮原子的新型吡咯并[2,3 - d]嘧啶抗叶酸剂（1a、b和2a、b）。尽管这些化合物的二氢叶酸还原酶（DHFR）抑制活性适中，但它们对人表皮样癌KB细胞和人非小细胞肺癌A549细胞的增殖表现出比甲氨蝶呤（MTX）更强的抑制活性。
