CAJ | 학술논문

设计和合成了一些4＇-和5＇-取代的17-(2＇-噁唑基)-雄甾-5,16-二烯衍生物作为17α-羟化酶/C17,20-裂解酶(P45017α)的抑制剂,用以治疗前列腺癌.药理筛选结果表明,化合物6C,即17-(2＇-噁唑基)-雄甾-5,16-二烯-3-醇为强的抑制剂,其活性可与欲进入临床I期的标准对VN85相当.在噁唑基4＇或5＇位上甲基或苯基基团的引入降低了生物活性.如预期所料,其3-醋酸酯5a～c和8的体外活性要弱于其相应的3-羟基物6a～c和9.化合物6c的深入药理实验在进行中.
설계화합성료일사4＇-화5＇-취대적17-(2＇-오서기)-웅치-5,16-이희연생물작위17α-간화매/C17,20-렬해매(P45017α)적억제제,용이치료전렬선암.약리사선결과표명,화합물6C,즉17-(2＇-오서기)-웅치-5,16-이희-3-순위강적억제제,기활성가여욕진입림상I기적표준대VN85상당.재오서기4＇혹5＇위상갑기혹분기기단적인입강저료생물활성.여예기소료,기3-작산지5a～c화8적체외활성요약우기상응적3-간기물6a～c화9.화합물6c적심입약리실험재진행중.
Several 4＇- and 5'-substituted 17-(2＇-oxazolyl)-androsta-5,16-diene derivatives were designedand synthesized as inhibitors of 17α-hydroxylase/C17,20 -Lyase (P45017α) for the treatment of prostatic cancer, thediene-3-ol was a strong inhibitor, comparable with that of the reference compound VN-85. The introduction ofacetate 5a～c and 8 were lower than their 3-ol counterparts 6a～c and 9 as expected. The further pharmacologicalstudy of 6c is in progress.