Mawdsley E A, Berlin K D, Chesnut R W, Durham N N
J Med Chem. 1976 Feb;19(2):239-43. doi: 10.1021/jm00224a008.
Pyrazole-, isoxazole-, and pyrazolone-containing systems were prepared from 3,4-dihydro-5,6,7-trimethoxy-1(2H)-naphthalenone, 3,4-dihydro-6,7,8-trimethoxy-1(2H)-naphthalenone, and 3,4-dihydro-6,7,8-trimethoxy-1(2H)-phenanthrone. Primarily, the pyrazoles displayed inhibition of growth in the microbial screens and in tissue culture. Correlation of the heteroatom distances between the oxygen atoms of two methoxy groups and a nitrogen atom in the pyrazole function with the percent plating efficiency on KB cell growth suggests increased inhibition as the (OA-N)/(OB-N) ratio deviates from one. No trend was observed in relating the OA-N-OB angle and activity for the examples studied.
含吡唑、异恶唑和吡唑啉酮的体系由3,4-二氢-5,6,7-三甲氧基-1(2H)-萘酮、3,4-二氢-6,7,8-三甲氧基-1(2H)-萘酮和3,4-二氢-6,7,8-三甲氧基-1(2H)-菲酮制备而成。首先，吡唑类化合物在微生物筛选和组织培养中表现出对生长的抑制作用。吡唑官能团中两个甲氧基的氧原子与一个氮原子之间的杂原子距离与KB细胞生长的平板接种效率百分比之间的相关性表明，随着(OA-N)/(OB-N)比值偏离1，抑制作用增强。在所研究的实例中，未观察到OA-N-OB角与活性之间的相关性。
