Chemistry Department, Faculty of Sciences, University of Sharjah, Sharjah 27272, UAE.
Drug Exploration & Development Chair (DEDC), Pharmaceutical Chemistry Department, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.
Molecules. 2019 May 29;24(11):2054. doi: 10.3390/molecules24112054.
A series of 16-(α-alkoxyalkane)-17-hydrazino-estra-1(10),2,4-trien[17,16-c]-3-ol (-) and estra-1(10),2,4-trien-[17,16-c]pyrazoline-3-ol derivatives (-) were synthesized from corresponding arylidines which was prepared from estrone as starting material. Condensation of 1 with aldehydes gave the corresponding arylidine derivatives which were treated with hydrazine derivatives in alcohols to give the corresponding derivatives -, respectively. Additionally, treatment of with methyl- or phenylhydrazine in ethanolic potassium hydroxide afforded the corresponding N-substituted pyrazoline derivatives -, respectively. All these derivatives showed potent anti-ovarian cancer both in vitro and in vivo The mechanism of anti-ovarian cancer was suggested to process via topoisomerase II and BRAF inhibition.
一系列 16-(α-烷氧基烷烃)-17-肼基雌甾-1(10)，2，4-三烯[17,16-c]-3-醇(-)和雌甾-1(10)，2，4-三烯-[17,16-c]吡唑啉-3-醇衍生物(-)是由相应的芳基亚胺合成的，这些芳基亚胺是由雌酮作为起始原料制备的。1 与醛缩合得到相应的芳基亚胺衍生物(-)，然后在醇中用肼衍生物处理，分别得到相应的衍生物(-)。此外，用甲肼或苯肼在乙醇氢氧化钾中处理可分别得到相应的 N-取代吡唑啉衍生物(-)。所有这些衍生物都表现出强大的抗卵巢癌的活性，无论是在体外还是体内。抗卵巢癌的机制被认为是通过拓扑异构酶 II 和 BRAF 抑制。
