Ahmad Irshad
Department of Mathematics and Natural Sciences, School of Arts and Sciences, American University of Ras Al Khaimah, Ras Al Khaimah, United Arab Emirates.
Eur J Med Chem. 2018 Jan 1;143:515-531. doi: 10.1016/j.ejmech.2017.11.056. Epub 2017 Nov 24.
Tamoxifen (ICI 46 474), trans-1-(4-β-dimethylaminoethoxyphenyl)-1,2-diphenylbut-1-ene, is the most commonly used drug for the treatment of estrogen receptor positive breast cancer and has been saving lives worldwide for the past four decades. Tamoxifen is considered a pioneering drug due to its ubiquitous use in both treatment and chemoprevention of breast cancer and also for research addressing novel selective estrogen receptor modulators (SERMs). Tamoxifen is cost effective, lifesaving, and devoid of major side effects in the majority of patients. The discovery of tamoxifen metabolites such as 4-hydroxy tamoxifen, N-desmethyl tamoxifen, and endoxifen has facilitated understanding of tamoxifen's and its metabolites' mechanisms of action in breast cancer therapy. Continuous efforts are being made by both industry and academia to synthesize novel tamoxifen derivatives in order to better understand the mechanism of this drug's action and to generate new agents with reduced side effects for many therapeutic targets. This review article comprises the tamoxifen derivatives reported in the literature in the last few years and we anticipate that it will assist medicinal chemists in the synthesis of novel and pharmacologically potent agents for various therapeutic targets.
他莫昔芬（ICI 46474），反式-1-（4-β-二甲基氨基乙氧基苯基）-1,2-二苯基丁-1-烯，是治疗雌激素受体阳性乳腺癌最常用的药物，在过去四十年里拯救了世界各地许多人的生命。他莫昔芬被认为是一种开创性药物，因为它在乳腺癌的治疗和化学预防中广泛使用，同时也用于新型选择性雌激素受体调节剂（SERM）的研究。他莫昔芬具有成本效益、能挽救生命，并且在大多数患者中没有严重副作用。他莫昔芬代谢物如4-羟基他莫昔芬、N-去甲基他莫昔芬和内昔芬的发现，有助于理解他莫昔芬及其代谢物在乳腺癌治疗中的作用机制。制药行业和学术界都在不断努力合成新型他莫昔芬衍生物，以便更好地理解这种药物的作用机制，并开发出副作用更小、适用于多种治疗靶点的新药物。这篇综述文章涵盖了过去几年文献中报道的他莫昔芬衍生物，我们预计它将有助于药物化学家合成针对各种治疗靶点的新型、具有药理活性的药物。
